lgnd-20201231

UNITED STATES

SECURITIES AND EXCHANGE COMMISSION

Washington, D.C. 20549

_____________________________________________________________________________________________

FORM 10-K

_____________________________________________________________________________________________

For the Fiscal Year Ended December 31, 2020

For the transition period from to .

Commission File No. 001-33093

LIGAND PHARMACEUTICALS INCORPORATED

(Exact name of registrant as specified in its charter)

3911 Sorrento Valley Boulevard, Suite 110

San Diego

(Address of Principal Executive Offices) (Zip Code)

Registrant’s telephone number, including area code: (858) 550-7500

Securities registered pursuant to Section 12(b) of the Act:

Title of Each Class Trading Symbol Name of Each Exchange on Which Registered

Common Stock, par value $.001 per share LGND The Nasdaq Global Market

Securities registered pursuant to Section 12(g) of the Act:

None

Indicate by check mark if the registrant is a well-known seasoned issuer, as defined in Rule 405 of the Securities Act. Yes ☒ No ☐

Indicate by check mark if the registrant is not required to file reports pursuant to Section 13 or Section 15(d) of the Securities Exchange Act of 1934. Yes ☐ No ☒

Indicate by check mark whether the registrant: (1) has filed all reports required to be filed by Section 13 or 15(d) of the Securities Exchange Act of 1934 during the preceding 12 months (or for such shorter period that the registrant was required to file such reports), and (2) has been subject to such filing requirements for the past 90 days. Yes☒ No ☐

Indicate by check mark whether the registrant has submitted electronically every Interactive Data File required to be submitted pursuant to Rule 405 of Regulation S-T (§ 232.405 of this chapter) during the preceding 12 months (or for such shorter period that the registrant was required to submit such files). Yes☒ No ☐

Indicate by check mark whether the registrant is a large accelerated filer, an accelerated filer, a non-accelerated filer, a smaller reporting company or an emerging growth company. See the definition of “large accelerated filer,” “accelerated filer,” “smaller reporting company” and "emerging growth company" in Rule 12b-2 of the Exchange Act.

If an emerging growth company, indicate by check mark if the registrant has elected not to use the extended transition period for complying with any new or revised financial accounting standards provided pursuant to Section 13(a) of the Exchange Act. ☐

Indicate by check mark whether the registrant has filed a report on and attestation to its management’s assessment of the effectiveness of its internal control over financial reporting under Section 404(b) of the Sarbanes-Oxley Act (15 U.S.C. 7262(b)) by the registered public accounting firm that prepared or issued its audit report. ☒

Indicate by check mark whether the registrant is a shell company (as defined in Exchange Act Rule 12b-2 of the Exchange Act). Yes ☐ No ☒

The aggregate market value of the Registrant’s voting and non-voting stock held by non-affiliates was approximately $1.2 billion based on the last sales price of the Registrant’s Common Stock on the Nasdaq Global Market of the Nasdaq Stock Market LLC on June 30, 2020. For purposes of this calculation, shares of Common Stock held by directors, officers and 10% stockholders known to the Registrant have been deemed to be owned by affiliates which should not be construed to indicate that any such person possesses the power, direct or indirect, to direct or cause the direction of the management or policies of the Registrant or that such person is controlled by or under common control with the Registrant.

As of February 18, 2021, the Registrant had 16,612,422 shares of Common Stock outstanding.

DOCUMENTS INCORPORATED BY REFERENCE

Portions of the Proxy Statement for the Registrant’s 2021 Annual Meeting of Stockholders to be filed with the Commission within 120 days of December 31, 2020 are incorporated by reference in Part III of this Annual Report on Form 10-K. With the exception of those portions that are specifically incorporated by reference in this Annual Report on Form 10-K, such Proxy Statement shall not be deemed filed as part of this Report or incorporated by reference herein.

Table of Contents

Part I

Item 1. Business 1

Item 1A. Risk Factors 28

Item 1B. Unresolved Staff Comments 40

Item 2. Properties 40

Item 3. Legal Proceedings 40

Item 4. Mine Safety Disclosures 40

Part II

Item 6. Selected Consolidated Financial Data 43

Item 7A. Quantitative and Qualitative Disclosures About Market Risk 51

Item 8. Consolidated Financial Statements and Supplementary Data 52

Item 9A. Controls and Procedures 97

Item 9B. Other Information 97

Part III

Item 10. Directors, Executive Officers and Corporate Governance 100

Item 11. Executive Compensation 100

Item 14. Principal Accountant Fees and Services 100

Part IV

Item 15. Exhibits, Financial Statement Schedules 101

GLOSSARY OF TERMS AND ABBREVIATIONS

Abbreviation Definition

AAALAC Accreditation of Laboratory Animal Care International

Ab Initio Ab Initio Biotherapeutics, Inc.

Abvivo Abvivo, LLC

ACOVA ACOVA, Inc.

ADHF Acute decompensated heart failure

Aldeyra Aldeyra Therapeutics, Inc.

Amgen Amgen, Inc.

ANDA Abbreviated New Drug Application

API Active pharmaceutical ingredient

Aptevo Aptevo Therapeutics

Arcus Arcus Biosciences, Inc.

ASC Accounting Standards Codification

ASCO American Society of Clinical Oncology

ASCT Autologous Stem Cell Transplantation

ASU Accounting Standards Update

Aurobindo Aurobindo Pharma Ltd

Aziyo Aziyo Med, LLC

Baxter Baxter International, Inc.

BeiGene BeiGene Switzerland GmbH

BendaRx BendaRx Corp.

Bexson Biomedical Bexson Biomedical, Inc.

BLA Biologics license application

CStone CStone Pharmaceuticals (Suzhou) Co., Ltd.

CASI CASI Pharmaceuticals, Inc.

Cardioxyl Cardioxyl Pharmaceuticals, Inc.

CI-AKI Contrast-induced acute kidney injury

Code of Conduct Code of Conduct and Ethics Policy

Coherus Coherus Biosciences, Inc.

CoM Composition of Matter

Company Ligand Pharmaceuticals Incorporated, including subsidiaries

Convertible Note Senior Convertible Promissory Note

COPD Chronic obstructive pulmonary disease

Cormatrix Cormatrix Cardiovascular, Inc.

Cormatrix Asset Sale Asset sale from CorMatrix to Aziyo

Corvus Corvus Pharmaceuticals, Inc.

COSO Committee of Sponsoring Organizations of the Treadway Commission

CRO Contract Research Organization

Crystal Crystal Bioscience, Inc.

Cumulus Cumulus Oncology, Ltd.

CVR Contingent value right

CyDex CyDex Pharmaceuticals, Inc.

Daiichi Sankyo Daiichi Sankyo Company, Ltd.

Dianomi Dianomi Therapeutics, Inc.

DMF Drug Master File

ESG Environmental, Social and Governance

Eisai Eisai Inc.

Eli Lilly Eli Lilly and Company

ECM Extracellular matrix

EPA Environmental Protection Agency

ESPP Employee Stock Purchase Plan, as amended and restated

EU European Union

Exelixis Exelixis, Inc.

FASB Financial Accounting Standards Board

FDA Food and Drug Administration

FSGS Focal segmental glomerulosclerosis

GAAP Generally accepted accounting principles in the United States

GBM Glioblastoma

Genagon Genagon Therapeutics AB

GCSF Granulocyte-colony stimulating factor

GigaGen GigaGen, Inc.

Gilead Gilead Sciences, Inc.

GPCR G-protein coupled receptor

GRA Glucagon receptor antagonist

HanAll HanAll Biopharma Co., Ltd.

Harbour Harbour BioMed Shanghai Co., Ltd.

HBV Hepatitis B Virus

HCC Hepatocellular Carcinoma

Hikma Hikma Pharmaceuticals PLC

HNO Nitroxyl

Hovione Hovione FarmCiencia, S.A.

Icagen Icagen, Inc.

IPR&D In-Process Research and Development

IRAK4 Interleukin-1 Receptor Associated Kinase-4

IRS Internal Revenue Service

IV Intravenous

iMBP iMetabolic Biopharma Corporation

Immunovant Immunovant Sciences GmbH

IND Investigational New Drug

Kira Pharma Kira Pharmaceuticals Ltd.

KSQ Therapeutics KSQ Therapeutics, Inc.

Ligand Ligand Pharmaceuticals Incorporated, including subsidiaries

LTP Liver targeting prodrug

Lundbeck Lundbeck A/S

Marinus Marinus Pharmaceuticals, Inc.

MCM Mineral Coated Microparticle

Melinta Melinta Therapeutics, Inc.

Merck Merck & Co., Inc.

Merrimack Merrimack Pharmaceuticals, Inc.

Metabasis Metabasis Therapeutics, Inc.

Metavant Metavant Sciences Ltd.

Millennium Millennium Pharmaceuticals, Inc.

MLA Master License Agreement

MRSA Methicillin-resistant Staphylococcus aureu

NASH Non-alcoholic steatohepatitis

NDA New Drug Application

NOLs Net Operating Losses

Novan Novan, Inc.

Novartis Novartis AG

Nucorion Nucorion Pharmaceuticals, Inc.

OMT Open Monoclonal Technology, Inc.

Ono Ono Pharmaceutical Co., Ltd.

Opthea Opthea Limited

Palvella Palvella Therapeutics, Inc.

Par Par Pharmaceutical, Inc.

Pfenex Pfenex Inc.

Pfizer Pfizer, Inc.

PFS Progression-free Survival

Pharmacopeia Pharmacopeia, Inc.

Phoenix Tissue Phoenix Tissue Repair

PhoreMost PhoreMost Limited

PPD Post-Partum Depression

PSU Performance stock unit

R&D Research and Development

Roivant Roivant Sciences GMBH

RSU Restricted stock unit

SAGE Sage Therapeutics, Inc.

SARM Selective Androgen Receptor Modulator

SEC Securities and Exchange Commission

Sedor Sedor Pharmaceuticals, Inc., or RODES, Inc.

Seelos Seelos Therapeutics, Inc.

Selexis Selexis, SA

Sermonix Sermonix Pharmaceuticals, LLC

SII Serum Institute of India

Spectrum Spectrum Pharmaceuticals, Inc.

SQ Innovation SQ Innovation, Inc.

Sunshine Lake Pharma Sunshine Lake Pharma Co., Ltd.

Takeda Takeda Pharmaceuticals Company Limited

Talem Talem Therapeutics LLC

Taurus Taurus Biosciences LLC

Tax Act The Tax Cuts and Jobs Act

TG Therapeutics TG Therapeutics, Inc.

Travere Travere Inc.

TR-Beta Thyroid hormone receptor beta

Valanbio Valanbio Therapeutics, Inc.

VDP Vernalis Design Platform

VentiRx VentiRx Pharmaceuticals, Inc.

Vernalis Vernalis plc

Verona Verona Pharma plc

Viking Viking Therapeutics

Vireo Vireo Health

WuXi WuXi Biologics Ireland Limited

Xi'an Xintong Xi'an Xintong Medicine Research

X-ALD X-linked adrenoleukodystrophy

xCella Biosciences xCella Biosciences, Inc.

Zydus Cadila Zydus Cadila Healthcare, Ltd

PART I

Cautionary Note Regarding Forward-Looking Statements:

You should read the following report together with the more detailed information regarding our company, our common stock and our financial statements and notes to those statements appearing elsewhere in this document.

This report contains forward-looking statements that involve a number of risks and uncertainties. Although our forward-looking statements reflect the good faith judgment of our management, these statements can only be based on facts and factors currently known by us. Consequently, these forward-looking statements are inherently subject to risks and uncertainties, and actual results and outcomes may differ materially from results and outcomes discussed in the forward-looking statements.

Forward-looking statements can be identified by the use of forward-looking words such as “believes,” “expects,” “may,” “will,” “plan,” “intends,” “estimates,” “would,” “continue,” “seeks,” “pro forma,” or “anticipates,” or other similar words (including their use in the negative), or by discussions of future matters such as those related to our future results of operations and financial position, royalties and milestones under license agreements, Captisol material sales, product development, and product regulatory filings and approvals, and the timing thereof, as well as other statements that are not historical. You should be aware that the occurrence of any of the events discussed under the caption “Risk Factors” could negatively affect our results of operations and financial condition and the trading price of our stock.

The cautionary statements made in this report are intended to be applicable to all related forward-looking statements wherever they may appear in this report. We urge you not to place undue reliance on these forward-looking statements, which speak only as of the date of this report. Except as required by law, we assume no obligation to update our forward-looking statements, even if new information becomes available in the future. This caution is made under the safe harbor provisions of Section 21E of the Securities Exchange Act of 1934, as amended.

References to “Ligand Pharmaceuticals Incorporated,” “Ligand,” the “Company,” “we,” “our” and “us” include Ligand Pharmaceuticals Incorporated and our wholly-owned subsidiaries.

Partner Information

Information regarding partnered products and programs comes from information publicly released by our partners and licensees.

Trademarks

Our trademarks, trade names and service marks referenced herein include Ligand®, Captisol®, LTPTM, LTP TechnologyTM, OmniAb®, OmniMouse®, OmniRat®, OmniFlic®, OmniClicTM, OmniChicken®, xCella®, xCella Biosciences®, xPloration®, IcagenTM, Pfenex Expression Technology® and XRPro® which are protected under applicable intellectual property laws and are our property. All other trademarks, trade names and service marks including Kyprolis®, Evomela®, Veklury®, Livogiva®, Zulresso®, Minnebro®, Baxdela®, CarnexivTM, ConbrizaTM, and Duavee®, are the property of their respective owners. Solely for convenience, trademarks, trade names and service marks referred to in this report may appear without the ®, TM or SM symbols, but such references are not intended to indicate, in any way, that we will not assert, to the fullest extent under applicable law, our rights or the right of the applicable licensor to such trademarks, trade names and service marks. Use or display by us of other parties’ trademarks, trade dress or products is not intended to and does not imply a relationship with, or endorsement or sponsorship of, us by the trademark or trade dress owners.

Item 1. Business

Overview

We are a biopharmaceutical company focused on developing or acquiring technologies that help pharmaceutical companies discover and develop medicines. We employ research technologies such as antibody discovery technologies, ion channel discovery technology, Pseudomonas fluorescens protein expression technology, formulation science and liver targeted pro-drug technologies to assist companies in their work toward securing prescription drug and biologic approvals. We currently have partnerships and license agreements with over 130 pharmaceutical and biotechnology companies. Over 300 programs are in various stages of commercialization, development or research and are fully funded by our collaboration partners and licensees. We have contributed novel research and technologies for approved medicines that treat cancer, osteoporosis, fungal infections and postpartum depression, among others. Our collaboration partners and licensees have programs currently in clinical development targeting cancer, seizure, diabetes, cardiovascular disease, muscle wasting, liver disease, and kidney disease, among others. We have over 1,400 issued patents worldwide.

We have assembled our large portfolio of fully-funded programs either by licensing our own proprietary drug development programs, licensing our platform technologies such as Captisol or OmniAb to partners for use with their proprietary programs, or acquiring existing partnered programs from other companies. Fully-funded programs, which we refer to as "shots on goal," are those for which our partners pay all of the development and commercialization costs. For our internal programs, we generally plan to advance drug candidates through early-stage drug development or clinical proof-of-concept and then seek partners to continue development and potential commercialization.

Our business model creates value for stockholders by providing a diversified portfolio of biotech and pharmaceutical product revenue streams that are supported by an efficient and low corporate cost structure. Our goal is to offer investors an opportunity to participate in the promise of the biotech industry in a profitable, diversified and lower-risk business than a typical biotech company. Our business model is based on doing what we do best: drug discovery, early-stage drug development, product reformulation and partnering. We partner with other pharmaceutical companies to leverage what they do best (late-stage development, regulatory management and commercialization) to ultimately generate our revenue. We believe that focusing on discovery and early-stage drug development while benefiting from our partners’ development and commercialization expertise will reduce our internal expenses and allow us to have a larger number of drug candidates progress to later stages of drug development.

Our revenue consists of three primary elements: royalties from commercialized products, sale of Captisol material, and contract revenue from license, milestone and other service payments. In addition to discovering and developing our own proprietary drugs, we selectively pursue acquisitions to bring in new assets, pipelines, and technologies to aid in generating additional potential new revenue streams.

Impact of COVID-19 Pandemic

Please see impact of COVID-19 pandemic described in Item 8. Consolidated Financial Statements -Note 1, “Basis of Presentation and Summary of Significant Accounting Policies”. For additional information on the various risks posed by COVID-19 pandemic, please read Item 1A. Risk Factors included in this report.

2020 and Recent Major Business Highlights

Major Transactions and Strategic Investments

Consistent with our business model, we pursued novel investments to augment our technology platforms and assets.

In April 2020, we closed the acquisition of the core assets, partnered programs and ion channel technology from Icagen for $15.1 million in cash. Icagen will also be entitled to receive up to an additional contingent earn-out payment of $25 million based on certain revenue achievements.

In September 2020, we acquired two privately held companies that strengthen and complement our OmniAb platform's technology stack. We acquired xCella Biosciences, Inc. for $7.1 million in cash plus potential earnouts, and acquired Taurus Biosciences LLC for $5.1 million in cash plus non-transferable CVRs. In addition, we invested $2.5 million in a new company,

Minotaur Therapeutics, which is led by Taurus Biosciences’ founder, in exchange for royalties on products from future programs.

In October 2020, we acquired Pfenex Inc. including its proprietary protein expression technology and existing collaboration contracts with Jazz Pharmaceuticals, Merck, Serum Institute of India and Alvogen, each of which has the potential to pay royalties. In October 2020, our partner Merck announced additional positive data from two Phase 3 studies with V114, which uses the protein expression technology, evaluating the safety, tolerability and immunogenicity of the investigational 15-valent pneumococcal conjugate vaccine. In November 2020, Merck announced they had submitted applications to the U.S. FDA and European Medicines Agency (EMA) for licensure of V114 for use in adults 18 years of age and older. Merck announced on January 12, 2021 that FDA accepted the BLA for V114 for priority review with a Prescription Drug User Fee Act (PDUFA) date of July 18, 2021. In December 2020, Jazz Pharmaceuticals initiated the submission of a BLA to the FDA seeking market approval for JZP-458, which is a recombinant Erwinia asparaginase produced using the protein expression platform that has resulted in a robust process showing manufacturing consistency and efficiency. The BLA was initiated and will be reviewed under the Real-Time Oncology Review (RTOR) pilot program, an initiative of the FDA's Oncology Center of Excellence designed to expedite the delivery of safe and effective cancer treatments to patients.

In December 2020, we sold the Vernalis research operations and internal programs to HitGen Inc. for $26.7 million in cash. Under the terms of the agreement, we retained economic rights on completed collaboration licenses as well as a share of the economic rights on current research collaboration contracts.

Corporate and Governance Highlights

We are committed to policies and practices focused on environmental sustainability, positively impacting our social community and maintaining and cultivating good corporate governance. By focusing on such ESG policies and practices, we believe we can affect a meaningful and positive change in our community and maintain our open, collaborative corporate culture. We will continue our proactive shareholder and employee engagement in 2021. See www.ligand.com for information about our ESG policies and practices.

OmniAb Technology Platform Updates

We continue to invest in and expand the OmniAb Technology platform. We entered into four new OmniAb platform license agreements in 2020 with Pandion Therapeutics, Adept Therapeutics, The Wistar Institute and RubrYc Therapeutics. In addition to the four platform license deals completed in 2020, we estimate that we and our partners initiated over 50 new programs in 2020.Our scientists and our partners presented data highlighting the utility of the OmniAb platform at multiple conferences throughout the year, and we published multiple papers in peer-reviewed journals.

Development-stage OmniAb partners continue to report progress clinically; notable advancements include:

•Janssen presented safety and response data of the OmniAb-derived teclistamab (anti-BCMA x CD3 T cell redirecting bispecific antibody) Phase 1 dose escalation trial for relapsed/refractory multiple myeloma at the 2020 American Society for Hematology (ASH) conference. Teclistamab showed a manageable safety profile with an overall response rate (ORR) of 73 percent (16/22) at the recommended subcutaneous (SC) Phase 2 dose. In addition, updated results for the intravenous formulation demonstrate the durability of responses. Janssen announced that it has chosen the recommended Phase 2 dose for the SC formulation.

•Gloria Biosciences submitted an application for marketing approval in China for OmniAb-derived zimberelimab for the treatment of classical Hodgkin lymphoma, marking multiple OmniAb drug applications filed seeking approval.

•Arcus Biosciences and Taiho Pharmaceutical announced Taiho’s exercise of its option for an exclusive license to zimberelimab (also known as AB122) for Japan and other Asian countries, excluding China.

•CStone announced an agreement to out-license ex-Greater China rights for sugemalimab (CStone licensed worldwide rights from our licensee WuXi) and CS1003 (anti-PD-1) to EQRx. Under the terms of the agreement, CStone will receive an upfront payment of $150 million and is eligible to receive up to $1.15 billion in milestone payments as well as separate tiered royalties. EQRx will obtain exclusive rights to lead development and commercialization worldwide, excluding certain territories in Asia. In October 2020, CStone entered into a major partnership with Pfizer for the commercialization of sugemalimab in greater China. As part of the partnership, Pfizer invested $200 million in CStone shares, and CStone is eligible to receive up to $280 million in milestone payments and additional royalties.

•CStone announced that China’s National Medical Products Administration accepted CStone’s New Drug Application for sugemalimab combined with chemotherapy for the first-line treatment of advanced squamous and non-squamous

non-small cell lung cancer (NSCLC). CStone previously announced updated results from two clinical studies of sugemalimab at the 2020 Chinese Society of Clinical Oncology Annual Meeting and announced that sugemalimab met the primary endpoint as first-line treatment in stage IV squamous and non-squamous NSCLC.

•CStone and Blueprint Medicines initiated a Phase 1b/2 clinical trial of fisogatinib in combination with OmniAb-derived CS1001 for patients with hepatocellular carcinoma. CStone announced the first patient was dosed in a proof-of-concept study of OmniAb-derived CS1001 in combination with Bayer's regorafenib in patients with advanced solid tumors.

•Aptevo announced two complete remissions in the ongoing APVO436 Phase 1/1b clinical trial for the treatment of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS). Preliminary data indicating that OmniAb-derived APVO436 was well tolerated with a manageable safety profile were presented at the 2020 ASH conference.

•Immunovant announced positive results from its Phase 2a proof-of-concept study of OmniAb-derived IMVT-1401 (also known as batoclimab, HL161, or HBM9161) in thyroid eye disease. IMVT-1401 is a novel investigational anti-FcRn antibody delivered by subcutaneous injection. The results showed a 65% mean reduction in total IgG observed from baseline to end of treatment, with a pharmacodynamic response nearly identical to modeled predictions for the dosing regimen tested in the trial. In February 2021, Immunovant announced a voluntary pause in its ongoing clinical trials of IMVT-1401 due to elevated total cholesterol and LDL levels in Phase 2b trial of thyroid eye disease. Immunovant announced that it plans to continue development of IMVT-1401 following discussions with regulators and protocol modifications. In addition, Immunovant announced positive topline results from a multicenter, placebo-controlled Phase 2a trial (ASCEND MG) of IMVT-1401, in patients with myasthenia gravis (MG).

•Harbour announced first patient dosing of Phase 1b/2a study of Batoclimab for treating neuromyelitis optica spectrum disorder. On January 27, 2021 Harbour announced that China Center for Drug Evaluation granted Breakthrough Therapy designation to Batoclimab for the treatment of adult patients with MG. This designation indicates that the development and review of Batoclimab in adults with MG will be expedited.

Captisol Technology Updates

Our Captisol business unit achieved its highest sales ever in 2020 and we anticipate substantial continued demand for Captisol. We are investing to significantly expand annual manufacturing capacity for Captisol.

Gilead utilizes Captisol to solubilize the active ingredient for Veklury® (remdesivir), the first FDA approved anti-viral treatment for severe COVID-19. The drug has now been authorized or approved for use in numerous countries around the world. Gilead announced the formation of a consortium of generic pharmaceutical companies to manufacture remdesivir for the developing world. We have supplied, established initial agreements or are in supply discussions with those companies, and are prepared to meet the Captisol needs of all companies manufacturing remdesivir as well as the needs from our other Captisol partners.

We made the decision to conduct a Phase 2 trial for Captisol-enabled Iohexol that we believe could serve as the basis for potential registration of the product candidate. CE-Iohexol is an iodine-based contrast agent for hospital-based imaging procedures. The market for iodinated contrast agents is substantial, with approximately 20 million imaging procedures per year in the U.S., representing an estimated $1.5 billion in sales. The objective of the CE-Iohexol clinical trial will be to demonstrate a reduction in the incidence of contrast-induced acute kidney injury and an equivalent image quality compared to GE’s Omnipaque®.

Vernalis Design Platform (VDP) Updates

In December 2020, we sold our Vernalis research operations and internal programs to HitGen Inc. for $26.7 million in cash. Under the terms of the agreement, we retain economic rights on completed collaboration licenses as well as a share of the economic rights on current research collaboration contracts. We continued to expand our portfolio of VDP-derived partnerships during 2020, prior to the sale. Notable VDP developments include:

•We entered into an exclusive worldwide license agreement with Neuritek Therapeutics to develop and commercialize V158866, a novel oral, selective fatty acid amide hydrolase inhibitor that was discovered using the Vernalis Design Platform. Neuritek plans to develop V158866 for post-traumatic stress disorder and other CNS diseases. Under the terms of the agreement, we received an upfront license fee and are eligible to receive over $240 million in milestones and tiered royalties on net sales of six to eight percent. Neuritek has secured approximately $27 million in a capital commitment from GEM Global Yield LLC SCS.

•In February 2021, Verona Pharma announced ensifentrine delivered by a pressurized metered-dose inhaler (pMDI) met all of the primary and secondary lung function endpoints in the 7 day, Phase 2 clinical trial in patients with moderate to severe chronic obstructive pulmonary disease (COPD). The magnitude of improvement in lung function was dose-ordered and highly statistically significant at peak and over the 12-hour dosing interval compared with placebo, and supports twice-daily dosing of ensifentrine via pMDI for the treatment of COPD. Verona is evaluating nebulized ensifentrine in the pivotal Phase 3 ENHANCE-1 and 2 clinical trials for COPD maintenance treatment.

Icagen Technology Platform Updates

We continue to advance partnership programs following our 2020 acquisition of the core assets from Icagen Inc. The following developments occurred in 2020:

•In May of 2020 we expanded our license with Roche by adding a second program to our agreement initiated in December 2018. This new program incorporates Icagen’s ion channel technology and is directed at a specific ion channel target relevant to neurodegenerative disease. Roche made a cash upfront payment and provides research funding to Icagen for this second program. In addition, Icagen is eligible to receive development and commercialization milestones up to $274 million for each program and royalty payments should a drug be commercialized from any of the collaboration’s programs.

•In December 2020, we signed a collaboration agreement with GlaxoSmithKline to identify and develop inhibitors of specific genetically-validated molecular targets relevant to neurological diseases. Under the terms of this agreement we received an upfront payment of $7 million and could receive development, regulatory and commercialization milestones up to $155 million. We will also receive tiered royalties on net sales should any drug from the collaboration be commercialized.

•We continue to advance other programs including our collaboration with the Cystic Fibrosis Foundation targeting nonsense suppression as well as multiple internal programs which potentially offer future partnering opportunities.

Other Business Updates

On February 2, 2021, our partner, Travere, announced that sparsentan achieved its pre-specified interim FSGS partial remission of proteinuria endpoint (FPRE) in the DUPLEX study after 36 weeks of treatment. Sparsentan demonstrated a statistically significant response on FPRE compared to the active control, irbesartan (p=0.0094). Preliminary results from the interim analysis suggest that sparsentan has been generally well-tolerated and has shown a comparable safety profile to irbesartan. Based on the data from the interim analysis, Travere intends to pursue submissions for accelerated approval of sparsentan for FSGS in the second half of 2021. In January the FDA granted sparsentan Orphan Drug Designation for the treatment of IgA nephropathy, and on February 18, 2021, Travere announced the European Commission (EC) had granted orphan designation to sparsentan for the treatment of IgA nephropathy. Topline efficacy data from the ongoing pivotal Phase 3 PROTECT Study in IgA nephropathy, and the 36-week interim proteinuria endpoint analysis, are anticipated in the third quarter of 2021.

Technologies

A variety of technology platforms that enable elements of drug discovery or development form the basis of our portfolio of fully-funded shots on goal. Platform technologies or individual drugs discovered by Ligand are related to a broad estate of intellectual property that includes over 1,400 patents issued worldwide.

OmniAb Technologies

The OmniAb antibody discovery platform provides our biopharmaceutical industry partners access to the most advanced antibody repertoires and state-of-the-art screening technologies to enable efficient discovery of next-generation novel therapeutics and to deliver the highest quality therapeutic antibody candidates for a wide range of human diseases.

At the heart of the OmniAb Technology Stack is the Biological IntelligenceTM (BI) of our proprietary and validated transgenic animals, including OmniRat, OmniChicken and OmniMouse, each capable of generating high quality fully human antibodies that have been optimized naturally through in vivo affinity maturation. OmniFlic (transgenic rat) and OmniClic (transgenic chicken) address industry needs for bispecific antibody applications though a common light chain approach, and OmniTaur features unique structural attributes of cow antibodies for complex targets. Our transgenic animals comprise the most diverse host systems available in the industry and they are optimally leveraged within the OmniAb Technology Stack through AI-enhanced antigen design and immunization methods, paired with high-throughput and microfluidic-based single B cell

screening and deep computational analysis of next-generation sequencing datasets to identify fully human antibodies with superior performance and developability characteristics. The OmniAb stack of technologies and differentiating AI and BI features have been combined to offer a highly efficient, scalable and customizable solution for the growing antibody discovery needs of the global biopharmaceutical industry.

We acquired the technologies in the OmniAb technology stack through the acquisition of OMT in January 2016, Crystal in October 2017, Ab Initio in July 2019, xCella Biosciences in September 2020 and Taurus Biosciences in September 2020. As of December 31, 2020, we had entered into OmniAb platform license agreements with more than 40 collaboration partners, including 7 partners who have rights through our partnership with WuXi. Our OmniAb partners were working on approximately 170 active programs, of which 15 were in various stages of clinical trials as of December 31, 2020.

Captisol Technology

Captisol is a patent-protected, chemically modified cyclodextrin with a structure designed to optimize the solubility and stability of drugs. Captisol was invented and initially developed by scientists in the laboratories of Dr. Valentino Stella, University Distinguished Professor at the University of Kansas’ Higuchi Biosciences Center for specific use in drug development and formulation. This unique technology has enabled several FDA-approved products, including Gilead’s Veklury®, Amgen’s Kyprolis®, Baxter International’s Nexterone®, Acrotech Biopharma L.L.C.’s and CASI Pharmaceuticals’ Evomela®, Melinta Therapeutics’ BaxdelaTM and Sage Therapeutics’ ZulressoTM. There are many Captisol-enabled products currently in various stages of development. We maintain a broad global patent portfolio for Captisol with more than 400 issued patents worldwide relating to the technology (including over 40 in the U.S.) and with the latest expiration date in 2033. Other patent applications covering methods of making Captisol, if issued, extend to 2040.

In addition to solid Captisol powder, we offer our partners access to cGMP manufactured aqueous Captisol concentrate. This product offering was established in 2017 to reduce cycle time and increase Captisol production capacity for large volume drug products. We maintain both Type IV and Type V DMFs with the FDA. These DMFs contain manufacturing and safety information relating to Captisol that our licensees can reference when developing Captisol-enabled drugs. We also have active DMFs in Japan, China and Canada. As of December 31, 2020, Captisol-enabled drugs were being marketed in more than 70 countries, and over 50 partners had Captisol-enabled drugs in development.

Protein Expression Technology Platform

The Protein Expression Technology Platform is a robust, validated, cost-effective and scalable platform for recombinant protein production, and is especially well-suited for complex, large-scale protein production where traditional systems are not suitable. Multiple global manufacturers have demonstrated consistent success with the platform and the technology is currently out-licensed for numerous commercial and development-stage programs. The versatility of the platform has been demonstrated in the production of enzymes, peptides, antibody derivatives and engineered non-natural proteins. Partners seek the platform as it can contribute significant value to biopharmaceutical development programs by reducing development timelines and costs for manufacturing therapeutics and vaccines. Given pharmaceutical industry trends toward large molecules with increasing structural complexities, the Protein Expression Technology Platform is well positioned to meet these growing needs as the most comprehensive broadly available protein production platform in the industry.

We acquired the Protein Expression Technology through our acquisition of Pfenex in October 2020. Former stockholders of Pfenex received a CVR which would result in payment if FDA determines that teriparatide injection (also referred to as PF708 or Bonsity) is therapeutically equivalent (as will be indicated by assignment of a therapeutic equivalence code that begins with an “A” in the FDA publication, Approved Drug Products with Therapeutic Equivalence Evaluations) with respect to the listed product, FORTEO® (teriparatide injection). We estimate that up to an additional $77.8 million in the aggregate will be payable to holders of the CVRs in the event that the CVR payment milestone is timely achieved. As of December 31, 2020, we have agreements with 15 partners for active research collaboration using this technology on more than 25 active programs.

Icagen Technology Platform

The Icagen Technology Platform is a novel drug discovery platform which uses primarily ion channels and transporters which are key components in a wide variety of biological processes that involve rapid changes in cells and we believe have broad therapeutic applicability including cancer, metabolic disease, pain, neurological diseases, infectious diseases and others. The Icagen Technology Platform leverages proprietary expertise in the combination of biological assays, medicinal chemistry, and in silico and computational chemistry applications. Partners in the pharmaceutical industry have leveraged our platform to develop therapeutic candidates to address unmet medical needs. We typically work closely with our partners through therapeutic candidate selection and, our partners are typically responsible for clinical development and commercialization. Our Icagen Technology Platform collaboration agreements typically include developmental milestone payments and royalties based on the net sales of any commercialized therapies. Royalties range from low to high single digits. The royalty terms typically expire upon the last to expire patents on a product-by-product basis.

We acquired the Icagen Technology Platform through our acquisition of the core assets of Icagen in April 2020 for $15.1 million in cash. Icagen is entitled to receive up to an additional $25.0 million based on certain revenue achievements. As of December 31, 2020, we have agreements with seven partners for active research collaboration using this technology on a total of 10 active programs.

HepDirect/LTP Technology Platform

The HepDirect platform is a first generation liver-targeting prodrug technology designed to deliver certain phosphorus-containing drugs to the liver by using a proprietary chemical modification that renders an API biologically inactive until cleaved by a liver-specific enzyme. The HepDirectTM technology may improve the efficacy and/or safety of certain drugs and can be applied to marketed or new drug products to treat liver diseases or diseases caused by hemostasis imbalance of circulating molecules controlled by the liver.

Our LTP platform is a broad second generation liver-targeting prodrug technology that has an activation mechanism similar to HepDirect but with broader applications and many improved features. The proprietary chemical modifications can be used with many chemical classes of drugs in addition to phosphorus-containing compounds and have multiple chemistry strategies, designed to improve flexibility and success rates. In addition, the second generation technology eliminates the undesirable by-products released during activation of the first generation prodrugs. As of December 31, 2020, we had active HepDirect/LTP programs with three partners, using this technology across five programs.

SUREtechnology Platform (owned by Selexis)

We acquired economic rights to various SUREtechnology Platform programs from Selexis. The SUREtechnology Platform, developed and owned by Selexis, is a novel technology that improves the way that cells are utilized in the development and manufacturing of recombinant proteins and drugs. As of December 31, 2020, we are entitled to certain economic rights to SUREtechnology Platform license agreements with 12 partners developing or having commercialized 20 programs.

Partners and Licensees

We currently have partnerships and license agreements with over 130 pharmaceutical and biotechnology companies. In addition to the table below, we also have more than 10 undisclosed partners and licensees.

Big Pharma Ticker Biotech Ticker Biotech, continued Ticker

Abbott ABT ABBA Private MEI MEIP

AbbVie ABBV ABL Bio 298380 Melinta Private

AstraZeneca AZN Abvivo Private Menarini Private

Baxter BAX Adept Private Meridian Labs Private

Boehringer Ingelheim Private Aldeyra ALDX Metavant Private

Daiichi Sankyo DSKY Amgen AMGN Merrimack MACK

Eli Lilly LLY Anebulo Private Nanjing King-Friend 603707

Eisai 4523 Aptevo APVO Neuritek Private

GSK GSK Arcellx Private Novan NOVN

Janssen JNJ Arcus RCUS Novogen NVGN

Jazz JAZZ Asahi Kasei 3407 Nucorion Private

Merck MRK Ascella Private Oncternal Private

Merck KGaA MRK.DE BendaRx Private OnKure Private

Novartis NVS Bexson Biomedical Private Opthea OPT

Ono 4528 Cantex Private Outlook OTLK

Otsuka 4768 Corvus CRVS Palvella Private

Pfizer PFE CR Double-Crane 600062 Pandion PAND

Roche RHHBY CStone 2616.HK Phoenix Tissue Private

Sanofi SNY Cumulus Private Precision Biologics Private

Takeda 4502 Electra Private Protagonist PTGX

Teva TEVA Elevation Private Revision Private

Specialty Pharma Ticker Exelixis EXEL RubrYc Private

Acrotech (Aurobindo) AUROPHARMA Five Prime FRPX SAGE SAGE

Aldevron Private Foghorn Private Seagen SGEN

Aytu Bioscience AYTU Genmab GEN Seelos SEEL

Aziyo AZYO Genagon Private Servier Private

Beloteca Private Genekey Biotech Private Serum Inst. of India Private

CASI CASI Genentech (Roche) RHHBY Softkemo Private

CorMatrix Private Genovac Private Sunshine Lake Private

CTI Biopharma CTIC GigaGen Private Talem Private

Ferring Private Gilead Sciences GILD Teneobio Private

Gloria 2437 Gordian Private TG Therapeutics TGTX

Lundbeck LUN HanAll 9420 Tizona Private

Sedor Private Harbour 2142 Travere TVTX

Sermonix Private IBC Generium Private Tremeau Private

SQ Innovation Private Ichnos Private Unity UBX

Vireo Health VREOF iMetabolic Private Valanbio Private

Immunovant IMVT Vaxxas Private

Generics Ticker Interventional Analgesix Private Vega Private

Alvogen Private J-Pharma Private VenBio Private

Apotex Private Jupiter Private VentiRx Private

BioCad Private Kangchen Private Verona VRNA

Gedeon Richter GEDSF Kira Private Viking VKTX

Hikma HIK KSQ Private Virtuoso Private

Mylan VTRS Marinus MRNS Xi'an Xintong Private

Zydus Cadila CADILAHC Zhilkang Hongyi Private

Commercial and Clinical Stage Partnered Portfolio

We have a large portfolio of current and future potential revenue-generating programs, including over 300 fully-funded by our partners. In addition to the table below, we also have more than 100 undisclosed preclinical programs.

Approved

Partner Name Program Therapeutic Area

Acrotech/CASI Evomela Cancer

Alvogen/Adalvo Teriparatide Women's Health

Alvogen/Hikma/Nanjing King-Friend Voriconazole Infectious Disease

Amgen/Ono Kyprolis Cancer

Aytu Tuzistra Infectious Disease

Aziyo ECM portfolio Medical device/Cardiology

Baxter Nexterone Cardiovascular

Biocad Teberif Inflammatory/Metabolic

Exelixis/Daiichi-Sankyo Minnebro Cardiovascular

Gilead Veklury Infectious Disease

Lundbeck Carnexiv Central Nervous System

Melinta Baxdela Infectious Disease

Menarini Frovatriptan Central Nervous System

Merck Noxafil-IV Infectious Disease

Par Posaconazole Infectious Disease

Pfizer Viviant/Conbriza Inflammatory/Metabolic

Pfizer Duavee Inflammatory/Metabolic

Pfizer Vfend-IV Infectious Disease

SAGE Zulresso Central Nervous System

Sedor Sesquient Central Nervous System

Serum Institute of India Pneumosil Infectious Disease

Zydus Cadila Vivitra Cancer

Zydus Cadila Bryxta/ZyBev Cancer

Zydus Cadila Exemptia Inflammatory/Metabolic

Zydus Cadila Vortuxi Inflammatory/Metabolic

Phase 3/Pivotal or Regulatory Submission Stage

Partner Name Program Therapeutic Area

Various Teriparatide Women's Health

Aldeyra Reproxalap Other/Undisclosed

Biocad BCD-066 Blood Disorders

CStone Sugemalimab Cancer

Gloria Zimberelimab Cancer

IBC Generium GNR-008 Severe and Rare

Jazz JZP-458 Cancer

Marinus Ganaxalone IV Central Nervous System

Merck V114 Infectious Disease

Novan SB206 Infectious Disease

Novartis Mekinist (CE-Trametinib) Cancer

Outlook Therapeutics ONS-5010 Other/Undisclosed

Palvella PTX-022 Other/Undisclosed

Sage Zulresso Infectious disease

Sanofi Sutimlimab Blood Disorders

Sedor CE-Fosphenytoin Central Nervous System

Serum Institute CRM197 Infectious Disease

Sunshine Lake Vilazodone Central Nervous System

Takeda Pevonedistat Cancer

Travere Sparsentan Severe and Rare

Verona Ensifentrine (RPL554) Respiratory Disease

Xi'an Xintong Pradefovir Infectious Disease

Phase 2

Partner Name Program Therapeutic Area

Arcus Zimberelimab Cancer

Cantex CX-01 Cancer

CTI Biopharma Tosedostat Cancer

Elevation Oncology Seribantumab Cancer

Eisai FYCOMPA Central Nervous System

Genmab Gen1046 Cancer

Harbour Batoclimab Inflammatory/Metabolic

Immunovant Batoclimab Inflammatory/Metabolic

Janssen Teclistimab Cancer

J-Pharma JPH-203 Cancer

Merck CRM197 Infectious Disease

Novartis ECF843 Inflammatory/Metabolic

Opthea OPT-302 Other/Undisclosed

Precision Biologics NPC-1C Cancer

Seelos Aplindore Central Nervous System

Sermonix Lasofoxifene Cancer

VentiRx Motolimod Cancer

Viking VK5211 Inflammatory/Metabolic

Viking VK2809 Inflammatory/Metabolic

Viking VK0214 Inflammatory/Metabolic

Viking VK0612 Inflammatory/Metabolic

Phase 1

Partner Name Program Therapeutic Area

Amgen AMG-330 Cancer

Apotex Meloxicam Migraine

Aptevo APVO436 Cancer

Exelixis ROR Inflammatory/Metabolic

Gedeon Richter Bevacizumab Cancer

Genmab Gen1046 Cancer

Jupiter Bioscience Viright Cancer

MEI Pharma ME-344 Cancer

Novartis MIK-665 Cancer

Novartis BCL-201 Cancer

Phoenix Tissue PTR-01 Other/Undisclosed

Protagonist Therapeutics PTG300 Hematology

Revision Therapeutics Rev0100 Ophthalmology

Takeda TAK-020 Inflammatory/Metabolic

Takeda TAK-925 Severe and Rare

Takeda TAK-243 Cancer

Vaxxas Nanopatch Infectious Disease

VentiRx Pharma VTX-1463 Cancer

Xi'an Xintong MB07133 Cancer

Selected Commercial Programs

We have multiple programs under license with other companies that have products that are already being commercialized. The following programs represent components of our current portfolio of revenue-generating assets and potential for near-term growth in royalty and other revenue. For information about the royalties owed to us for these programs, see “Royalties” later in this business section.

Kyprolis (Amgen)

We supply Captisol to Amgen for use with Kyprolis (carfilzomib), and granted Amgen an exclusive product-specific license under our patent rights with respect to Captisol. Kyprolis is formulated with Ligand’s Captisol technology and is approved in the United States for the following:

•In combination with dexamethasone, lenalidomide plus dexamethasone, or daratumumab plus dexamethasone for the treatment of patients with relapsed or refractory multiple myeloma who have received one to three lines of therapy.

•As a single agent for the treatment of patients with relapsed or refractory multiple myeloma who have received one or more lines of therapy.

Our agreement with Amgen may be terminated by either party in the event of material breach or bankruptcy, or unilaterally by Amgen with prior written notice, subject to certain surviving obligations. Absent early termination, the agreement will terminate upon expiration of the obligation to pay royalties. Under this agreement, we are entitled to receive revenue from clinical and commercial Captisol material sales and royalties on annual net sales of Kyprolis.

Veklury® (Gilead)

We supply Captisol to Gilead for sales of Veklury® (remdesivir). Gilead received marketing approval in the US in October 2020. Veklury is the first and only antiviral treatment of Covid-19 that is FDA approved. The product has regulatory approvals for the treatment of moderate or severe COVID-19 in over 50 countries and is included in more than 30 ongoing clinical trials. We are supplying Captisol to Gilead under a recently signed 10-year supply agreement. We are also supplying Captisol to Gilead’s voluntary licensing generic partners who are manufacturing remdesivir for 127 low- and middle-income countries. We receive our commercial compensation for this program through the sale of Captisol.

Teriparatide Injection Product (PF708) (Alvogen/Adalvo)

We acquired the Teriparatide Injection product with the acquisition of Pfenex Inc. in October 2020. Teriparatide Injection is a drug indicated for uses including the treatment of osteoporosis in certain patients at high risk for fracture. Teriparatide Injection was developed using our Protein Expression Technology and was approved by the FDA in 2019 in accordance with the 505(b)(2) regulatory pathway, with FORTEO as the reference product. Our partner, Alvogen launched the product in June 2020 in the United States.

Outside the U.S., PF708 received marketing authorization throughout the European Union in August 2020 under the tradename Livogiva®, was approved in Saudi Arabia in December 2020 under the name Bonteo, and is in various stages of regulatory and marketing application processes around the globe and, upon approval, may be marketed as Teriparatide Injection or under various tradenames, such as Bonsity® or Livogiva®.

Our partner Alvogen has exclusively licensed the rights to commercialize and manufacture the teriparatide injection product in the United States, while their Adalvo business has the rights to commercialize in the European Union (EU), certain countries in the Middle East and North Africa (MENA), and the rest of world (ROW) territories (the latter defined as all countries outside of the EU, US and MENA, excluding Mainland China, Hong Kong, Singapore, Malaysia and Thailand). Kangchen has exclusively licensed to commercialize PF708, upon receipt of applicable marketing authorizations, in Mainland China, Hong Kong, Singapore, Malaysia and Thailand and granted a non-exclusive right to conduct development activities in such countries with respect to PF708. Kangchen is responsible for all regulatory submissions, development costs and costs associated with regulatory approvals in these countries.

In accordance with our agreements with Alvogen/Adlavo, we are eligible to receive additional payments of up to $9.0 million based on the achievement of certain development, regulatory, and sales-related milestones. In addition, we may be eligible to receive tiered royalties on net sales between 25% and 40% prior to an “A” therapeutic equivalence designation, which increases to a flat 50% if an “A” rating is achieved.

In accordance with our EU, MENA and ROW agreements with Alvogen’s Adalvo subsidiary, we may be eligible to receive additional upfront and milestone payments of $1.5 million and may also be eligible to receive up to 60% of Alvogen’s gross profit derived from product sales and regional license fees, if approved, depending on geography, cost of goods sold and sublicense fees.

In accordance with our agreement with Kangchen, we may be eligible to receive additional payments of up to $22.5 million upon the achievement of certain development, regulatory, and sales-related milestones. We may be eligible to receive double-digit royalties on any net sales of PF708 in Kangchen’s territory.

Evomela (Acrotech and CASI)

We supply Captisol to Acrotech Biopharma for sales of Evomela in the U.S. and to CASI Pharmaceuticals for sales of Evomela in China. Evomela received market approval by the China National Medical Products Administration (NMPA). It is the only approved and commercially available melphalan product in China. Evomela is a Captisol-enabled melphalan IV formulation which is approved by the FDA for use in two indications:

•A high-dose conditioning treatment prior to ASCT in patients with multiple myeloma.

•For the palliative treatment of patients with multiple myeloma for whom oral therapy is not appropriate.

Evomela has been granted Orphan Designation by the FDA for use as a high-dose conditioning regimen for patients with multiple myeloma undergoing ASCT. The Evomela formulation avoids the use of propylene glycol, which has been reported to cause renal and cardiac side-effects that limit the ability to deliver higher quantities of therapeutic compounds. The use of the Captisol technology to reformulate melphalan is anticipated to allow for longer administration durations and slower infusion rates, potentially enabling clinicians to safely achieve a higher dose intensity of pre-transplant chemotherapy.

Under the terms of the license agreement, Acrotech Biopharma has marketing rights worldwide excluding China and CASI Pharmaceuticals has rights to market in China. We are eligible to receive over $50 million in potential milestone payments under this agreement and royalties on global net sales of the Captisol-enabled melphalan product. Acrotech and CASI’s obligation to pay royalties will expire at the end of the life of the relevant patents or when a competing product is launched, whichever is earlier, but in no event within ten years of the commercial launch. Our patents and applications relating to the Captisol component of melphalan are not expected to expire until 2033. As described herein, we have entered into a settlement agreement with Teva and Acrotech Biopharma (the holder of the NDA for Evomela) which will allow Teva to market a generic version of Evomela in the United States on June 1, 2026, or earlier under certain circumstances. Absent early termination, the agreement will terminate upon expiration of the obligation to pay royalties. The agreement may be terminated by either party for an uncured material breach or unilaterally by Acrotech and CASI by prior written notice.

Nexterone (Baxter)

We have a license agreement with Baxter, related to Baxter's Nexterone, a Captisol-enabled formulation of amiodarone, which is marketed in the United States and Canada. We supply Captisol to Baxter for use in accordance with the terms of the license agreement under a separate supply agreement. Under the terms of the license agreement we will continue to earn milestone payments, royalties, and revenue from Captisol material sales. We are entitled to earn royalties on sales of Nexterone through early 2033.

Zulresso (SAGE)

We have a license agreement with SAGE, related to SAGE's Zulresso, a Captisol-enabled formulation of brexanolone for the treatment of PPD. Under the terms of the agreement, we receive royalties and revenue from Captisol material sales.

Noxafil-IV (Merck)

We have a supply agreement with Merck related to Merck’s NOXAFIL-IV, a Captisol-enabled formulation of posaconazole for IV use. NOXAFIL-IV is marketed in the United States, EU and Canada. We receive our commercial compensation for this program through the sale of Captisol, and we do not receive a royalty on this program.

Duavee or Duavive (bazedoxifene/conjugated estrogens) and Viviant/Conbriza (Pfizer)

Pfizer is marketing bazedoxifene, a selective estrogen receptor modulator, under the brand names Viviantand Conbriza in various territories for the treatment of postmenopausal osteoporosis. Pfizer is responsible for the marketing of bazedoxifene, a synthetic drug specifically designed to reduce the risk of osteoporotic fractures while also protecting uterine tissue. Pfizer has combined bazedoxifene with the active ingredient in Premarin to create a combination therapy for the treatment of post-menopausal symptoms in women. Pfizer is marketing the combination treatment under the brand names Duavee and Duavive in various territories. Net royalties on annual net sales of Viviant/Conbriza and Duavee/Duavive are each payable to us through the life of the relevant patents or ten years from the first commercial sale, whichever is longer, on a country by country basis.

Aziyo Portfolio (Aziyo)

We receive a share of revenue from the currently marketed Aziyo portfolio of commercial pericardial repair and CanGaroo® Envelope ECM products. In addition, we have the potential to receive a share of revenue and potential milestones from the currently marketed CanGaroo® ECM Envelope for cardiac implantable electronic devices. Aziyo’s products are medical devices that are designed to permit the development and regrowth of human tissue.

Exemptia, Vivitra, Zybev and Bryxta (Zydus Cadila)

Zydus Cadila’s Exemptia (adalimumab biosimilar) is marketed in India for autoimmune diseases. Zydus Cadila uses the Selexis technology platform for Exemptia. We are entitled to earn royalties on sales by Zydus Cadila for ten years following the first commercial sale.

Zydus Cadila’s Vivitra (trastuzumab biosimilar) is marketed in India for breast cancer. Zydus Cadila uses the Selexis technology platform for Vivitra. We are entitled to earn royalties on sales by Zydus Cadila for ten years following the first commercial sale.

Zydus Cadila’s Bryxta and Zybev (bevacizumab biosimilar) is marketed in India for various indications. Zydus Cadila uses the Selexis technology platform for Bryxta and Zybev. We are entitled to earn royalties on sales by Zydus Cadila for ten years following the first commercial sale.

Minnebro (Exelixis)

Minnebro is marketed in Japan for the treatment of hypertension. Our partner, Exelixis, entered into a collaboration agreement with Daiichi Sankyo for the development of esaxerenone, a mineralocorticoid receptor antagonist. Under the terms of the agreement with Exelixis, we are entitled to receive a royalty on future sales.

Summary of Selected Development Stage Programs

We have multiple fully-funded partnered programs that are either in or nearing the regulatory approval process, or given the area of research or value of the license terms, we consider particularly noteworthy. We are eligible to receive milestone payments and royalties on these programs. This list does not include all of our partnered programs. For information about the royalties owed to Ligand for these programs, see “Royalties” later in this business section. In the case of Captisol-related programs, we are also eligible to receive revenue for the sale of Captisol material supply.

Sparsentan (Travere)

Our partner, Travere, is developing sparsentan for orphan indications of severe kidney diseases, and is running an on-going global pivotal Phase 3 clinical trial (DUPLEX) for sparsentan for the treatment of FSGS. Additionally, Travere is running

a global pivotal Phase 3 clinical trial (PROTECT) evaluating the long-term nephroprotective potential of sparsentan for the treatment of IgA nephropathy, a rare, immune complex mediated chronic glomerular disease. Certain patient groups with severely compromised renal function, including those with FSGS and IgA nephropathy, exhibit extreme proteinuria resulting in progression to dialysis and a high mortality rate. Sparsentan, with its unique dual blockade of angiotensin and endothelin receptors, is expected to provide meaningful clinical benefits in mitigating proteinuria in indications where there are no approved therapies.

In February of 2021, Travere announced that sparsentan achieved its pre-specified interim FSGS partial remission of proteinuria endpoint (FPRE) in the DUPLEX Phase 3 study after 36 weeks of treatment. Sparsentan demonstrated a statistically significant response on FPRE compared to the active control, irbesartan (p=0.0094). Preliminary results from the interim analysis suggest that sparsentan has been generally well-tolerated and has shown a comparable safety profile to irbesartan. Based on the data from the interim analysis, Travere intends to pursue submissions for accelerated approval of sparsentan for FSGS in the second half of 2021.

Travere has stated that topline efficacy data from the ongoing pivotal Phase 3 PROTECT Study in IgA nephropathy, and the 36-week interim proteinuria endpoint analysis, are anticipated in the third quarter of 2021.

Under our license agreement with Travere, we may be entitled to receive potential milestones of over $70 million and net royalties on future worldwide sales by Travere. The royalty term is expected to be 10 years following the first commercial sale. Travere is responsible for all development costs related to the program.

TR-Beta - VK2809 and VK0214 (Viking)

Batoclimab (Immunovant, HanAll and Harbour)

Our partner, HanAll has granted Immunovant an exclusive license for the development, manufacture and marketing of Batoclimab for the treatment of pathogenic IgG-mediated autoimmune diseases in the U.S., Canada, Mexico, the EU, the United Kingdom, Switzerland, Latin America, the Middle East and North Africa. Immunovant is currently conducting a Phase 2 clinical trial in myasthenia gravis and other inflammatory diseases. Additionally, HanAll and Harbour BioMed, are collaborating to develop Batoclimab for similar treatment in China and Korea and are currently conducting a Phase 2 trial in China. HanAll retains the rights to Batoclimab in Korea and Harbour will control the marketing in China. As part of our agreement with HanAll, we are entitled to development and regulatory milestones and royalties on potential future sales from HanAll and sublicense revenues from Immunovant and Harbour based on amounts received by HanAll.

V114 (Merck)

Merck’s 15-valent pneumococcal conjugate vaccine, PCV-15 (V114) is in late stage clinical development with 17 Phase 3 clinical trials. In October 2020, Merck released additional positive data from two Phase 3 studies evaluating the safety, tolerability and immunogenicity of V114 and submitted applications in November 2020 to the FDA and EMA for licensure of V114. On January 12, 2021, Merck announced the FDA accepted the BLA for V114 for priority review with a PDUFA of July 18, 2021. V114 previously received Breakthrough Therapy Designation from the FDA for the prevention of invasive pneumococcal disease in pediatric patients 6 weeks to 18 years of age and adults 18 years of age and older. Pneumococcal disease in adults is on the rise in many countries, and V114 consists of pneumococcal polysaccharides from 15 serotypes conjugated to CRM197carrier protein, including serotypes 22F and 33F, which are commonly associated with invasive pneumococcal disease in older adults and are not contained in the currently licensed vaccine for adults.

In accordance with our CRM197 commercial license agreements, we are eligible to earn an additional $11.5 million in development and regulatory milestones and may also be eligible to receive low single digit royalties derived from net sales, depending on territory.

Pneumosil® (Serum Institute of India, SII)

SII began commercialization of its 10-valent pneumococcal conjugate vaccine, Pneumosil® in the second quarter of 2020. Pneumosil is designed primarily to help fight against pneumococcal pneumonia among children, with an advantage of targeting the most prevalent serotypes of the bacterium causing serious illness in developing countries. Pneumosil achieved WHO Prequalification in December 2019, allowing the product to be procured by United Nations agencies and Gavi, the Vaccine Alliance, and subsequently achieved Indian Marketing Authorization in July 2020, and announced commercial launch of the product in India in December 2020. Additionally, SII is currently testing a meningococcal conjugate vaccine in a Phase 3 study in India.

JZP-458 and JZP-341 (Jazz Pharmaceuticals)

We are developing hematologic oncology products with our partner Jazz Pharmaceuticals Ireland Limited (Jazz) including PF743 (JZP-458), a recombinant Erwinia asparaginase, PF745 (JZP-341), a long-acting Erwinia asparaginase, and PF690, a pegaspargase. Both PF743 and PF745 are being developed for the treatment of acute lymphoblastic leukemia and other hematological malignancies. Jazz has worldwide rights to develop and commercialize PF743 and PF745 and an exclusive option to license PF690 subject to certain option triggers.

In accordance with the Jazz agreement, we are eligible to earn remaining milestones of $162.5 million. We may also be eligible to receive tiered royalties on worldwide sales of any product resulting from the collaboration.

CRM197

CRM197 is a non-toxic mutant of diphtheria toxin. It is a well characterized protein and functions as a carrier for polysaccharides and haptens, making them immunogenic. CRM197 is used in prophylactic and therapeutic vaccine candidates. We have developed CRM197 production strains using our Protein Expression Technology platform and supply preclinical grade and cGMP CRM197 to several vaccine development focused pharmaceutical customers. Our partners Merck & Co., Inc. (Merck) and Serum Institute of India Private Limited (SII) have exclusively licensed unique production strains for use in their conjugate vaccine products and candidates for pneumococcal and meningitis bacterial infections. Pneumococcus bacterium (Streptococcus pneumoniae) is a leading cause of severe pneumonia and major cause of morbidity and mortality worldwide.

Pevonedistat - TAK-924 (Millennium/Takeda)

Our partner, Millennium/Takeda, is currently conducting Phase 3 trials for the development of pevonedistat for the treatment of hematological malignancies and solid tumors. Pevonedistat is a Captisol-enabled Nedd8-Activating Enzyme Inhibitor. Under the terms of the clinical-stage agreement, we may be entitled to over $25 million in regulatory and development milestones from Millennium/Takeda, revenue from Captisol material sales, and royalties on potential future net sales.

Ensifentrine – RPL554 (Verona)

Our partner, Verona, is currently conducting a comprehensive Phase 3 clinical trial to evaluate the efficacy and safety of nebulized ensifentrine in patients with moderate to severe COPD. Under the terms of our agreement with Verona, we are entitled to development and regulatory milestones, including a £5.0 million payment upon the first approval of any regulatory authority, and royalties on potential future sales.

Teclistamab (Janssen)

Our partner, Janssen, is developing Teclistamab, a BCMAxCD3 bispecific antibody discovered in part with the OmniAb platform technology. Janssen is currently conducting two Phase 2 trials, as a single agent and in combination with daratumumab in multiple myeloma. We are entitled to earn development and regulatory milestones based on the development of Teclistamab.

JNJ-67371244 (Janssen)

Janssen is also developing JNJ-67371244, an anti-CD33xCD3 antibody discovered in part with the OmniAb platform technology. Janssen is currently conducting a Phase I trial for cancer therapy. We are entitled to earn development and regulatory milestones based on the development of JNJ-67371244.

JNJ-70218902 (Janssen)

Janssen is also developing JNJ-70218902, a T-cell redirecting agent antibody discovered in part with the OmniAb platform technology. Janssen is currently conducting a Phase I trial for cancer therapy for patients with metastatic castration resistant prostate cancer. We are entitled to earn development and regulatory milestones based on the development of JNJ-70218902.

M6223 (Merck KGaA)

Our partner, Merck KGaA, is currently conducting a Phase 1 trial of M6223, an anti-TIGIT antibody discovered with the OmniAb platform, in patients with metastatic or locally advanced solid unresectable tumors in combination with bintrafusp alfa. Under the terms of the agreement, we are entitled to sublicense revenues, milestones and royalties on potential future net sales.

SARM - VK5211 (Viking)

Ganaxalone IV (Marinus)

Our partner, Marinus, is conducting Phase 3 clinical trials with Captisol-enabled ganaxolone IV in patients with PPD and refractory status epilepticus. Marinus has exclusive worldwide rights to Captisol-enabled ganaxolone, a GABAA receptor modulator, for use in humans. We are entitled to development and regulatory milestones, revenue from Captisol material sales, and royalties on potential future sales.

APVO436 (Aptevo)

Our partner, Aptevo, is currently conducting a Phase 1 trial of APVO436 for the treatment of acute myeloid leukemia and high-grade myelodysplastic syndrome. There is a high unmet medical need for targeted immunotherapies such as APVO436, that can potentially treat patients with relapsed or refractory disease, or patients who cannot tolerate traditional chemotherapy. Under the terms of the agreement with Aptevo, we are entitled to development and regulatory milestones and royalties on potential future net sales.

Gen1046 (GenMab)

Our partner, GenMab, is currently conducting a Phase 1/2 trial of Gen1046 for use in patients with malignant solid tumors. Under the terms of the agreement with GenMab, we are entitled to clinical and regulatory milestones and royalties on potential future sales.

SYM022 and SYM023 (Symphogen/Servier)

Our partner, Symphogen (acquired by Servier), is currently conducting Phase 1 trials of SYM022 and SYM023 to determine if it is safe and tolerable for patients with locally advanced/unresectable or metastatic solid tumor malignancies or lymphomas that are refractory to available therapy for which no standard therapy is available. Under the terms of the agreement with Symphogen, we are entitled to sublicense revenues, milestones and royalties on potential future net sales.

WuXi Partnership

Pursuant to the WuXi Agreement, we have granted WuXi a non-exclusive license to use our OmniRat, OmniMouse and OmniFlic platforms solely to research, develop and make antibodies, and we have agreed to use commercially reasonable efforts to deliver to WuXi animals from such platforms to support WuXi’s licensing rights under the WuXi Agreement. Further, WuXi has the right to out-license antibodies it discovers (whether for itself or at the direction of out-licensees) under the WuXi Agreement to out-licensees worldwide. We are entitled to royalties in the low single digits on net sales of products. Unless earlier terminated, the term of the WuXi Agreement shall continue indefinitely. Either party may terminate the WuXi Agreement upon specified notice of the other party's uncured material breach of the WuXi Agreement. In addition, we have the right to terminate the WuXi Agreement if WuXi or one of its out-licensees challenges the validity of one of our patents covering the platform and WuXi has the right to terminate the WuXi Agreement for convenience following a specified period after notice of termination.

In addition to other earlier stage programs, the following programs have been licensed pursuant to the WuXi Agreement:

Zimberelimab AB122/GLS010/WBP3055 (Arcus and Gloria)

Our partner, WuXi, has outlicensed the rights to certain programs using the OmniAb technology to Arcus and Gloria. Arcus is conducting multiple Phase 1 trials and a Phase 2 trial to evaluate the safety and tolerability of Zimberelimab in subjects with advanced solid tumors. Additionally, Gloria, has submitted an NDA in China for the treatment of recurrent or refractory classical Hodgkin’s lymphoma. Under the terms of our agreement with WuXi, we are entitled to royalties on potential future sales.

Sugemalimab CS1001 (CStone)

WuXi has also outlicensed the rights to certain programs using the OmniAb technology to CStone. CStone is currently conducting a Phase 3 trial to evaluate the efficacy and safety of CS1001 to treat patients with natural killer cell/T-cell lymphoma and classical Hodgkin’s lymphoma. Under the terms of our agreement with WuXi, we are entitled to royalties on potential future sales.

Ciforadenant – CPI-444 (Corvus)

Our partner, Corvus, is conducting a Phase 1b/2 clinical trial in patients with renal cell carcinoma and metastatic castration resistant prostate cancer to evaluate Ciforadenant, an antagonist of adenosine A2A, in combination with the immunotherapy drug atezolizumab. Positive preliminary data was presented in February at ASCO 2020 Genitourinary Cancers Symposium (ASCO-GU) and additional data was presented at ASCO 2020 in May/June. Ciforadenant is also being evaluated in a Phase 1b/2 trial in combination with atezolizumab in patients with non-small cell lung cancer who have failed no more than two prior regimens. Under the terms of our agreement with Corvus, we are entitled to development and regulatory milestones and tiered royalties on potential future sales. The aggregate potential milestone payments from Corvus are approximately $220 million for all indications.

FYCOMPA IV (Eisai)

Our partner, Eisai, recently completed an open-label, single group assignment, multicenter, Phase 2 study in Japan to evaluate the safety and tolerability of intravenous perampanel, formulated with Captisol, as substitute for oral tablets as an adjunctive therapy in patients with partial onset seizures (including secondarily generalized seizures) or primary generalized tonic-clonic seizures. The primary endpoint was the number of patients with adverse events and serious adverse events. We are entitled to revenue from Captisol material sales and tiered royalties on potential future sales.

SB206 (Novan)

We acquired certain economic rights to SB206 from Novan in May 2019. SB206 is a topical nitric-oxide antiviral gel for the treatment of viral skin infections, including molluscum contagiosum (MC). MC is an infection which causes skin lesions that affect approximately 6 million people in the United States annually, with the greatest incidence in children aged one to 14 years. During the first quarter of 2020, Novan announced that it did not achieve statistically significant results for its primary end point from its Phase 3 pivotal trials of SB206 in MC. Novan continues to explore financial as well as strategic options in order to progress SB206.

PTX - 022 (Palvella)

Lasofoxifene (Sermonix)

Lasofoxifene is a selective estrogen receptor modulator for osteoporosis treatment and other diseases, discovered through the research collaboration between Pfizer and us.

Our partner, Sermonix has a license for the development of oral lasofoxifene for the United States and additional territories. Under the terms of the agreement, we are entitled to receive over $45 million in potential regulatory and commercial milestone payments as well as royalties on potential future net sales.

Sermonix announced in October 2020 the enrollment and dosing of the first patient into the Phase 2 ELAINE 2 clinical trial of lasofoxifene in combination with Eli Lilly’s FDA-approved CDK 4 and 6 inhibitor, abemaciclib for the treatment of pre- and postmenopausal women with locally advanced metastatic estrogen receptor-positive (ER+)/HER2- breast cancer and an ESR1 mutation. The Phase 2 ELAINE 1 trial, which began enrollment in September 2019, is assessing the efficacy of oral lasofoxifene versus intramuscular fulvestrant for the treatment of postmenopausal women with locally advanced or metastatic ER+/HER2- breast cancer with an ESR1 mutation.

Pradefovir (Xi'an Xintong)

Our Chinese licensee, Xi'an Xintong Medicine Research (following its acquisition of Chiva Pharmaceuticals), is developing pradefovir, an oral liver-targeting prodrug of the HBV DNA polymerase/reverse transcriptase inhibitor adefovir, for the potential treatment of hepatitis B virus (HBV) infection. Pradefovir was developed using Ligand’s HepDirect technology. In September 2019, Xi'an Xintong Medicine Research reported positive results from a Phase 2 trial of pradefovir, showing good efficacy, safety and tolerability. At the dose of 75 mg, the reduction of DNA viral load, the percentage of no viral load detected, and HBeAg negative conversion rate were better than tenofovir disoproxil fumarate (TDF) after 24 weeks of treatment. Overall incidence of side effects was less than TDF and there was no renal or skeletal toxicity. Xi'an Xintong Medicine Research is planning for a Phase 3 trial. We are entitled to an annual licensing maintenance fee and royalties on potential future sales.

MB07133 (Xi'an Xintong)

Chinese licensee Xi'an Xintong Medicine Research is also developing MB07133, a liver specific, HepDirect prodrug of cytarabine monophosphate, for the potential treatment of hepatocellular carcinoma (HCC) and intrahepatic cholangiocarcinoma. MB07133 is currently in Phase 1 in China. We are entitled to an annual licensing maintenance fee and royalties on potential future sales.

Summary of Selected Collaborations

GSK Collaboration

In December 2020, we entered into a license and collaboration agreement with GSK to leverage our unique expertise in small molecule therapeutics targeting transmembrane proteins. The goal of this collaboration is to identify and develop inhibitors of a specific, genetically validated molecular target relevant to neurological diseases. Under the terms of the agreement, we received an upfront payment of $7.0 million and could receive additional development, regulatory and commercialization milestones of up to $154.5 million. We are also entitled to receive tiered royalties should any drug from the collaboration be commercialized. We will be responsible for the majority of preclinical activities up to lead optimization with both Ligand and GSK collaborating to identify candidates of IND-enabling studies. GSK has the exclusive option to license any identified inhibitors and will be responsible for further development and commercialization of any drug candidates identified through the collaboration.

Roche Collaboration

In December 2018, prior to the acquisition by Ligand, Icagen entered into a license and collaboration agreement with Roche to develop and commercialize small molecule ion channel modulators for the treatment of neurological disorders and in May 2020 amended the license and collaboration agreement to include a second target. These programs incorporate our technology platform for ion channel drug discovery and are directed at specific ion channel targets expressed in neurons. Under the terms of the agreement, Roche paid us on a per target basis an upfront payment for program exclusivity and research funding. In addition, we are eligible to potentially receive development and commercial milestone payments of up to $274 million per program and royalty payments if a drug is commercialized. We will be responsible for most preclinical activities up to lead optimization with both us and Roche applying resources to identify candidates for entry into late stage preclinical and IND enabling studies. Thereafter, Roche will be responsible for the further development and commercialization of the programs.

Cystic Fibrosis Foundation Collaboration

In May 2018, prior to the acquisition by Ligand, Icagen announced an award of up to $11 million from the Cystic Fibrosis Foundation for a project focused on the discovery of therapeutics to treat patients with cystic fibrosis (CF) caused by nonsense mutations. Nonsense mutations in the Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”) gene result in the premature termination of protein synthesis and the formation of truncated, non-functional CFTR. Patients with these mutations in both copies of their CFTR genes currently have no therapies that treat the underlying cause of their disease. The aim of this program is to provide these patients with a transformative therapeutic that will markedly improve their quality of life and lifespan. The award is to support an integrated, multi-year drug discovery initiative. At the North American Cystic Fibrosis Conference in October 2020, we reported the identification and characterization of a class of small molecule agents that enhance CFTR-PTC mutant readthrough and enable functional CFTR currents in combination with aminoglycosides.

Royalties

We have multiple programs under license with other companies that have products that are already being commercialized. In addition to the table below, we have generally described a typical Captisol and OmniAb royalty arrangement as low- to mid-single digit royalties. The following table represents substantially all of the disclosed information about our royalty arrangements:

Royalty Table

Ligand Licenses With Tiered Royalties

Program Licensee Royalty Rate

CE-Meloxicam Sedor 8.0% - 10.0%

Ciforadenant Corvus Mid-single digit to low-teen royalty

Duavee Pfizer 0.5% - 2.5%

Ensifentrine (RPL554) Verona Low to mid-single digit royalty

FBPase Inhibitor (VK0612) Viking 7.5% - 9.5%

Kyprolis Amgen 1.5% - 3.0%

Lasofoxifene Sermonix 6.0% - 10.0%

Mineral Coated Microparticle Dianomi 2.0% - 3.0%

OmniAb-Genagon Genagon 4.0% - 6.0%

OmniAb-GigaGen GigaGen Mid-single digit royalty

OmniAb-iMetabolic iMetabolic <6%

OmniAb-Kira Kira Low to mid-single digit royalty

OmniAb-Takeda Takeda Low single digit royalty

Oral EPO Viking 4.5% - 8.5%

Viviant/Conbriza Pfizer 0.5% - 2.5%

Various Nucorion 4.0% - 9.0%

Various Seelos 4.0% - 10.0%

Ligand Licenses With Fixed Royalties

Program Licensee Royalty Rate

4-1BB Zhilkang Hongyi Low single digit royalty

AB122 Arcus Low single digit royalty

Baxdela Melinta 2.5%

CE-Fosphenytoin Sedor 11%

Sugemalimab CStone 3%

Evomela Acrotech/CASI 20%

V114 Merck Low single digit royalty

Pneumosil Serum Institute Low single digit royalty

ME-344 MEI Pharma Low single digit royalty

OmniAb-KSQ Therapeutics KSQ Therapeutics Single digit royalty

PCSK-9 Genekey Low single digit royalty

Pradefovir Xi'an Xintong 9%

Reproxalap Aldeyra Therapeutics Low single digit royalty

Sparsentan Travere 9%

Various Gloria Low single digit royalty

Zulresso SAGE 3%

Contract Payments (Milestones)

Many of our programs under license with our partners will generate contract payments to us if our partners reach certain development, regulatory and commercial milestones. The following table represents the potential maximum value of our contract payment pipeline on milestones by development stage, technology and partner (in thousands):

Technology* Stage* Partner*

*All tables exclude our annual access fees and collaboration revenue for development work.

Internal Development Programs

We have a number of internal development or unpartnered programs focused on a wide-range of potential indications or disease.

The Captisol-enabled (CE)-Iohexol program was established in January 2018 to develop a next-generation contrast agent for diagnostic imaging with a reduced risk of renal toxicity. Contrast-induced acute kidney injury (CI-AKI) is the acute impairment of renal function following intravascular administration of an iodinated contrast agent, and occurs most frequently following coronary angiography, percutaneous coronary intervention and contrast-enhanced computed tomography, especially among patients at risk of renal injury such as those with advanced age, diabetes or heart failure. Currently no products are approved to prevent or treat CI-AKI in this setting, and therefore we believe a significant opportunity exists for a safer formulation of contrast agents. The goal is for CE-Iohexol to improve upon the limitations of existing contrast agents and enable a future partner to gain meaningful market share. In July 2019, we announced positive top-line results from a Phase 1 clinical trial CE-Iohexol conducted in Canada. The trial achieved the primary endpoint by demonstrating pharmacokinetic bioequivalence of CE-Iohexol injection and a reference Iohexol injection (OMNIPAQUETM) after IV administration in healthy adults. CE-Iohexol injection was well tolerated, and adverse events were in line with the known safety profile of OMNIPAQUE. We submitted an IND with the FDA in November and received a “Study May Proceed” letter in December 2020 along with feedback from the FDA on the clinical plan. We plan to initiate a Phase 2 study in the U.S. in the first quarter of 2021.

LGND US Equity

LGND · 10-K · period ended 2020-12-31

Item 1. Business

LGND US Equity☆

LGND · 10-K · period ended 2020-12-31

Item 1. Business

LGND US Equity