Ligand Portfolio

We believe Ligand has assembled one of the largest portfolio of assets among its biotech peers with 70 fully funded partnered programs.

The portfolio covers a diverse array of indications with many programs in late stages of development.

Distribution of Therapeutic Areas
Oncology	28
CNS	8
Inflammation	5
Metabolic Disease	4
Blood Disorder	5
Anti-microbial	5
Anti-viral	4
Cardiology	3
Other	8

Distribution of Partners
GSK	7
Merck	7
Pfizer	5
BMS	5
AstraZeneca	2
Sanofi Aventis	2
Eli Lilly	4

Partnered Portfolio

Program Molecule Indication Pre Clinical Phase I Phase II Phase III Marketed
Promacta	TPO Receptor AgonistPromacta is an FDA-approved treatment for chronic ITP in adults who have had an insufficient response to corticosteroids, immunoglobulins or surgical removal of the spleen. Promacta is authorized for use in all 27 member states of the European Union, as well as India, Australia, Ireland, Japan, Taiwan, Turkey, Singapore, Kuwait, Chile, Russia and Bahrain under the trade name Revolade®. Promacta was co-discovered by Ligand and GSK. Partner: GSK	ITP	GSK	Marketed
Promacta	TPO Receptor AgonistPromacta is being developed for the treatment of patients with hepatitis C-related thrombocytopenia. Promacta was co-discovered by Ligand and GSK.	HepC	GSK	Marketed
Kyprolis	Captisol-enabled CarfilzomibKyprolis is a selective next-generation proteasome inhibitor with a mechanism of action aimed at increasing therapeutic efficacy and limiting the side effects associated with currently available therapies.	Oncology	Onyx	Marketed
Avinza	ER- MorphineAvinza is an FDA-approved extended-release morphine treatment. Ligand currently receives a royalty on all sales. Partner: Pfizer	Pain	Pfizer	Marketed
Nexterone	Captisol- enabled Amiodarone	Arrhythmia	Baxter	Marketed
Viviant	SERMViviant is a selective estrogen receptor modulator (SERM) used for the treatment of osteoporosis. Ligand receives royalties on sales of Viviant that Pfizer sells in the EU (branded as Conbriza in the EU). Ligand receives royalties on sales of a SERM (selective estrogen receptor modulator) product called Viviant that Pfizer sells in the EU (called Conbriza in the EU). Viviant is used to treat osteoporosis. Partner: Pfizer	Osteoporosis	Pfizer	Marketed
Cerenia	Captisol- enabled Canine Anti-NauseaCerenia is an FDA-approved anti-emetic developed specifically for dogs. Partner: Pfizer	Animal Health	Pfizer	Marketed
VFEND	Captisol- enabled IV- VoraconazoleVfend is an FDA-approved drug for the treatment of candidemia in nonneutropenic patients and the following Candida infections: disseminated (deep tissue) infections in skin and infections in abdomen, kidney, bladder wall, and wounds. Partner: Pfizer	Antifungal	Pfizer	Marketed
Geodon	Captisol- enabled IV- ZiprasidoneGeodon is an FDA-approved treatment for acute manic or mixed episodes associated with bipolar disorder. Partner: Pfizer	Schizophrenia	Pfizer	Marketed
Aprela	SERM + PremarinAprela, bazedoxifene + Premarin(R) is a SERM (selective estrogen receptor modulator) discovered at Ligand. Aprela is being developed for the treatment of postmenopausal osteoporosis.	Menopause	Pfizer	P4
Carbamazepine- IV	Captiol- enabled carbamazepine	CNS	Lundbeck	Phase 3
Undisclosed Captisol Program	Undisclosed	Undisclosed	Merck	Phase 3
Clopidogrel IV	Captisol- enabled ClopidogrelCaptisol -enabled Clopidogrel is being developed in IV solution. Clopidogrel is the active ingredient in Plavix(R), the world's leading anti-platelet medication which is currently only available in an oral formulation. Ligand is entitled to royalties on annual worldwide sales net.	Anti-arrhythmia	The Medicines Company	P2
Undisclosed Captisol Program	UndisclosedUndisclosed	Undisclosed	Hospira	P2
Melphalan IV	Captisol-enabled MelphalanCaptisol-enabled Melphalan	Oncology	Spectrum	P2
Promacta	TPO Receptor Agonist	Oncology	GSK	P2
Dinaciclib¹	CDK InhibitorA CXCR2 (chemokine receptor 2) inhibitor is being developed for the treatment of COPD. The compound was discovered at Ligand.	Oncology	Merck	P2
BACE²	Beta Secretase Inhibitor	Alzheimer's	Merck	P2
Tanaproget	Progesterone Receptor AntagonistCTanaproget is a tissue-selective, non-steroidal contraceptive progesterone receptor agonist that has the potential for an improved side-effect profile over current steroidcontaining contraceptives. Pfizer granted a sublicense to a multi-national pharmaceutical company for Tanaproget. Ligand is entitled to additional payments based on clinical and regulatory milestones, along with royalties on future sales.	Contraceptive	Undisclosed	P2
GSK2285921	TPO Receptor AgonistGSK 2285921 is a follow-on compound to Promacta, an agonist of the thrombopoietin (TPO) receptor. GSK 2285921 was discovered at Ligand.	ITP	GSK	P2
Delafloxacin	FluoroquinoloneFluoroquinolone	Infection	Rib-X	P2
SAR125844	Captisol-enabled MET kinase inhibitor	Oncology – Malignant Neoplasm	Sanofi-Aventis	P2
RE-021	DARADARA	FSGS	Retrophin	P1
Pradefovir	HepDirect HepB InhibitorPradefovir is being developed in China for the treatment of HepB.	HepB	Chiva	P1
MB07133 (HCC)	HepDirect HepB InhibitorMB07133 is being developed in China for the treatment of hepatocellular carcinoma.	HCC	Chiva	P1
XL652	LXR AgonistAn LXR (Liver X Receptor) agonist (XL652) is being developed in collaboration with Bristol-Myers Squibb for dyslipidemia and atheroclerosis that was based on technology that Ligand licensed to Exelixis.	Atherosclerosis	Exelixis	P1
XL550	MR AntagonistA MR (Mineralocorticoid Receptor) antagonist (XL550) is in collaboration with Daiichi Sankyo that was based on technology that Ligand licensed to Exelixis. The drug is in development for a variety of conditions, including diabetes, hypertension, and congestive heart failure.	Metabolic Disorders	Exelixis	P1
ME-143	Captisol-enabled	Oncology	MEI Pharma	Phase I
ME-344	Captisol-enabled	Oncology	MEI Pharma	P1
CXCR4 (inflammation)	CXCR4 Antagonist	Inflammation	Proximagen	Preclinical
ML061	Captisol-enabled Docetaxel	Oncology	Meridian Laboratories	Preclinical
Undisclosed	Captisol-enabled CNS therapeutics	CNS	SAGE	Preclinical

More than 25 other undisclosed Captisol-enabled® programs with partners.

1. Phase IIb/III adaptive design in patients with chronic lymphocytic leukemia.

2. Phase II/III in patients with mild-to-moderate Alzheimer's disease.