Hepatitis Program “Metabasis entered into a fully funded collaboration and license agreement with Roche in 2008 to develop new treatments for hepatitis C viral infection utilizing the proprietary HepDirect?® liver-targeting technology. The lead HepDirect Nucleoside, MB11362, was declared a clinical candidate in the second quarter of 2009. Advanced preclinical development studies are ongoing in preparation for a first-in-human clinical program. Under the terms of the license agreement, Roche will fund 100% of the program costs and will make milestone and royalty payments upon the achievement of certain development events and commercialization of MB11362 and/or other applicable HepDirect compounds covered under the agreement. Ligand will retain approximately one-third of any payments received. Glucagon Receptor Antagonist Program “ Metabasis has developed chemically novel, potent, orally bioavailable glucagon antagonists for treating type 2 diabetes. The lead compound, MB11262, has shown significant and consistent lowering of blood glucose when dosed orally in numerous diabetic animal models and is currently in advanced lead optimization stage. Ligand will retain 50% to 80% of the net proceeds of any transaction for this program. Thyroid Receptor Agonist Program “ Thyroid receptor activation in the liver affects the expression of several genes, leading to reductions in LDL, triglycerides and LP(a) while its activation in extra-hepatic tissues result in dose-limiting side effects. Metabasis has developed a liver-targeted TR agonist, MB07811, using HepDirect prodrug technology and other structural characteristics for the treatment of hyperlipidemia. Phase I single and multi-dose clinical trials of MB07811 have been completed. In addition, Metabasis has an advanced discovery program to identify second-generation TR agonists with potential improvements in the therapeutic index for lowering cholesterol and other lipids associated with cardiovascular risks. Ligand will retain 50% to 80% of the net proceeds of any transaction for this program. MB07133 Program “ Metabasis has developed MB07133, a HepDirect prodrug of the intermediate form of a known oncolytic, which is designed to deliver high concentration of the active form of the drug for the treatment of hepatocellular carcinoma. Metabasis has completed a repeat cycle Phase I/II clinical trial of MB07133. Ligand will retain 10% to 90% of the net proceeds of any transaction for this program. PeriCor Therapeutics “ Metabasis has a common stock ownership position in PeriCor Therapeutics, Inc., a private, clinical-stage company focused on myocardial protection. PeriCor sublicensed rights from Metabasis to acadesine and three additional Adenosine Regulating Agents in 2005. PeriCor recently licensed acadesine to Schering-Plough and the compound is in a Phase III clinical trial for the prevention of adverse cardiovascular and cerebrovascular outcomes in patients undergoing coronary artery bypass graft surgery. Ligand will retain 40% of the net proceeds of any disposition of its PeriCor stock. HepDirect Technology: HepDirect technology supplements Ligand ™s core drug discovery technology platform of ligand-dependent gene expression and ultra-high throughput combinatorial chemistry screening. HepDirect is a prodrug technology that targets delivery of certain drugs to the liver by using a proprietary chemical modification that renders a drug biologically inactive until cleaved by a liver-specific enzyme. HepDirect may improve efficacy and/or safety of certain drugs and can be applied to marketed or new drug products. Ligand will retain 50% to 75% of any net proceeds received for licensing or selling the HepDirect technology. Other Product Candidates and R&D Programs “ Metabasis has other product candidates, including MB07803 for diabetes and pradefovir for hepatitis B, and early stage R&D programs including glucokinase activators for diabetes and DGAT-1 inhibitors for obesity. Ligand will retain 50% to 75% of the net proceeds for any deal generated from these programs.

Source: Ligand Pharmaceuticals Incorporated