Ligand to Present Positive Data from Phase 1 Study of Effect of SERN Lasofoxifene

Ligand Pharmaceuticals Incorporated

announced that data from a Phase 1 study of the selective estrogen receptor modulator (SERM) lasofoxifene were featured in a poster presentation today at ICE/ENDO 2014 in Chicago. The presentation provided data from a first-in-human clinical study of lasofoxifene that was performed by Pfizer and recently analyzed by Ligand demonstrating the potent and prolonged effect of a single dose to increase circulating testosterone and gonadotropin levels in healthy young men. Highlights of the presentation include: * In an investigator-blinded, randomized, placebo-controlled, single-ascending dose study involving 36 healthy male volunteers, lasofoxifene was well-absorbed after oral administration with peak plasma concentrations reached approximately 6 to 9 hours post-dose and a long elimination half-life of approximately 106 hours * There were no serious adverse events and no clinically significant changes in safety laboratory, vital signs or ECG assessments * Single oral doses of lasofoxifene of 1, 3, 10, 30 and 100 mg increased levels of testosterone (T); doses of 30 and 100 mg increased levels of T by more than 80% * Levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) were also elevated with single oral doses of 30 and 100 mg * Levels of T, LH and FSH peaked between 3 and 7 days post-dose and elevations induced by higher doses were maintained through at least 28 days * T levels plateaued at the high normal range of 30-40 nmol/L between 7 and 28 days post-dose regardless of lasofoxifene dose or LH levels “This is the first time clinical efficacy data for lasofoxifene in males has been presented,” commented Matthew W. Foehr, Executive Vice President and Chief Operating Officer of Ligand. “Significant market need exists for safe, effective and convenient oral treatments in this area, as approximately 5 million men in the US suffer from low testosterone. These data create yet another potential clinical-stage partnering opportunity for our lasofoxifene asset in a variety of growing and higher-profile men's health applications, including secondary hypogonadism and other disorders that are associated with low testosterone levels.”