Ligand Pharma (LGND) Initiates Phase I Trial with LGD-4033

June 17, 2009 8:20 AM EDT

Ligand Pharmaceuticals Incorporated (NASDAQ: LGND) today announced the initiation of a Phase I clinical trial with LGD-4033, a next-generation selective androgen receptor modulator designed to provide the benefits of androgen receptor stimulation on skeletal muscle and bone without the side effects of currently marketed androgens. The Phase I study will evaluate the safety, tolerability and pharmacokinetic profile of orally administered LGD-4033.

In preclinical studies, LGD-4033 demonstrated a highly tissue-selective profile with increased skeletal muscle mass and bone mineral density while largely sparing the prostate in males and masculinizing effects in females. Extensive preclinical studies with LGD-4033 demonstrate the following:

• LGD-4033 is highly selective for the androgen receptor.
  
• Gene transcriptional regulation assays using muscle or bone cells demonstrate that LGD-4033 is a potent, full agonist producing efficacy comparable to the natural steroidal androgen dihydrotestosterone.
  
• In repeat oral dosing studies LGD-4033 increases skeletal muscle mass.
  
• In the ovariectomized rat model of post-menopausal osteoporosis, LGD-4033 had anabolic activity in cortical bone, significantly increasing cortical bone formation rates, bone strength and bone density. LGD-4033 also suppressed bone turnover at cancellous bone sites, leading to an increase in lumbar spine bone density and strength.
  
• In repeat oral dosing studies, LGD-4033 is a weak partial agonist on the prostate gland with more than 500-fold selectivity for muscle versus prostate. This indicates an absence of the prostatic hypertrophy that occurs with the currently marked androgens.

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