Neurocrine Biosciences announces positive phase I results with GnRH receptor antagonist.(gonadotropin-releasing hormone receptor antagonist)

2002 JUN 20 - (NewsRx.com & NewsRx.net) -- Neurocrine Biosciences, Inc., (NBIX) announced the completion of the first phase I clinical trial with its proprietary, orally active small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist compound for the treatment of women's health disorders and prostate cancer.

Initial pharmacokinetic evaluation indicates rapid absorption and good dose-linearity for both C[subscript]max (maximum concentration attained) and AUC (area under the plasma concentration time curve). Initial pharmacodynamic assessment after a single dose indicates rapid suppression of circulating leutinizing hormone (LH) up to approximately 60% in a dose-dependent manner. Suppression of LH was observed for all dose groups compared with placebo. The compound was well tolerated and no laboratory or clinical safety issues were noted.

This first-in-human study was a randomized, double-blind, placebo-controlled, single-dose, trial conducted in 56 normal healthy postmenopausal women 45-65 years of age, and was designed to evaluate the safety, tolerability, pharmacokinetics, and pharmacodynamics, including endocrine profiles, over a range of 8 escalating doses. A 2-week multiple-dose, dose-escalating, phase I, placebo-controlled clinical trial will be initiated shortly to further evaluate the safety and endocrine profiles of this compound to prepare for phase II safety and efficacy evaluation.

"Because of the well established mechanism of action for injectable drugs acting at the GnRH receptor, the level of LH suppression which we observed in this first in human clinical study gives us confidence that this orally-active compound will be effective in treating hormone dependent diseases such as endometriosis, uterine ...