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Updated: Aug 20, 2026

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
Published on: March 21, 2017
Synthesis of orally active small-molecule gonadotropin-releasing hormone antagonists
1Neurocrine Biosciences Inc, San Diego, CA 92130, USA.
Abstract:
Recent success in the search for orally active gonadotropin-releasing hormone antagonists for the treatment of sex hormone-related diseases, such as endometriosis, uterine fibroids and prostate cancer, has resulted in the discovery of non-peptide compounds from several different chemical classes. At least two such compounds have advanced to the clinic for testing in humans, while multiple series of compounds have demonstrated oral activity in animal studies. This review covers the basic biological activity and the syntheses of these compounds, focusing on progress made over the past year.
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