Synthesis of orally active small-molecule gonadotropin-releasing hormone antagonists
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This review discusses the biological activity and syntheses of non-peptide, orally active gonadotropin-releasing hormone antagonists that have shown promise for treating sex hormone-related diseases.
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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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- europepmc
- last seen: 2026-09-06T09:34:12.023084+00:00
- pubmed
- last seen: 2026-05-13T22:12:26.305326+00:00
License: public-domain-us
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Courtesy of the U.S. National Library of Medicine
Courtesy of the U.S. National Library of Medicine