Identification of the Clinical Candidate (<i>R</i>)-(1-(4-Fluorophenyl)-6-((1-methyl-1<i>H</i>-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1<i>H</i>-pyrazolo[3,4-<i>g</i>]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist
Hazel Hunt(Corcept Therapeutics (United States)), Joseph K. Belanoff(Corcept Therapeutics (United States)), Iain A. S. Walters(Signature Research (United States)), Benoit Gourdet(Signature Research (United States)), Jennifer A. Thomas(Signature Research (United States)), Naomi Barton(Signature Research (United States)), John Unitt(Signature Research (United States)), Timothy D. Phillips(Signature Research (United States)), Denise Swift(Signature Research (United States)), Emily P. Eaton(Signature Research (United States))
Cited by 67Open Access
Abstract
The nonselective glucocorticoid receptor (GR) antagonist mifepristone has been approved in the U.S. for the treatment of selected patients with Cushing's syndrome. While this drug is highly effective, lack of selectivity for GR leads to unwanted side effects in some patients. Optimization of the previously described fused azadecalin series of selective GR antagonists led to the identification of CORT125134, which is currently being evaluated in a phase 2 clinical study in patients with Cushing's syndrome.
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