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The Identification of the Clinical Candidate (R)-(1-(4-fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1Hpyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134):– A Selective Glucocorticoid Receptor (GR) Antagonist

Hunt, H.J., Belanoff, J.K., Walters, I., Gourdet, B., Thomas, J., Barton, N., Unitt, J., Phillips, T., Swift, D., Eaton, E.

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.

Ref: J Med Chem. 2017 Apr 27;60(8):3405-3421

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