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Mifepristone is a synthetic steroid that acts as a competitive antagonist at both the glucocorticoid receptor (GR) and the progesterone receptor (PR). Originally developed by Roussel-Uclaf, it is currently marketed by Corcept Therapeutics under the brand name Korlym for the treatment of hyperglycemia secondary to endogenous hypercortisolism in adult patients with endogenous Cushing's syndrome who have type 2 diabetes mellitus or glucose intolerance and have failed surgery or are not candidates for surgery. By blocking the GR, mifepristone antagonizes the effects of excess cortisol on glucose metabolism and adipose tissue. Additionally, its progesterone receptor antagonism has led to its use in reproductive health and its investigation as a potential treatment for various hormone-dependent cancers, including triple-negative breast cancer and castration-resistant prostate cancer, where it may help overcome cortisol-mediated resistance to therapy.
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