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Description: Exemestane (formerly also known as FCE24304, PNU155971; FCE 24304; EXE), a drug used in ER-positive breast cancer, is a synthetic and potent aromatase inhibitor, which inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively. Exemestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens. Structurally similar to androstenedione, exemestane might have a big impact on androgenic effect.
References: J Steroid Biochem Mol Biol. 1994 Jun; 49(4-6):289-94; Clin Cancer Res. 2004 Sep 1; 10(17):5717-23.
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