17?-Hydroxy exemestane

Description

17?-Hydroxy exemestane 17-H-EXE is the primary active metabolite of Exemestane HY-13632 . 17?-Hydroxy exemestane is an aromatase inhibitor IC50 = 69 nM and an androgen receptor AR agonist IC50 = 39.6 nM that is selective for AR over estrogen receptor ? ER?; IC50 = 21.2 ?M . 17?-Hydroxy exemestane stimulates growth of AR- and ER?-positive MCF-7 EC50= 2.7 ?M and T47D breast cancer cells EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17?-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats.