Research Area: Endocrinology
Biological Activity:
Exemestane is an irreversible, oral steroidal aromatase inhibitor used in the adjuvant treatment of hormonally-responsive breast cancer in postmenopausal women. [1]Its structure was related to the natural substrate androstenedione and it acts as a false substrate for the aromatase enzyme, an effect also known as "suicide inhibition."[1]The estrogen suppression rate for exemestane varies from 85% for estradiol (E2) to 95% for estrone (E1). [1]Exemestane was found to inhibit human placental aromatase with IC50 of 42 nM. [2]References on Exemestane[] Biochimica et Biophysica Acta, 2002, 1587:326– 337