2015 Antineoplastics

Drugs that inhibit aromatase: AMINOGLUTETHIMIDE, ANASTROZOLE, LETROZOLE, EXEMESTANE

Mechanism

Aromatase inhibitors target the conversion of testosterone and androstenedione to estradiol and estrone, respectively.  Steroid analogues, such as EXEMESTANE, IRREVERSIBLY inhibit aromatase, while non-steroidal drugs (AMINOGLUTETHIMIDE, ANASTROZOLE and LETROZOLE) compete REVERSIBLY for the androstenedione binding site.  AMINOGLUTETHIMIDE also blocks conversion of cholesterol to pregnenolone, decreasing concentrations of adrenal gluco- and mineralocorticoids as well as sex hormones.

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Email: Dr. Janet Fitzakerley | ©2015 University of Minnesota Medical School Duluth | Last modified: 11-apr-15 9:39 AM