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Anastrozole


Mechanism of action:

Anastrozole is a nonsteroidal aromatase inhibitor. Estrogens are mainly produced in peripheral tissues such as adipose tissue, muscle, and liver, where aromatase converts androstenedione and testosterone into estrone and estradiol, respectively. Anastrozole reversibly inhibits the active site of aromatase, blocking the conversion of androgens into estrogens and thereby lowering estrogen levels in the blood and tissues.

Reference(s):

1. Miyajima M et al. (2013). Investigation of the effect of active efflux at the blood-brain barrier on the distribution of nonsteroidal aromatase inhibitors in the central nervous system. J Pharm Sci. 


2. Gervasini G et al. (2017). Polymorphisms in ABCB1 and CYP19A1 genes affect anastrozole plasma concentrations and clinical outcomes in postmenopausal breast cancer patients. Br J Clin Pharmacol.

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