The Biology of Aromatase Inhibition

Aromatase is a naturally occurring enzyme that catalyzes the conversion of androgens to estrogen.  An AI can be used to regulate the quantity of estrogen by inhibiting the conversion of androgens to estrogen.

 

Estrogens are the hormones that govern a woman’s reproductive life from puberty to menopause.  At puberty, hormones produced in the hypothalamus gland stimulate the anterior pituitary gland to produce other hormones that cause the ovaries to develop and produce estrogen.  During the reproductive years, estrogen interacts with other hormones to control the menstrual cycle, including the growth of the endometrium, which is the lining of the uterus.

At almost any stage of life too much or too little estrogen can be related to medical conditions that adversely affect quality of life and can be life-threatening.  Medical research has produced numerous therapeutic approaches to regulate estrogen to improve the lives of patients with estrogen-dependent conditions.

One such approach involves AIs, such as Meditrina’s lead product candidate, MPI-676. This class of drugs decreases the amount of estrogen circulating in the body by binding to and inhibiting the enzyme aromatase, which converts certain hormones to estrogen, locally in the endometriotic tissue.