Enclomiphene Citrate

Clomiphene is being studied for its potential to increase serum total testosterone levels while maintaining sperm counts in the normal range in men with secondary hypogonadism.

Clomiphene is thus a powerful estrogen receptor (ER) modulator. It acts as an ER antagonist in humans, sheep, and rabbits and an ER agonist in rats. Enclomiphene works ny inhibiting the binding of 17beta-estradiol in isolated rabbit uterus. It decreases E2-induced inhibition of follicle stimulating hormone (FSH) secretion in primary sheep pituitary cells in a concentration-dependent manner. Enclomiphene (0.25 and 0.5 mg/animal) inhibits spermatogenesis and decreases serum luteinizing hormone (LH) and testosterone levels in intact or castrated rats. Formulations containing clomiphene have been used in the treatment of ovarian dysfunction. In addition, this compound may bind to estrogen receptors on breast cancer cells, resulting in the inhibition of estrogen-stimulated proliferation in susceptible cell populations.