Romanian Society of Pharmaceutical Sciences
 

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AROMATASE INHIBITORS IN MEN – OFF-LABEL USE, MISUSE, ABUSE AND DOPING

CAMIL-EUGEN VARI1, BIANCA-EUGENIA ŐSZ1*, AMALIA MIKLOS2, ANCA BERBECARUIOVAN4, AMELIA TERO-VESCAN3

1.Pharmacology and Clinical Pharmacy Department, Faculty of Pharmacy, University of Medicine and Pharmacy Tîrgu Mureş, Romania
2 .Advanced Medical and Pharmaceutical Research Centre (CCMAF), Faculty of Pharmacy, University of Medicine and Pharmacy Tîrgu Mureş, Romania
3 .Biochemistry Department, Faculty of Pharmacy, University of Medicine and Pharmacy Tîrgu Mureş, Romania
4 .Faculty of Pharmacy, University of Medicine and Pharmacy, 2 Petru Rareş, 200349, Craiova, Romania

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Aromatase (oestrogen synthase, CYP19A1, EC 1.14.14.1) is a monooxygenase from the cytochrome P450 family involved in the conversion of androgens to oestrogens. It is the final step in steroidogenesis of oestrogens, catalysing androgen aromatisation (with the formation of oestradiol from testosterone, and of oestrone from androstenedione, respectively). Tissue localization is ubiquitous, being found mainly in gonads, brain, adipose tissue, bone. Congenital aromatase deficiency is a very rare genetic disease characterized by androgen impregnation, pseudo-hermaphroditism and osteopenia in women, and high stature in both sexes, due to delayed ossification of growth cartilage. Aromatase inhibitors (anastrozole, letrozole, exemestane) are indicated according to data included in the marketing authorization, in the treatment of oestrogen-dependent cancers in women (breast cancer with positive oestrogen receptors in postmenopausal women, including relapsing forms after prior therapy with antioestrogens). Aromatase inhibitors have no official recommendation in male pathology. However, these substances are used off-label in selected cases of male infertility (in case of inadequate testosterone/ oestradiol ratio, and in patients with hypogonadotropic hypogonadism, including that caused by anabolic steroid abuse). Also, aromatase inhibitors are detoured from medical use in athletes, as indirect doping, as corrective treatment of paradoxical feminisation (gynecomastia), following administration of androgens and as “therapy” after doping cycle to restore endogenous testicular secretory activity.