The preclinical and clinical profile of dienogest. A short overview

Dienogest is the first of the so-called hybrid progestins which on the basi s of their unique chemical structure combine the typical pharmacodynamic pr operties of progesterone derivatives (excellent tolerability, antiandrogeni c action, low antigonadotropic efficacy, mainly peripheral mode of action, low penetration through the skin, dose in the milligram range) with those o f the modern 19-norprogestins possessing a 17 alpha-ethinyl group (strong p rogestational activity on the endometrium, short half-life, high oral bioav ailability, low liver impact, inconspicuous toxicological or genotoxicologi cal pattern, perfect cycle control if combined with estrogens, e.g., for or al contraception). The present paper gives a short overview of the preclini cal profile of dienogest and the different clinical options, including the treatment of endometriosis, oral contraception (including combination with the natural estrogen 17 beta-estradiol), and hormone replacement therapy. ( C) 1999 Prous Science. All rights reserved.