Why dienogest as a progestogenic component of postmenopausal nonandrogenichormone replacement therapy?

Dienogest (17 alpha -cyanomethyl-17 beta -hydroxy-4,9-estradien-3-one) comb ines the benefits of norprogestogens with the typical properties of the 17 alpha -hydroxy-progesterone derivatives. Dienogest is the first representat ive of the so-called hybrid progestogens and is entering the hormone replac ement therapy (HRT) market as a progestogenic component of the continuous c ombined regimen containing 2 mg 17 beta -estradiol valerate plus 2 mg dieno gest daily (Lafamme(R) or Climodien(R)). Based on the pharmacodynamic profi le, dienogest is suitable for combined HRT containing nonandrogenic progest ogen. Preclinical and clinical studies show distinct bone protective, antip roliferative, and antiandrogenic activities. Compared with other progestoge ns, the portion of free, biologically available compound in the serum is ve ry high enabling sufficient tissue penetration and additionally, there is a clear dissociation between central nervous system (CNS) and peripheral (en dometrium) activities. Some of the special pharmacodynamic properties of di enogest can be explained by a "nonclassic" mode of action. This progestogen is easily transformed by different microorganisms, thus indicating no envi ronmental risk after excretion. (C) 2001 Prous Science. All rights reserved .