What is past is prologue: estrogen/progestin replacement tomorrow

Abstract

The 'depletion' of the granulosa cells and associated cessation of the secretion of 17 b -estradiol by the ovary mark the menopause. The well-known 17 b -estradiol deficiency syndrome occurs. Replacement with 17 b -estradiol (in the most varying dosages and in different administration regimens) will remain the 'gold standard' in times to come. Combination with a progestin-delivering intrauterine system can optimize 17 b -estradiol replacement. Future developments include dietary measures (so-called 'nutriceuticals') or the potency-enhanced phytoestrogens, essentially improved selective estrogen receptor modulators (SERMs) including central nervous system-focused estrogens with reduced peripheral action, and the estrogen sulfamates with a unique pharmacokinetic pattern after oral administration ('oral patch'). In the field of progestins, the so-called hybrid progestins (e.g. dienogest, drospirenone, and the selective progesterone receptor modulators (mesoprogestins)) will probably predominate. A very attractive approach is the use of selective androgen-receptor modulators (SARMs) as non-masculinizing androgens.

Hormonal contraception without estrogens

“…New compounds for hormonal contraception are rather rare, with only 22 progestogens (norprogestogens as well as derivatives of 17a-hydroxyprogesterone) having been launched worldwide since the 1960s. The launch of the different progestogens can be seen as two large waves in the 1960s and 1980s (Figure 1), whilst the most recent developments have been dienogest, drospirenone and trimegestone (Oettel et al, 2001;Sitruk-Ware, 2002). At present, the pharmaceutical industry commits only a small amount of capacity to the search for and development of new progestogens.…”