New progestagens for contraceptive use

Regine Sitruk-Ware, Régine Sitruk‐Ware
Human Reproduction Update · 2005 · vol. 12(2) , pp. 169–178 · doi:10.1093/humupd/dmi046 · PMID:16291771 · W2100560126
Review OA: closed CC0 ⤵ 38 in-corpus citations
View on OpenAlex View on PubMed View at publisher
⚙ AI-generated summary by gemini-2.5-flash-lite, 2026-06-09 ⓘ

New progestins like dienogest, drospirenone, Nestorone, nomegestrol acetate, and trimegestone have been developed with improved selectivity and reduced androgenic effects for contraceptive use.

One-sentence paraphrase of the abstract; not a substitute for reading it. No clinical advice. How this works

Abstract

The progestins have different pharmacologic properties depending upon the parent molecule, usually testosterone or progesterone (P), from which they are derived. Very small structural changes in the parent molecule may induce considerable differences in the activity of the derivative. In hormonal contraceptives, progestins represent the major agent designed for suppressing ovulation and are used in combination with estrogen (E) usually ethinyl-estradiol (EE). The development of new generations of progestins with improved selectivity profiles has been a great challenge. Steroidal and nonsteroidal progesterone receptor (PR) agonists have been synthesized as well, although the latter are still in a very early stage of development. Several new progestins, have been synthesized in the last two decades. These include dienogest (DNG), drospirenone (DRSP), Nestorone (NES), nomegestrol acetate (NOMAc) and trimegestone (TMG). These new progestins have been designed to have no androgenic or estrogenic actions and to be closer in activity to the physiological hormone P. DRSP differs from the classic progestins as it is derived from spirolactone. It is essentially an antimineralocorticoid steroid with no androgenic effect but a partial antiandrogenic effect. The antiovulatory potency of the different progestins varies. TMG and NES are the most potent progestins synthesized to date, followed by two of the older progestins, keto-desogestrel (keto-DSG) and levonorgestrel (LNG). The new molecules TMG, DRSP and DNG also have antiandrogenic activity. Striking differences exist regarding the side effects among the progestins and the combination with EE leads to other reactions related to the E itself and whether the associated progestin counterbalances, more or less, the estrogenic action. The 19-norprogesterone molecules and the new molecules DRSP and DNG are not androgenic and, therefore, have no negative effect on the lipid profile. Given their pharmacological properties, it is likely that the new progestins may have neutral effects on metabolic or vascular risks. However, this hypothesis must be confirmed in large clinical trials.

My notes (saved in your browser only)

MeSH descriptors

Contraceptive Agents, Female Progestins Progestins Androstenes Androstenes Breast Breast Contraceptive Agents, Female Female Humans Megestrol Megestrol Nandrolone Nandrolone Nandrolone Norpregnadienes Norpregnadienes Norprogesterones Norprogesterones Pregnanes

Citation neighborhood (2-hop)

Papers in the corpus that this work cites (lower rings, blue) and that cite this one (upper rings, green). Dot size scales with the paper's in-corpus citation count — bigger dot = more influential within the endo/adeno field. Click a dot to open that paper. Outer rings show 2-hop neighbours — papers reached through the immediate citers/citees. [ collapse to 1-hop ]

References (64)

Cited by (31)

Source provenance

openalex
last seen: 2026-05-11T06:09:19.794676+00:00
pubmed
last seen: 2026-10-08T21:03:30.943773+00:00
unpaywall
last seen: 2026-10-15T06:24:24.424788+00:00
License: CC0 · commercial use OK