1. APIs
  2. Desogestrel
  3. Metabolites

Desogestrel Metabolites

Name Structure Notes
3-Keto-5α-dihydrodesogestrel structure Lower Progesterone Receptor and Estrogen Receptor activity than etonogestrel.
Other Desogestrel Metabolites Glucuronide and sulfate conjugates of desogestrel and some of its metabolites (3β-hydroxydesogestrel, 15β-hydroxydesogestrel) are also formed.
15β-Hydroxydesogestrel structure
16-Hydroxydesogestrel structure
6α-Hydroxydesogestrel structure
2-Hydroxydesogestrel structure Pharmacologically inactive.
3β,5α-Tetrahydrodesogestrel structure
3α,5α-Tetrahydrodesogestrel structure
13-Hydroxyethyldesogestrel structure
15α-Hydroxydesogestrel structure
6β-Hydroxydesogestrel structure Catalyzed by CYP3A4.
5α-Dihydrodesogestrel structure
3β-Hydroxydesogestrel structure Minor metabolite. Rapidly oxidized to etonogestrel. Initial in vitro studies indicated that CYP2C9 and CYP2C19 were responsible for this conversion, however later human in vivo studies refuted this and indicated CYP3A4 (Korhonen et al. 2005).
3α-Hydroxydesogestrel structure Primary metabolite. Rapidly oxidized to etonogestrel. Initial in vitro studies indicated that CYP2C9 and CYP2C19 were responsible for this conversion, however later human in vivo studies refuted this and indicated CYP3A4 (Korhonen et al. 2005).
Etonogestrel structure Primary metabolite of desogestrel, resulting from the rapid oxidation of desogestrel metabolites 3α- and 3β-hydroxydesogestrel by 3β-hydroxysteroid dehydrogenase/Delta 5-->4 isomerase type 1.