Citations for: Oettel, M.; Breitbarth, H.; Elger, W.; Gräser, T.; Hübler, D.; Kaufmann, G.; Moore, C.; Patchev, V.; Römer, W.; Schröder, J.; et al. The Pharmacological Profile of Dienogest. Eur. J. Contracept. Reprod. Heal. Care 1999, 4 (sup1), 2–13.

Entry Type
Name
Value
Parent Entry
Pharmacology Data Field
Agonist. Some antagonist behavior.
Dienogest (API)
Pharmacology Data Field
Antagonist (40% of CPA, the most potent anti-androgenic progestin)
Dienogest (API)
Pharmacology Data Field
Weak or no agonist and antagonist activity
Dienogest (API)
Pharmacology Data Field
Low to no activity
Dienogest (API)
Pharmacology Data Field
No activity
Dienogest (API)
Pharmacology Data Field
90-96.2%
Dienogest (API)
Pharmacology Data Field
8-10 h
Dienogest (API)
Pharmacology Data Field
90% bound to serum albumin, 10% free. No binding to SHBG or CBG.
Dienogest (API)
Toxicology Data Field
No evidence in vivo and in vitro.
Dienogest (API)
Toxicology Data Field
No evidence in vivo and in vitro.
Dienogest (API)
Pharmacology Data Field
Mainly via kidneys.
Dienogest (API)
Pharmacology Data Field
Oettel et al: 75 mL/h/kg
Foster et al: 3 L/h from 2 mg/day oral dose
Dienogest (API)
Pharmacology Data Field
3β-hydroxysteroid dehydrogenase-Δ5-4-isomerase: inhibitor
Dienogest (API)
Pharmacology Data Field
Oettel: 4.0 ng/mL
Foster: 1 mg/day oral dose for inhibition of ovulation in cyclical women
Dienogest (API)
Metabolites
N/A
Metabolites Data Field
  • STS 749
  • 17α-cyanomethyl-11β,17-dihydroxy-4,9-estradien-3- one
11β-Hydroxydienogest (Metabolite)
Metabolites Data Field
STS 825
17α-Cyanomethyl-1,3,5(10),9(11)-estratetraene-3,17-diol (Metabolite)