Citations for: Laine, K.; Yasar, U.; Widen, J.; Tybring, G. A Screening Study on the Liability of Eight Different Female Sex Steroids to Inhibit CYP2C9, 2C19 and 3A4 Activities in Human Liver Microsomes. Pharmacol. Toxicol. 2003, 93 (2), 77–81.

Entry Type
Name
Value
Parent Entry
Pharmacology Data Field
  • Competitive inhibitor of 3β-hydroxysteroid dehydrogenase/Δ5-4 isomerase II (3β-HSDII), which is essential for the biosynthesis of sex steroids and corticosteroids.
  • CYP3A4: substrate, inducer
  • CYP2C8, CYP2C9: inhibitor
Medroxy­progesterone Acetate (API)
Metabolites
N/A
Metabolites
N/A
Pharmacology Data Field
  • Inhibits CYP2C9, CYP2C19, CYP3A4, CYP2B6
  • After formation of very reactive intermediate by oxidation of C17 ethinyl, can irreversibly inhibit cytochrome P450 enzymes (e.g. CYP2C8, CYP3A4). Thus it exerts strong effects on hepatic metabolism.
  • Nuclear receptor subfamily 1 group I member 2: agonist
  • Bile salt export pump: inhibitor, inducer
  • Sodium/bile acid cotransporter: inducer
  • Canalicular multispecific organic anion transporter 1: inducer
  • Multidrug resistance protein 1: substrate
  • Uridine diphosphate glucuronosyltransferase (UGT): inducer
Ethinyl Estradiol (API)
Pharmacology Data Field
  • CYP3A4: inducer (PubChem, Toxnet), inhibitor (KEGG, Laine et al.)
  • CYP3A7, CYP3A5, CYP2C19: inhibitor
Gestodene (API)
Pharmacology Data Field
CYP2C19, CYP3A4: inhibitor
Etonogestrel (API)