Reaction: Clascoterone to 1 product

Reaction
Reaction type
hydrolysis
Direction
Major circulating metabolite?
Yes
Spontaneous?
No
Activity
inactive
References
  1. Hebert A, Thiboutot D, Stein Gold L, Cartwright M, Gerloni M, Fragasso E, Mazzetti A: Efficacy and Safety of Topical Clascoterone Cream, 1%, for Treatment in Patients With Facial Acne: Two Phase 3 Randomized Clinical Trials. JAMA Dermatol. 2020 Apr 22. pii: 2765025. doi: 10.1001/jamadermatol.2020.0465. [Article]
  2. Mazzetti A, Moro L, Gerloni M, Cartwright M: Pharmacokinetic Profile, Safety, and Tolerability of Clascoterone (Cortexolone 17-alpha propionate, CB-03-01) Topical Cream, 1% in Subjects With Acne Vulgaris: An Open-Label Phase 2a Study J Drugs Dermatol. 2019 Jun 1;18(6):563. [Article]
  3. Eichenfield L, Hebert A, Gold LS, Cartwright M, Fragasso E, Moro L, Mazzetti A: Open-label, long-term extension study to evaluate the safety of clascoterone (CB-03-01) cream, 1% twice daily, in patients with acne vulgaris. J Am Acad Dermatol. 2020 Aug;83(2):477-485. doi: 10.1016/j.jaad.2020.04.087. Epub 2020 Apr 26. [Article]
  4. Pyo SM, Maibach HI: Skin Metabolism: Relevance of Skin Enzymes for Rational Drug Design. Skin Pharmacol Physiol. 2019;32(5):283-294. doi: 10.1159/000501732. Epub 2019 Jul 29. [Article]
  5. Tokudome Y, Katayanagi M, Hashimoto F: Esterase Activity and Intracellular Localization in Reconstructed Human Epidermal Cultured Skin Models. Ann Dermatol. 2015 Jun;27(3):269-74. doi: 10.5021/ad.2015.27.3.269. Epub 2015 May 29. [Article]
  6. Ferraboschi P, Legnani L, Celasco G, Moro L, Ragonesi L, Colombo D: A full conformational characterization of antiandrogen cortexolone-17α-propionate and related compounds through theoretical calculations and nuclear magnetic resonance spectroscopy MedChemComm. 2014 April 4;5:904-914. [Article]
  7. FDA Approved Drug Products: WINLEVI (clascoterone) cream, for topical use [Link]
Comments
Not Available
Enzymes
EnzymeKmVmaxRole
CarboxylesteraseNot AvailableNot Availableimplied