Peringatan Keamanan

There is no information available on the toxicity profile of clascoterone, such as LD50 and overdose in humans.

Clascoterone

DB12499

small molecule approved investigational

Deskripsi

Clascoterone (cortexolone 17?-propionate, CB-03-01) is a novel antagonist of androgen receptors. It binds to androgen receptors with high affinity.A218771 By competing with androgens for binding to androgen receptors, clascoterone works by blocking the androgen receptor signalling cascades that promote acne pathogenesis, such as sebaceous gland proliferation, excess sebum production, and inflammatory pathways.A218846 In August 2020, FDA approved clascoterone for the first-in-class topical treatment of acne (acne vulgaris) in male and female patients 12 years and older.L15621 Clascoterone is also being investigated as a novel treatment for androgenetic alopecia.A218766

Struktur Molekul 2D

Berat 402.531
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) There is limited information on the half life of clascoterone.[L15626]
Volume Distribusi There is no information available on the volume of distribution.
Klirens (Clearance) There is limited information on clearance of clascoterone.[L15626]

Absorpsi

Upon topical application, clascoteronet permeates the skin to the dermal levels with minimal systemic absorption.A218776 In clinical trials, adult subjects with moderate to severe facial acne vulgaris received twice-daily topical application of six grams of clascoterone. The steady-state concentrations of the drug were reached within five days. Following two weeks, the mean ± SD Cmax was 4.5 ± 2.9 ng/mL and the mean ± SD area under the plasma concentration-time over the dosing interval (AUC?) was 37.1 ± 22.3 h*ng/mL. The mean ± SD average plasma concentration (Cavg) was 3.1 ± 1.9 ng/mL.L15626

Metabolisme

According to in vitro and clinical studies, the main possible primary metabolite of clascoterone is cortexolone, which is an inactive metabolite. The plasma concentrations of cortexolone were generally below or near the lower limit of quantitation (0.5 ng/mL).L15626 Although clascoterone penetrates the skin, the systemic activity of the drug is limited due to rapid hydrolysis of clascoterone into the inactive metabolite by skin and plasma esterases,A218761,A218846,A218861 namely carboxylesterase.A218851

Rute Eliminasi

Excretion of clascoterone has not been fully characterized in humans.L15626 Upon topical application, clascoterone is quickly hydrolyzed in the epidermis.A218761

Interaksi Obat

1 Data
Flotufolastat F-18 Clascoterone may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent.

Target Protein

Androgen receptor AR

Referensi & Sumber

Artikel (PubMed)
  • PMID: 32320027
    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.
  • PMID: 30811143
    Rosette C, Rosette N, Mazzetti A, Moro L, Gerloni M: Cortexolone 17alpha-Propionate (Clascoterone) is an Androgen Receptor Antagonist in Dermal Papilla Cells In Vitro J Drugs Dermatol. 2019 Feb 1;18(2):197-201.
  • PMID: 31141847
    Rosette C, Agan FJ, Mazzetti A, Moro L, Gerloni M: Cortexolone 17alpha-propionate (Clascoterone) Is a Novel Androgen Receptor Antagonist that Inhibits Production of Lipids and Inflammatory Cytokines from Sebocytes In Vitro J Drugs Dermatol. 2019 May 1;18(5):412-418.
  • PMID: 31251549
    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.
  • PMID: 32348828
    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.
  • PMID: 31357203
    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.
  • PMID: 26082583
    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.
  • PMID: -
    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.

Contoh Produk & Brand

Produk: 2 • International brands: 2
Produk
  • Winlevi
    Cream • 1 g/100g • Topical • US • Approved
  • Winlevi
    Cream • 1 % w/w • Topical • Canada • Approved
International Brands
  • Breezula
  • Winlevi

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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