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Details

Stereochemistry ABSOLUTE
Molecular Formula C24H34O5
Molecular Weight 402.5238
Optical Activity UNSPECIFIED
Defined Stereocenters 6 / 6
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Clascoterone

SMILES

CCC(=O)O[C@@]1(CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C)C(=O)CO

InChI

InChIKey=GPNHMOZDMYNCPO-PDUMRIMRSA-N
InChI=1S/C24H34O5/c1-4-21(28)29-24(20(27)14-25)12-9-19-17-6-5-15-13-16(26)7-10-22(15,2)18(17)8-11-23(19,24)3/h13,17-19,25H,4-12,14H2,1-3H3/t17-,18+,19+,22+,23+,24+/m1/s1

HIDE SMILES / InChI

Description

Cortexolone 17α-propionate (WINLEVI, BREEZULA) is a steroid belonging to the family of cortexolone derivatives. It is a topical and peripherally selective androgen antagonist. WINLEVI is used for the treatment of acne and has completed Phase II clinical trials and Phase III trials. BREEZULA is used for the treatment of androgenic alopecia and is currently undergoing a Phase II trial in the US.

CNS Activity

CNS Non-penetrant
1,040

Originator

Cosmo Pharmaceuticals
3

Approval Year

2020
691

Targets

Primary TargetPharmacologyConditionPotency
androgen receptor
3
Antagonist
2,849

Conditions

ConditionModalityTargetsHighest PhaseProduct
Androgenic alopecia
8
 Primary
Phase II
1,147
BREEZULA
Acne vulgaris
34
 Primary
Phase III
665
WINLEVI

Cmax

ValueDoseCo-administeredAnalytePopulation
4.81 ng/mL
225 mg 2 times / day multiple, topical
 CLASCOTERONE plasma
Homo sapiens
7.65 ng/mL
225 mg 2 times / day multiple, topical
 CLASCOTERONE plasma
Homo sapiens
1.16 ng/mL
225 mg 2 times / day multiple, topical
 CORTODOXONE plasma
Homo sapiens
1.27 ng/mL
225 mg 2 times / day multiple, topical
 CORTODOXONE plasma
Homo sapiens
4.5 ng/mL
6 g 2 times / day steady-state, topical
 CLASCOTERONE plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
19.96 ng × h/mL
225 mg 2 times / day multiple, topical
 CLASCOTERONE plasma
Homo sapiens
59.86 ng × h/mL
225 mg 2 times / day multiple, topical
 CLASCOTERONE plasma
Homo sapiens
15.52 ng × h/mL
225 mg 2 times / day multiple, topical
 CORTODOXONE plasma
Homo sapiens
11.24 ng × h/mL
225 mg 2 times / day multiple, topical
 CORTODOXONE plasma
Homo sapiens
37.1 ng × h/mL
6 g 2 times / day steady-state, topical
 CLASCOTERONE plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
26.8 h
225 mg 2 times / day multiple, topical
 CLASCOTERONE plasma
Homo sapiens
90.1 h
225 mg 2 times / day multiple, topical
 CORTODOXONE plasma
Homo sapiens

Funbound

ValueDoseCo-administeredAnalytePopulation
11%
CLASCOTERONE plasma
Homo sapiens

Doses

AEs

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
2,217

OverviewOther

Other InhibitorOther SubstrateOther Inducer

Tox targets

PubMed

Patents

US20160303141
1
US9486458
1

Sample Use Guides

In Vivo Use Guide
Cortexolone 17α-propionate 1% cream was applied every 12 hours for 2 weeks in children 9-12 years old with acne.
Route of Administration: Topical
In Vitro Use Guide
Unknown
ACTIVE MOIETY
Structure of Clascoterone
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