CLASCOTERONE

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 Search

SMILES

[H][C@@]12CC[C@](OC(=O)CC)(C(=O)CO)[C@@]1(C)CC[C@@]3([H])[C@@]2([H])CCC4=CC(=O)CC[C@]34C

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
Sources: http://www.cassiopea.com/activities/product-pipeline/winlevi.aspx | https://www.ncbi.nlm.nih.gov/mesh/67496269

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

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
androgen receptor 3 Target ID: 1.01838792E8 Gene Symbol: Ar Sources: http://www.cassiopea.com/activities/product-pipeline/winlevi.aspx	Antagonist 2778

Conditions

Condition	Modality	Targets	Highest Phase	Product
Androgenic alopecia 8 Sources: http://www.cassiopea.com/activities/product-pipeline/breezula.aspx	Primary		Phase II 1132	BREEZULA Approved Use Unknown
Acne vulgaris 34 Sources: http://www.cassiopea.com/activities/product-pipeline/winlevi.aspx	Primary		Phase III 656	WINLEVI Approved Use Unknown

PubMed

Title	Date	PubMed
Cortexolone 17α-propionate 1% cream, a new potent antiandrogen for topical treatment of acne vulgaris. A pilot randomized, double-blind comparative study vs. placebo and tretinoin 0·05% cream.	2011 Jul	21428978
The use of hormonal agents in the treatment of acne.	2016 Jun	27416311

Patents

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

Name

Type

Language

CLASCOTERONE

Official Name

English

Clascoterone [WHO-DD]

Common Name

English

PREGN-4-ENE-3,20-DIONE, 17,21-DIHYDROXY-, 17-PROPIONATE

Systematic Name

English

CLASCOTERONE [USAN]

Common Name

English

WINLEVI

Brand Name

English

CLASCOTERONE [MI]

Common Name

English

clascoterone [INN]

Common Name

English

21-Hydroxy-3,20-dioxopregn-4-en-17-yl propanoate

Systematic Name

English

PREGN-4-ENE-3,20-DIONE, 21-HYDROXY-17-(1-OXOPROPOXY)-

Systematic Name

English

CORTODOXONE 17.ALPHA.-PROPIONATE

Common Name

English

CORTEXOLONE 17.ALPHA.-PROPIONATE

Common Name

English

CLASCOTERONE [ORANGE BOOK]

Common Name

English

BREEZULA

Brand Name

English

CB-03-01

Code

English

Code System Code Type Description

ChEMBL

CHEMBL3545016