Synonym
CB-03-01; CB 03-01; CB0301; CB-0301; CB 0301; CB03-01; cortexolone 17alpha-propionate; Clascoterone;
IUPAC/Chemical Name
(8R,9S,10R,13S,14S,17R)-17-(2-hydroxyacetyl)-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl propionate
InChi Key
GPNHMOZDMYNCPO-PDUMRIMRSA-N
InChi Code
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
SMILES Code
CCC(O[C@]1(C(CO)=O)CC[C@@]2([H])[C@]3([H])CCC4=CC(CC[C@]4(C)[C@@]3([H])CC[C@]12C)=O)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
In vitro activity:
Clascoterone was found to bind the androgen receptor (AR) with high affinity in vitro, inhibit AR-regulated transcription in a reporter cell line, and antagonize androgen-regulated lipid and inflammatory cytokine production in a dose-dependent manner in human primary sebocytes.
Reference: J Drugs Dermatol. 2019 May 1;18(5):412-418. https://pubmed.ncbi.nlm.nih.gov/31141847/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
20.0 |
49.69 |
| DMSO |
63.3 |
157.34 |
| Ethanol |
50.0 |
0.05 |
| Ethanol:PBS (pH 7.2) (1:9) |
0.1 |
0.25 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
402.53
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Rosette C, Agan FJ, Mazzetti A, Moro L, Gerloni M. Cortexolone 17α-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: 31141847.
2. Rosette C, Rosette N, Mazzetti A, Moro L, Gerloni M. Cortexolone 17α-Propionate (Clascoterone) is an Androgen Receptor Antagonist in Dermal Papilla Cells In Vitro. J Drugs Dermatol. 2019 Feb 1;18(2):197-201. PMID: 30811143.
In vitro protocol:
1. Rosette C, Agan FJ, Mazzetti A, Moro L, Gerloni M. Cortexolone 17α-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: 31141847.
2. Rosette C, Rosette N, Mazzetti A, Moro L, Gerloni M. Cortexolone 17α-Propionate (Clascoterone) is an Androgen Receptor Antagonist in Dermal Papilla Cells In Vitro. J Drugs Dermatol. 2019 Feb 1;18(2):197-201. PMID: 30811143.
1: Burma NE, Woo TE, Parsons L. Topical Clascoterone for Acne Vulgaris. Skin Therapy Lett. 2022 Jan;27(1):1-3. PMID: 35081302.
2: Dhillon S. Clascoterone: First Approval. Drugs. 2020 Nov;80(16):1745-1750. doi: 10.1007/s40265-020-01417-6. PMID: 33030710.
3: Manjaly C, Martinez J, Barbieri J, Mostaghimi A. Clascoterone for treatment of acne. Drugs Today (Barc). 2023 Feb;59(2):71-81. doi: 10.1358/dot.2023.59.2.3507749. PMID: 36811407.
4: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Clascoterone. 2023 Jan 15. PMID: 36701501.
5: 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 Jun 1;156(6):621-630. doi: 10.1001/jamadermatol.2020.0465. PMID: 32320027; PMCID: PMC7177662.
6: Kalabalik-Hoganson J, Frey KM, Ozdener-Poyraz AE, Slugocki M. Clascoterone: A Novel Topical Androgen Receptor Inhibitor for the Treatment of Acne. Ann Pharmacother. 2021 Oct;55(10):1290-1296. doi: 10.1177/1060028021992053. Epub 2021 Feb 3. PMID: 33533262.
7: Harris C. Clascoterone (Winlevi) for the Treatment of Acne. Am Fam Physician. 2021 Jul 1;104(1):93-94. PMID: 34264597.
8: Piszczatoski CR, Powell J. Topical Clascoterone: The First Novel Agent for Acne Vulgaris in 40 Years. Clin Ther. 2021 Oct;43(10):1638-1644. doi: 10.1016/j.clinthera.2021.08.007. Epub 2021 Oct 2. PMID: 34607697.
9: Kircik LH. Androgens and acne: perspectives on clascoterone, the first topical androgen receptor antagonist. Expert Opin Pharmacother. 2021 Sep;22(13):1801-1806. doi: 10.1080/14656566.2021.1918100. Epub 2021 Apr 27. PMID: 33906537.
10: Clascoterone. Am J Health Syst Pharm. 2022 Jan 24;79(3):115-116. doi: 10.1093/ajhp/zxab416. PMID: 34849570.
11: Drake L, Reyes-Hadsall S, Barbieri JS, Mostaghimi A. New Developments in Topical Acne Therapy. Am J Clin Dermatol. 2022 Mar;23(2):125-136. doi: 10.1007/s40257-021-00666-9. Epub 2022 Jan 18. PMID: 35041198.
12: Clascoterone cream (Winlevi) for acne. Med Lett Drugs Ther. 2021 Dec 27;63(1640):202-204. PMID: 35100239.
13: Han JJ, Faletsky A, Barbieri JS, Mostaghimi A. New Acne Therapies and Updates on Use of Spironolactone and Isotretinoin: A Narrative Review. Dermatol Ther (Heidelb). 2021 Feb;11(1):79-91. doi: 10.1007/s13555-020-00481-w. Epub 2021 Jan 6. PMID: 33409936; PMCID: PMC7859022.
14: Santhosh P, George M. Clascoterone: a new topical anti-androgen for acne management. Int J Dermatol. 2021 Dec;60(12):1561-1565. doi: 10.1111/ijd.15752. Epub 2021 Jul 9. PMID: 34242398.
15: Del Rosso J, Stein Gold L, Squittieri N, Thiboutot D. Is There a Clinically Relevant Risk of Hyperkalemia with Topical Clascoterone Treatment? J Clin Aesthet Dermatol. 2023 Jun;16(6):20-24. PMID: 37361363; PMCID: PMC10286882.
16: Sanchez C, Keri J. Androgen Receptor Inhibitors in the Treatment of Acne Vulgaris: Efficacy and Safety Profiles of Clascoterone 1% Cream. Clin Cosmet Investig Dermatol. 2022 Jul 15;15:1357-1366. doi: 10.2147/CCID.S289750. PMID: 35874458; PMCID: PMC9297041.
17: Gold M. Clascoterone cream (1%) topical androgen receptor inhibitor for the treatment of acne in patients 12 years and older. Expert Rev Clin Immunol. 2021 Apr;17(4):301-308. doi: 10.1080/1744666X.2021.1894131. Epub 2021 Mar 5. PMID: 33616473.
18: Purvis CG, Balogh EA, Feldman SR. Clascoterone: How the Novel Androgen Receptor Inhibitor Fits Into the Acne Treatment Paradigm. Ann Pharmacother. 2021 Oct;55(10):1297-1299. doi: 10.1177/1060028021992055. Epub 2021 Feb 5. PMID: 33543640.
19: Sun HY, Sebaratnam DF. Clascoterone as a novel treatment for androgenetic alopecia. Clin Exp Dermatol. 2020 Oct;45(7):913-914. doi: 10.1111/ced.14292. Epub 2020 Jun 23. PMID: 32421862.
20: Cunningham KN, Moody K, Alorainy M, Rosmarin D. Use of topical clascoterone for the treatment of hidradenitis suppurativa. JAAD Case Rep. 2023 Apr 15;36:38-39. doi: 10.1016/j.jdcr.2023.04.002. PMID: 37215295; PMCID: PMC10196707.
