Clascoterone
Identification
- Summary
Clascoterone is an androgen receptor antagonist used for the topical treatment of acne vulgaris in patients 12 years of age and older.
- Brand Names
- Winlevi
- Generic Name
- Clascoterone
- DrugBank Accession Number
- DB12499
- Background
Clascoterone (cortexolone 17α-propionate, CB-03-01) is a novel antagonist of androgen receptors. It binds to androgen receptors with high affinity.3 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.5 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.9 Clascoterone is also being investigated as a novel treatment for androgenetic alopecia.2
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
- Weight
- Average: 402.531
Monoisotopic: 402.240624195 - Chemical Formula
- C24H34O5
- Synonyms
- 11-deoxycortisol 17α-propionate
- Clascoterone
- Cortexolone 17alpha-propionate
- Cortexolone 17α-propionate
- External IDs
- CB-03-01
Pharmacology
- Indication
Clascoterone is indicated for the topical treatment of acne vulgaris in patients 12 years of age and older.10,11
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Acne vulgaris •••••••••••• ••••••••••• ••••• ••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Clascoterone exerts anti-androgenic effects by working as an antagonist at androgen receptors (ARs) expressed throughout the skin, including sebaceous glands, sebocytes, and dermal papilla cells.1 Clascoterone blocks the effects of testosterone and dihydrotestosterone (DHT), which are androgens that bind to the ARs and contribute to the development of androgen-dependent conditions such as acne and alopecia.1 In vitro, the antiandrogenic effects of clascoterone in human primary sebocytes occurred in a dose-dependent manner.3 Clascoterone mediates selective topical activity by mainly targeting androgen receptors at the site of application. It has limited systemic effects.1
In clinical trials, HPA axis suppression was observed as a 30-minute post-stimulation serum cortisol level of ≤18 mcg/dL in 5% of adult subjects and 9% of adolescent subjects with acne vulgaris following two weeks of topical treatment of clascoterone. HPA axis function returned to normal following the discontinuation of drug treatment.10
- Mechanism of action
Acne is a multifactorial skin condition characterized by excess sebum production, epithelial hyperkeratinization, proliferation of the skin commensal bacteria, and inflammation.1,3 Circulating and locally synthesized natural ligands, testosterone and dihydrotestosterone (DHT), serve as causative factors in both males and females. Upon binding of DHT, the DHT-androgen receptor complex dimerizes and translocates to the nucleus where it promotes the transcription of genes involved in acne pathogenesis, including proliferation and differentiation of sebocytes, excess sebum production, and inflammatory cytokine production.3 Clascoterone is a potent antagonist at ARs and competes for androgens in binding to the receptor, thereby inhibiting downstream signalling of ARs that promote acne.1
Androgenetic alopecia is also an androgen-dependent and highly genetic condition. Dihydrotestosterone (DHT) binds to ARs expressed on dermal papilla cells (DPC) in the scalp to induce AR-mediated transcription of genes that contribute to androgenic alopecia. By blocking the interaction between DHT and aARs, clascoterone inhibits AR-regulated transcription and DHT-induced IL-6 synthesis.2
Target Actions Organism AAndrogen receptor antagonistHumans - Absorption
Upon topical application, clascoteronet permeates the skin to the dermal levels with minimal systemic absorption.4 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 (AUCꞇ) was 37.1 ± 22.3 h*ng/mL. The mean ± SD average plasma concentration (Cavg) was 3.1 ± 1.9 ng/mL.10
- Volume of distribution
There is no information available on the volume of distribution.
- Protein binding
Clascoterone is 84% to 89% bound to plasma proteins in vitro, regardless of drug concentrations.10
- Metabolism
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).10 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,1,5,8 namely carboxylesterase.6
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- Route of elimination
Excretion of clascoterone has not been fully characterized in humans.10 Upon topical application, clascoterone is quickly hydrolyzed in the epidermis.1
- Half-life
There is limited information on the half life of clascoterone.10
- Clearance
There is limited information on clearance of clascoterone.10
- Adverse Effects
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- Toxicity
There is no information available on the toxicity profile of clascoterone, such as LD50 and overdose in humans.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareFlotufolastat F-18 Clascoterone may decrease effectiveness of Flotufolastat F-18 as a diagnostic agent. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- International/Other Brands
- Breezula / Winlevi
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Winlevi Cream 1 % w/w Topical Sun Pharmaceutical Industries Limited 2023-09-08 Not applicable Canada Winlevi Cream 1 g/100g Topical Sun Pharmaceutical Industries, Inc. 2021-10-04 Not applicable US
Categories
- ATC Codes
- D10AX06 — Clascoterone
- Drug Categories
- 17-Hydroxycorticosteroids
- Acids, Acyclic
- Adrenal Cortex Hormones
- Androgen Receptor Antagonists
- Androgen Receptor Inhibitors
- Anti-Acne Preparations
- Anti-Acne Preparations for Topical Use
- Antiandrogens
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (weak)
- Cytochrome P-450 CYP2B6 Inhibitors
- Cytochrome P-450 CYP2B6 Inhibitors (weak)
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 Inhibitors (weak)
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (weak)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (weak)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (weak)
- Cytochrome P-450 CYP2E1 Inhibitors
- Cytochrome P-450 CYP2E1 Inhibitors (weak)
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (weak)
- Cytochrome P-450 Enzyme Inhibitors
- Dermatologicals
- Fatty Acids
- Fatty Acids, Volatile
- Fused-Ring Compounds
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hydroxycorticosteroids
- Lipids
- Pregnanes
- Pregnenediones
- Pregnenes
- Steroids
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 21-hydroxysteroids. These are steroids carrying a hydroxyl group at the 21-position of the steroid backbone.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Hydroxysteroids
- Direct Parent
- 21-hydroxysteroids
- Alternative Parents
- Gluco/mineralocorticoids, progestogins and derivatives / Steroid esters / 20-oxosteroids / 3-oxo delta-4-steroids / Delta-4-steroids / Cyclohexenones / Alpha-acyloxy ketones / Alpha-hydroxy ketones / Carboxylic acid esters / Monocarboxylic acids and derivatives show 3 more
- Substituents
- 20-oxosteroid / 21-hydroxysteroid / 3-oxo-delta-4-steroid / 3-oxosteroid / Alcohol / Aliphatic homopolycyclic compound / Alpha-acyloxy ketone / Alpha-hydroxy ketone / Carbonyl group / Carboxylic acid derivative show 15 more
- Molecular Framework
- Aliphatic homopolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- XN7MM8XG2M
- CAS number
- 19608-29-8
- InChI Key
- GPNHMOZDMYNCPO-PDUMRIMRSA-N
- InChI
- 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
- IUPAC Name
- (1R,3aS,3bR,9aR,9bS,11aS)-1-(2-hydroxyacetyl)-9a,11a-dimethyl-7-oxo-1H,2H,3H,3aH,3bH,4H,5H,7H,8H,9H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-1-yl propanoate
- SMILES
- [H][C@@]12CC[C@](OC(=O)CC)(C(=O)CO)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C
References
- General References
- 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]
- 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. [Article]
- 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. [Article]
- 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]
- 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]
- 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]
- 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]
- 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]
- Drugs.com: FDA Approves Winlevi [Link]
- FDA Approved Drug Products: WINLEVI (clascoterone) cream, for topical use [Link]
- Health Canada Approved Drug Products: WINLEVI (clascoterone) cream for topical use (June 2023) [Link]
- External Links
- Human Metabolome Database
- HMDB0304870
- PubChem Compound
- 11750009
- PubChem Substance
- 347828732
- ChemSpider
- 9924713
- 2474340
- ChEMBL
- CHEMBL3590187
- ZINC
- ZINC000006716459
- Wikipedia
- Clascoterone
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 3 Completed Treatment Acne Vulgaris 3 3 Recruiting Treatment Androgenetic Alopecia (AGA) 2 2 Completed Treatment Acne Vulgaris 3 2 Completed Treatment Androgenetic Alopecia (AGA) 1 1 Completed Other Healthy Subjects (HS) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Cream Topical 1 % w/w Cream Topical 1 g/100g - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US10159682 No 2018-12-25 2028-08-14 US US8143240 No 2012-03-27 2023-01-12 US US9486458 No 2016-11-08 2028-07-24 US US8865690 No 2014-10-21 2022-07-24 US US9433628 No 2016-09-06 2029-02-08 US US9211295 No 2015-12-15 2022-07-24 US US8785427 No 2014-07-22 2030-07-25 US US11207332 No 2021-12-28 2028-11-20 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.00753 mg/mL ALOGPS logP 4.1 ALOGPS logP 3.73 Chemaxon logS -4.7 ALOGPS pKa (Strongest Acidic) 13.78 Chemaxon pKa (Strongest Basic) -3.3 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 80.67 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 109.59 m3·mol-1 Chemaxon Polarizability 44.86 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-0udi-0019700000-2280fa15d327ca816ba8 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-1019000000-c9c67631db8ba3e8814a Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-0frb-0389200000-b9135bd7e78970dbe04f Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0abc-9010000000-8be5b8d407d068aef97b Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-05fr-9022000000-bafd40be5dafde0ed75f Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-01bc-1941100000-61560a6546758a18c96d Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 209.3252577 predictedDarkChem Lite v0.1.0 [M-H]- 188.31245 predictedDeepCCS 1.0 (2019) [M+H]+ 209.9312577 predictedDarkChem Lite v0.1.0 [M+H]+ 190.70802 predictedDeepCCS 1.0 (2019) [M+Na]+ 208.6771577 predictedDarkChem Lite v0.1.0 [M+Na]+ 196.62056 predictedDeepCCS 1.0 (2019)
Targets
![](https://go.drugbank.com/assets/locked/DrugTargets2-682eb846d210ae4bf33ca03febccfb57bb1c61318e699b729e5df4dfab2c5b67.png)
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- General Function
- Zinc ion binding
- Specific Function
- Steroid hormone receptors are ligand-activated transcription factors that regulate eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Transcription ...
- Gene Name
- AR
- Uniprot ID
- P10275
- Uniprot Name
- Androgen receptor
- Molecular Weight
- 98987.9 Da
References
- Celasco G, Moro L, Bozzella R, Ferraboschi P, Bartorelli L, Quattrocchi C, Nicoletti F: Biological profile of cortexolone 17alpha-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist. Arzneimittelforschung. 2004;54(12):881-6. doi: 10.1055/s-0031-1297043. [Article]
- 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. [Article]
- 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. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Clascoterone inhibited this enzyme in vitro with an IC50 value of >40 µM.
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- FDA Approved Drug Products: WINLEVI (clascoterone) cream, for topical use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Clascoterone inhibited this enzyme in vitro with an IC50 value of >40 µM.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- FDA Approved Drug Products: WINLEVI (clascoterone) cream, for topical use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Clascoterone inhibited this enzyme in vitro with an IC50 value of >40 µM.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- FDA Approved Drug Products: WINLEVI (clascoterone) cream, for topical use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Clascoterone inhibited this enzyme in vitro with an IC50 value of >40 µM.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- FDA Approved Drug Products: WINLEVI (clascoterone) cream, for topical use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Clascoterone inhibited this enzyme in vitro with an IC50 value of >40 µM.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- FDA Approved Drug Products: WINLEVI (clascoterone) cream, for topical use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Clascoterone inhibited this enzyme in vitro with an IC50 value of >40 µM.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- FDA Approved Drug Products: WINLEVI (clascoterone) cream, for topical use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Clascoterone inhibited this enzyme in vitro with an IC50 value of >40 µM.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- Molecular Weight
- 56848.42 Da
References
- FDA Approved Drug Products: WINLEVI (clascoterone) cream, for topical use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- Curator comments
- Clascoterone inhibited this enzyme in vitro with an IC50 value of >40 µM.
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- FDA Approved Drug Products: WINLEVI (clascoterone) cream, for topical use [Link]
Drug created at October 20, 2016 22:38 / Updated at June 27, 2023 01:10