| 词条 | Clascoterone |
| 释义 |
| Verifiedfields = | Watchedfields = | verifiedrevid = | IUPAC_name = [(8R,9S,10R,13S,14S,17R)-17-(2-hydroxyacetyl)-10,13-dimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl] propanoate | image = Cortexolone 17α-propionate.svg | width = 250px | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = Topical (cream) | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number_Ref = | CAS_number = 19608-29-8 | CAS_supplemental = | ATC_prefix = | ATC_suffix = | ATC_supplemental = | PubChem = 11750009 | IUPHAR_ligand = | DrugBank_Ref = | DrugBank = | ChemSpiderID_Ref = | ChemSpiderID = 9924713 | UNII = XN7MM8XG2M | KEGG = D11451 | ChEBI = | ChEMBL = 3590187 | synonyms = CB-03-01; 11-Deoxycortisol 17α-propionate; 17α-(Propionyloxy)- deoxycorticosterone; 21-Hydroxy-3,20-dioxopregn-4-en-17-yl propionate | C=24 | H=34 | O=5 | molecular_weight = 402.531 g/mol | SMILES = CCC(=O)O[C@@]1(CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=CC(=O)CC[C@]34C)C)C(=O)CO | StdInChI_Ref = | StdInChI = 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 | StdInChIKey_Ref = | StdInChIKey = GPNHMOZDMYNCPO-PDUMRIMRSA-N |drug_name= |type=|MedlinePlus=|licence_EU=|licence_US=}}Clascoterone,[1][2] or cortexolone 17α-propionate, or 11-deoxycortisol 17α-propionate, (developmental code name CB-03-01; tentative brand names Breezula (for androgenic alopecia), Winlevi (for acne)) is a synthetic steroidal antiandrogen – specifically, an androgen receptor antagonist – that is under development by Cassiopea and Intrepid Therapeutics for use as a topical medication in the treatment of androgen-dependent conditions including acne vulgaris and androgenic alopecia (male-pattern hair loss).[3][4][5] It is the C17α propionate ester of 11-deoxycortisol (cortexolone);[4] C17α esters of 11-deoxycortisol were unexpectedly found to possess antiandrogen activity, and cortexolone 17α-propionate was selected for development based on its optimum drug profile.[4] In rats, the drug has been found to possess strong local antiandrogen activity, but negligible systemic antiandrogen activity when administered via subcutaneous injection.[4] In addition, cortexolone 17α-propionate is not progonadotropic, suggesting that it is peripherally selective.[4] In a bioassay, the topical potency of the drug was greater than that of progesterone, flutamide, and finasteride and was equivalent to that of cyproterone acetate.[4] A pilot clinical trial in 2011 of men treated with topical cortexolone 17α-propionate 1% cream for acne found that the drug was very well-tolerated and significantly reduced symptoms of acne.[5] Moreover, its effectiveness was significantly greater than that of the active comparator, tretinoin 0.05% cream.[5] As of 2019, the drug has finished phase III clinical trials for acne vulgaris with a NDA expected for the first half of 2019 and is expected to start phase III clinical trials for androgenic alopecia.[3] See also
References1. ^{{Cite web|url=http://www.cassiopea.com/news-and-media/press-releases/yr-2018/180710.aspx|title=Cassiopea Announces Very Positive Top-Line Phase 3 Results for Winlevi® (Clascoterone) cream in Treating Acne|website=www.cassiopea.com|language=en|access-date=2018-07-18}} 2. ^{{Cite web|url=http://www.cassiopea.com/news-and-media/press-releases/yr-2018/180716.aspx|title=Cassiopea Announces Very Positive Interim Analysis Phase 2 Results for Breezula® (Clascoterone) in Treating Androgenetic Alopecia|website=www.cassiopea.com|language=en|access-date=2018-07-18}} 3. ^1 http://adisinsight.springer.com/drugs/800026561 4. ^1 2 3 4 5 {{cite journal | vauthors = Celasco G, Moro L, Bozzella R, Ferraboschi P, Bartorelli L, Quattrocchi C, Nicoletti F | title = Biological profile of cortexolone 17alpha-propionate (CB-03-01), a new topical and peripherally selective androgen antagonist | journal = Arzneimittelforschung | volume = 54 | issue = 12 | pages = 881–6 | year = 2004 | pmid = 15646372 | doi = 10.1055/s-0031-1297043 | url = }} 5. ^1 2 {{cite journal | vauthors = Trifu V, Tiplica GS, Naumescu E, Zalupca L, Moro L, Celasco G | title = 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 | journal = Br. J. Dermatol. | volume = 165 | issue = 1 | pages = 177–83 | year = 2011 | pmid = 21428978 | doi = 10.1111/j.1365-2133.2011.10332.x | url = }} External links
5 : Diketones|Pregnanes|Propionate esters|Steroid esters|Steroidal antiandrogens |
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