Clotrimazole是咪唑衍生物,有抗真菌活性,是P450抑制剂。
Clotrimazole alters the permeability of the fungal cell wall by inhibiting the biosynthesis of ergosterol, used in the treatment of fungal infections [1].
Clotrimazole as a potent agent for treating the oomycete fish pathogen Saprolegnia parasitica through inhibition of sterol 14α-demethylase (CYP51) [2]. The demethylated products of the CYP51 reaction are vital intermediates in pathways leading to the formation of cholesterol in humans, ergosterol in fungi, and other types of sterols in plants (Lepesheva et al.).
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Aktas H, et al. Proc Natl Acad Sci U S A,?998, 95(14), 8280-8285.
[2] Appl Environ Microbiol. 2014 Oct;80(19):6154-66. doi: 10.1128/AEM.01195-14.
[3] Jensen, B.S., et al. 2001. Curr Drug Targets. 2: 401-422.
[4] Carrillo-Muñoz, A.J., et al. 2002. Int. J. Antimicrob. Agents. 20: 375-379.
分子式 C22H17ClN2 |
分子量 344.84 |
CAS号 23593-75-1 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 10 mg/mL |
Water <1 mg/mL |
Ethanol 66 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00835029 | Oral Candidiasis|Denture Stomatitis | Drug: Clotrimazole varnish|Drug: Clotrimazole troches | Hadassah Medical Organization | Phase 2 | 2009-03-01 | 2015-03-24 |
NCT01547221 | Otomycosis | Drug: clotrimazole|Drug: 3% Boric acid | Khon Kaen Hospital | 2012-03-01 | 2015-04-27 | |
NCT02180828 | Candidiasis, Vulvovaginal | Drug: Clotrimazole vaginal tablet|Drug: Fluconazole | Peking University Shenzhen Hospital|Bayer | Phase 4 | 2014-07-01 | 2016-08-08 |
NCT01697826 | Vaginal Infections | Drug: ClinSupV3 -soft gelatin capsule|Drug: ClinSupV3ER- Extended release tablet | Dr Bharti Daswani|Resilient Cosmeceuticals Pvt. Ltd, Pune|Daswani, Bhart, M.D. | Phase 4 | 2011-04-01 | 2012-10-01 |
NCT02847286 | HIV- Prevention | Drug: Dapivirine Ring-004|Drug: Dapivirine Ring-004 for 28 days along with clotrimazole|Drug: Clotrimazole | International Partnership for Microbicides, Inc. | Phase 1 | 2015-09-01 | 2016-12-16 |
NCT00755053 | Clotrimazole|Ovulen|Vulvovaginal Candidiasis | Drug: Clotrimazole, vaginal ovule|Drug: Clotrimazole, vaginal tablet | Bayer | Phase 3 | 2008-09-01 | 2015-08-04 |
NCT02184351 | Candidiasis, Oral | Drug: Roxanes's clotrimazole troches|Drug: Mycelex庐 troches | Boehringer Ingelheim | Phase 3 | 2001-05-01 | 2014-07-11 |
NCT02907307 | Vulvovaginal Candidiasis | Device: LactiSal vaginal gel 1%|Device: LactiSal vaginal tablet 50mg|Drug: Clotrimazole vaginal tablet 100mg | Medinova AG | Phase 3 | 2017-05-01 | 2016-09-14 |
NCT00002282 | Candidiasis, Oral|HIV Infections | Drug: Clotrimazole|Drug: Fluconazole | Pfizer|NIH AIDS Clinical Trials Information Service | null | 2005-06-23 | |
NCT02713139 | Sexual Active Women|Vaginal Discharge | Drug: Clotrimazole + Metronidazole|Drug: Metronidazole|Drug: Clotrimazole | Ache Laboratorios Farmaceuticos S.A. | Phase 3 | 2013-09-01 | 2016-03-15 |
NCT01244256 | Folliculitis | Drug: Clotrimazole + Gentamicin + Beclomethasone|Drug: Clotrimazole + Gentamicin | Azidus Brasil | Phase 2|Phase 3 | 2007-04-01 | 2010-11-18 |
NCT02635438 | Oropharyngeal Candidiasis | Drug: Unique Pharmaceutical Laboratories, India|Drug: Roxane Laboratories Inc., USA | Thinq Pharma-CRO Pte. Ltd.|Unique Pharmaceuticals Ltd, India|THINQ Pharma CRO Ltd. | Phase 3 | 2016-12-01 | 2016-12-22 |
NCT00000676 | Candidiasis|Mycoses|HIV Infections | Drug: Clotrimazole|Drug: Fluconazole | National Institute of Allergy and Infectious Diseases (NIAID)|Pfizer | Phase 3 | null | 2012-03-28 |
NCT01993823 | Otomycosis | Drug: G238|Drug: Clotrimazole | Salvat | Phase 3 | 2013-05-01 | 2016-12-21 |
NCT00390780 | HIV Infections | Drug: miconazole Lauriad|Drug: Clotrimazole | Onxeo | Phase 3 | 2006-07-01 | 2013-09-05 |
NCT02242695 | Vulvovaginal Candidiasis | Drug: Fluomizin vaginal tablets|Drug: Canesten vaginal tablets | Medinova AG|Mahidol University | Phase 4 | 2014-11-01 | 2016-09-14 |
NCT02248506 | Candidiasis, Vulvovaginal | Other: Clotrimazole | Instituto Palacios|GYNEA Laboratorios S. L. | Phase 4 | 2013-06-01 | 2015-03-24 |
NCT02582177 | Tinea | Drug: Ketoconazole + betamethasone dipropionate|Drug: Clotrimazole + Dexamethasone acetate | Ache Laboratorios Farmaceuticos S.A. | Phase 3 | 2017-08-01 | 2017-02-14 |
NCT00004492 | Sickle Cell Anemia | Drug: clotrimazole|Drug: hydroxyurea | University of North Carolina|FDA Office of Orphan Products Development | Phase 1|Phase 2 | 1999-10-01 | 2015-03-24 |
NCT00671528 | Dermatitis, Atopic|Eczema, Atopic|Skin Diseases, Eczematous | Drug: Cream (betamethasone diproprionate, clotrimazole, and gentamicin sulfate)|Drug: Cream (betamethasone diproprionate and gentamicin)|Drug: Cream (betamethasone diproprionate) | Merck Sharp & Dohme Corp. | Phase 4 | 2009-07-01 | 2014-12-29 |
NCT00629122 | Kidney Failure, Chronic | Drug: Tacrolimus/Clotrimazole Troche|Drug: Tacrolimus/Nystatin Suspension | Weill Medical College of Cornell University | Phase 4 | 2008-02-01 | 2010-11-04 |
NCT03026478 | Oral Lichen Planus | Drug: Betamethasone Dipropionate|Drug: Clobetasol Propionate | Garlapati Komali|Panineeya Mahavidyalaya Institute of Dental Sciences & Research Centre | Phase 2 | 2016-05-01 | 2017-01-21 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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