"目录号: HY-14273
Anti-infectionMetabolic Enzyme/Protease-
Isavuconazole 是一种水溶的苯三唑，具有抗真菌作用，同时也是CYP3A4的温和抑制剂。
FungalCytochrome P450
相关产品
Cycloheximide-Talarozole-Abiraterone acetate-Amphotericin B-Hygromycin B-Micafungin sodium-Cobicistat-Fenofibrate-FICZ-Nystatin-Anidulafungin-Caspofungin Acetate-Itraconazole-Ketoconazole-Posaconazole-
生物活性
Description
Isavuconazole is a moderate inhibitor ofCYP3A4and a water-soluble triazole with broad-spectrumantifungalactivity.
In Vitro
Isavuconazole shows good activity against allCandidaspp., with active MIC50of 0.004 mg/L. The MIC50s/MIC90s range from 0.002/0.004 mg/L forC. albicansto 0.25/0.5 mg/L forC. glabrata[1]. Isavuconazole has potent in vitro activity against most commonAspergillusspecies,Purpureocillium lilacinum, andScedosporium apiospermum[2]. Isavuconazole shows potent activity against molds, yeasts, and dimorphic fungi. Rhizopus isolates have MIC values to isavuconazole as low as 0.12 μg/mL with others as high as 32 μg/mL[3]. In the study of pharmacokinetics and pharmacodynamics of isavuconazole against the GFP transformant, F/11628, NIH 4215, and F/16216, the modal MICs of isavuconazole are 1, 8, 1, 4 mg/L, respectively[4].
Clinical Trial
NCT01657890
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Healthy Volunteers-Safety and Tolerability in Elderly
June 2012
Phase 1
NCT01657838
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Ketoconazole-Healthy Adult Volunteers
May 2012
Phase 1
NCT03149055
Memorial Sloan Kettering Cancer Center-Astellas Pharma US, Inc.
Hematologic Malignancy-Myeloproliferative Disorder
May 4, 2017
Phase 2
NCT01809860
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Healthy Subjects-Pharmacokinetics of Isavuconazole-Pharmacokinetics of Sirolimus
November 2011
Phase 1
NCT01660477
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Lopinavir/Ritonavir-Healthy Volunteers
June 2012
Phase 1
NCT01582412
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Digoxin-Healthy Volunteers
March 2012
Phase 1
NCT01711827
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Healthy Subjects-Pharmacokinetics of Isavuconazole-Pharmacokinetics of Prednisolone
February 2012
Phase 1
NCT01635946
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Atorvastatin-Healthy Volunteers
August 2012
Phase 1
NCT01582425
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Methadone-Healthy Volunteers
April 2012
Phase 1
NCT01635972
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Bupropion-Healthy Volunteers
June 2012
Phase 1
NCT01884636
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Methotrexate-Pharmacokinetics of 7-hydroxymethotrexate-Healthy Subjects
February 2013
Phase 1
NCT03019939
M.D. Anderson Cancer Center
Acute Myeloid Leukemia-Myelodysplastic Syndrome
March 28, 2017
Phase 2
NCT00634049
Astellas Pharma Inc-Basilea Pharmaceutica International Ltd
Aspergillosis-Invasive Fungal Infections
April 2008
Phase 3
NCT01884558
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Metformin-Healthy Subjects
February 2013
Phase 1
NCT01406171
Astellas Pharma Inc-Basilea Pharmaceutica
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Midazolam-Healthy Volunteers
May 2011
Phase 1
NCT01535547
Astellas Pharma Inc-Basilea Pharmaceutica International Ltd
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Tacrolimus-Healthy Volunteers
December 2011
Phase 1
NCT01657825
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of S- and R-warfarin-Pharmacodynamics of Warfarin-Healthy Volunteers
June 2012
Phase 1
NCT01597986
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Ethinyl Estradiol and Norethindrone-Healthy Volunteers
April 2012
Phase 1
NCT02128893
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Healthy Subjects
January 2014
Phase 1
NCT01494597
Astellas Pharma Inc-Basilea Pharmaceutica International Ltd
Healthy
November 2011
Phase 1
NCT01565720
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Healthy Volunteers
March 2012
Phase 1
NCT01555866
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Healthy Volunteers-Renal Impaired
March 2012
Phase 1
NCT01651325
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Dextromethorphan-Healthy Adult Volunteers
May 2012
Phase 1
NCT01555918
Astellas Pharma Inc-Basilea Pharmaceutica International Ltd
Pharmacokinetics of BAL4815-Pharmacokinetics of BAL8728-Healthy Volunteers
August 2012
Phase 1
NCT01711489
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Healthy Subjects-Pharmacokinetics of Isavuconazole-Pharmacokinetics of Plasma Mycophenolic Acid (MPA)-Pharmacokinetics of Plasma Phenolic Glucuronide of MPA (MPAG)
March 2012
Phase 1
NCT00412893
Astellas Pharma Inc-Basilea Pharmaceutica International Ltd
Invasive Fungal Infection-Aspergillosis
March 2007
Phase 3
NCT02128321
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Repaglinide-Pharmacokinetics of Caffeine-Healthy Subjects
January 2014
Phase 1
NCT00413218
Astellas Pharma Inc-Basilea Pharmaceutica
Mycoses-Candidiasis, Invasive-Candidemia
December 2006
Phase 3
NCT00413439
Basilea Pharmaceutica
Acute Myeloid Leukemia
May 2006
Phase 2-Phase 3
View MoreCollapse
References
[1].Seifert H, et al. In vitro activities of isavuconazole and other antifungal agents against Candida bloodstream isolates. Antimicrob Agents Chemother. 2007 May;51(5):1818-21.
[2].Steinmann J, et al. In Vitro Activity of Isavuconazole against Rasamsonia Species. Antimicrob Agents Chemother. 2016 Oct 21;60(11):6890-6891.
[3].Donnelley MA, et al. Isavuconazole in the treatment of invasive aspergillosis and mucormycosis infections. Infect Drug Resist. 2016 Jun 2;9:79-86.
[4].Box H, et al. Pharmacodynamics of Isavuconazole in a Dynamic In Vitro Model of Invasive Pulmonary Aspergillosis. Antimicrob Agents Chemother. 2015 Oct 26;60(1):278-87.