"目錄號(hào): HY-14273

Anti-infectionMetabolic Enzyme/Protease-

Isavuconazole 是一種水溶的苯三唑呵曹，具有抗真菌作用撩嚼，同時(shí)也是CYP3A4的溫和抑制劑尾抑。

FungalCytochrome P450

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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

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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.