Autor: |
Yanan, Zhao, Min Hee, Lee, Padmaja, Paderu, Annie, Lee, Cristina, Jimenez-Ortigosa, Steven, Park, Robert S, Mansbach, Karen Joy, Shaw, David S, Perlin |
Rok vydání: |
2018 |
Předmět: |
|
Zdroj: |
Antimicrobial agents and chemotherapy. 62(10) |
ISSN: |
1098-6596 |
Popis: |
APX001 is a first-in-class, intravenous and orally available, broad-spectrum antifungal agent in clinical development for the treatment of life-threatening invasive fungal infections. The half-life of APX001A, the active moiety of APX001, is significantly shorter in mice than in humans (1.4 to 2.75 h in mice versus 2 to 2.5 days in humans), making the exploration of efficacy in mouse models difficult. After pretreatment with 1-aminobenzotriazole (ABT), a nonspecific cytochrome P450 inhibitor, greatly increased plasma APX001A exposure was observed in mice of different strains and of both genders. As a consequence, 26 mg/kg APX001 plus ABT sterilized kidneys in mice infected with |
Databáze: |
OpenAIRE |
Externí odkaz: |
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