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依布康唑,一种正在研发的新型口服三萜类抗真菌药物:抗真菌活性概述

Ibrexafungerp, a Novel Oral Triterpenoid Antifungal in Development: Overview of Antifungal Activity Against .

作者信息

Gamal Ahmed, Chu Sherman, McCormick Thomas S, Borroto-Esoda Katyna, Angulo David, Ghannoum Mahmoud A

机构信息

Department of Dermatology, Case Western Reserve University, Cleveland, OH, United States.

College of Osteopathic Medicine of the Pacific, Northwest (COMP), Lebanon, OR, United States.

出版信息

Front Cell Infect Microbiol. 2021 Mar 11;11:642358. doi: 10.3389/fcimb.2021.642358. eCollection 2021.

DOI:10.3389/fcimb.2021.642358
PMID:33791244
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8006402/
Abstract

Systemic infections caused by species are an important cause of morbidity and mortality among immunocompromised and non-immunocompromised patients. In particular, is an emerging species within the family that causes infections ranging from superficial to life-threatening systemic disease. Echinocandins and azoles are typically the first-line therapies used to treat infections caused by , however, there is an increasing prevalence of resistance to these antifungal agents in patients. Thus, a need exists for novel therapies that demonstrate high efficacy against . Ibrexafungerp is a first-in-class glucan synthase inhibitor with oral availability developed to address this increasing antifungal resistance. Ibrexafungerp demonstrates broad activity against wild-type, azole-resistant, and echinocandin-resistant species. Furthermore, ibrexafungerp has shown efficacy in low pH environments, which suggests its potential effectiveness in treating vulvovaginal candidiasis. Additional preclinical and clinical studies are needed to further examine the mechanism(s) of ibrexafungerp, including acting as a promising new agent for treating infections.

摘要

由该菌种引起的全身感染是免疫功能低下和非免疫功能低下患者发病和死亡的重要原因。特别是,该菌种是某菌科中一种新出现的菌种,可导致从浅表感染到危及生命的全身性疾病。棘白菌素和唑类药物通常是用于治疗由该菌种引起的感染的一线疗法,然而,患者中对这些抗真菌药物的耐药性患病率正在上升。因此,需要有对该菌种显示出高疗效的新型疗法。艾伯康唑是一种一流的葡聚糖合酶抑制剂,具有口服可用性,旨在应对这种日益增加的抗真菌耐药性。艾伯康唑对野生型、唑类耐药和棘白菌素耐药的该菌种表现出广泛的活性。此外,艾伯康唑在低pH环境中已显示出疗效,这表明其在治疗外阴阴道念珠菌病方面具有潜在有效性。需要进一步开展临床前和临床研究,以进一步研究艾伯康唑的作用机制,包括作为一种有前景的治疗该菌种感染的新药物。

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Efficacy of Ibrexafungerp (SCY-078) against Candida auris in an Guinea Pig Cutaneous Infection Model.伊柏呋喃(SCY-078)在豚鼠皮肤感染模型中抗耳念珠菌的疗效。
Antimicrob Agents Chemother. 2020 Sep 21;64(10). doi: 10.1128/AAC.00854-20.
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Penetration of Ibrexafungerp (Formerly SCY-078) at the Site of Infection in an Intra-abdominal Candidiasis Mouse Model.伊布列康唑(前称 SCY-078)在腹腔念珠菌病小鼠模型感染部位的渗透。
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