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口服伊布利康唑:一种治疗外阴阴道念珠菌病的研究药物。

Oral Ibrexafungerp: an investigational agent for the treatment of vulvovaginal candidiasis.

机构信息

Clinical Development, SCYNEXIS Inc , Jersey City, NJ, USA.

Clinical Development, El Camino Medical Group , Mountain View, CA, USA.

出版信息

Expert Opin Investig Drugs. 2020 Sep;29(9):893-900. doi: 10.1080/13543784.2020.1791820. Epub 2020 Aug 19.

Abstract

INTRODUCTION

Vulvovaginal candidiasis (VVC) is a common fungal infection caused by predominantly , and is diagnosed in up to 40% of women with vaginal complaints in the primary care setting. Approximately 75% of women experience at least one episode during their reproductive years.

AREAS COVERED

Ibrexafungerp is an orally active, semi-synthetic triterpenoid glucan synthase inhibitor under development for treatment and prevention of VVC. We present the chemistry, mechanism of action, pharmacology, microbiology, and results from clinical studies with ibrexafungerp in women with VVC.

EXPERT OPINION

Ibrexafungerp addresses several unmet needs with existing antifungal drugs as a first in a new class of antifungal agents with a novel mechanism of action demonstrating no antifungal cross resistance with azoles, and fungicidal activity against spp., including fluconazole-resistant species. Some of the key attributes of ibrexafungerp related to VVC include oral one-day dosing, high tissue penetration, enhanced activity at low pH seen in the vagina, low risk for clinically significant drug-drug interactions, and a low risk of adverse events. If approved, ibrexafungerp will be the first new antifungal agent available for the treatment of VVC in more than 20 years and the only oral, non-azole antifungal approved for women suffering from VVC.

摘要

简介

外阴阴道假丝酵母菌病(VVC)是一种常见的真菌感染,主要由 引起,在初级保健环境中,多达 40%的阴道不适妇女被诊断患有 VVC。大约 75%的女性在生育期至少会经历一次发作。

涵盖领域

Ibrexafungerp 是一种新型半合成三萜类葡萄糖合酶抑制剂,目前正在开发中,用于治疗和预防 VVC。我们介绍了 Ibrexafungerp 的化学、作用机制、药理学、微生物学以及在患有 VVC 的女性中的临床研究结果。

专家意见

Ibrexafungerp 解决了现有抗真菌药物的一些未满足需求,作为一种新型作用机制的新型抗真菌药物的首创药物,与唑类药物没有抗真菌交叉耐药性,对 属具有杀菌活性,包括氟康唑耐药株。Ibrexafungerp 与 VVC 相关的一些关键属性包括口服一天一次给药、高组织穿透性、在阴道中低 pH 值下增强的活性、低发生临床显著药物相互作用的风险以及低发生不良事件的风险。如果获得批准,Ibrexafungerp 将成为 20 多年来第一种可用于治疗 VVC 的新型抗真菌药物,也是唯一一种用于治疗 VVC 的口服、非唑类抗真菌药物。

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