Regis University School of Pharmacy, Denver, CO, USA.
Palm Beach Atlantic University Gregory School of Pharmacy, West Palm Beach, FL, USA.
Am J Health Syst Pharm. 2022 Dec 5;79(24):2208-2221. doi: 10.1093/ajhp/zxac256.
The pharmacology, microbiology, pharmacokinetics, pharmacodynamics, efficacy, safety, and role of ibrexafungerp in the treatment of fungal infections are reviewed.
Ibrexafungerp is the first triterpenoid antifungal. Similarly to echinocandins, it inhibits the synthesis of 1,3-β-d-glucan. However, it binds to a different site on the enzyme than echinocandins, resulting in limited cross-resistance. Ibrexafungerp exerts concentration-dependent fungicidal activity against Candida species and retains in vitro activity against most fluconazole-resistant strains. It is also active against Aspergillus species. Ibrexafungerp has been shown to be safe and effective in the treatment of vulvovaginal candidiasis caused by Candida albicans in phase 2 and phase 3 clinical trials. It is approved for vulvovaginal candidiasis in adult and postmenarchal pediatric females and is given as two 150-mg tablets orally, administered 12 hours apart. Ibrexafungerp is contraindicated in pregnancy. The most commonly reported adverse reactions were diarrhea, nausea, abdominal pain, dizziness, and vomiting. Ibrexafungerp should be avoided with strong or moderate CYP3A inducers, and the dose should be reduced with strong CYP3A inhibitors. Ibrexafungerp may be useful for patients who are not able to receive fluconazole or prefer oral therapy for the treatment of vulvovaginal candidiasis. However, it is more expensive than the 150-mg tablet of generic fluconazole, which is the current standard of care for vulvovaginal candidiasis. Clinical trials are ongoing for recurrent and complicated vulvovaginal candidiasis as well as invasive candidiasis and pulmonary aspergillosis.
Ibrexafungerp is an alternative to fluconazole for the treatment of vulvovaginal candidiasis in nonpregnant females. It has the potential to be useful for recurrent and complicated vulvovaginal candidiasis as well as certain invasive fungal infections.
综述伊布康唑的药理学、微生物学、药代动力学、药效学、疗效、安全性及其在真菌感染治疗中的作用。
伊布康唑是第一种三萜类抗真菌药物。与棘白菌素类药物类似，它抑制 1,3-β-d-葡聚糖的合成。然而，它与棘白菌素类药物结合在不同的酶位上，导致有限的交叉耐药性。伊布康唑对念珠菌属具有浓度依赖性杀菌活性，并保留对大多数氟康唑耐药株的体外活性。它对曲霉菌属也具有活性。在 2 期和 3 期临床试验中，伊布康唑已被证明可安全有效地治疗由白色念珠菌引起的外阴阴道念珠菌病。它被批准用于成年和初潮后女性的外阴阴道念珠菌病，口服给药，每次 150mg 片剂 2 片，间隔 12 小时。伊布康唑禁用于妊娠。最常见的不良反应是腹泻、恶心、腹痛、头晕和呕吐。伊布康唑应避免与强或中度 CYP3A 诱导剂同时使用，与强 CYP3A 抑制剂同时使用时应减少剂量。对于不能使用氟康唑或更喜欢口服治疗外阴阴道念珠菌病的患者，伊布康唑可能有用。然而，它比氟康唑 150mg 片剂更昂贵，氟康唑是目前治疗外阴阴道念珠菌病的标准药物。目前正在进行用于复发性和复杂性外阴阴道念珠菌病以及侵袭性念珠菌病和肺曲霉病的临床试验。
伊布康唑是氟康唑治疗非妊娠女性外阴阴道念珠菌病的替代药物。它有可能对复发性和复杂性外阴阴道念珠菌病以及某些侵袭性真菌感染有用。
