Ibrexafungerp: A First-in-Class Oral Triterpenoid Glucan Synthase Inhibitor

oleh: Sabelle Jallow, Nelesh P. Govender

Format: Article
Diterbitkan: MDPI AG 2021-02-01

Deskripsi

Ibrexafungerp (formerly SCY-078 or MK-3118) is a first-in-class triterpenoid antifungal or “fungerp” that inhibits biosynthesis of β-(1,3)-D-glucan in the fungal cell wall, a mechanism of action similar to that of echinocandins. Distinguishing characteristics of ibrexafungerp include oral bioavailability, a favourable safety profile, few drug–drug interactions, good tissue penetration, increased activity at low pH and activity against multi-drug resistant isolates including <i>C. auris</i> and <i>C. glabrata.</i> In vitro data has demonstrated broad and potent activity against <i>Candida</i> and <i>Aspergillus</i> species. Importantly, ibrexafungerp also has potent activity against azole-resistant isolates, including biofilm-forming <i>Candida</i> spp., and echinocandin-resistant isolates. It also has activity against the asci form of <i>Pneumocystis</i> spp., and other pathogenic fungi including some non-<i>Candida</i> yeasts and non-<i>Aspergillus</i> moulds. In vivo data have shown IBX to be effective for treatment of candidiasis and aspergillosis. Ibrexafungerp is effective for the treatment of acute vulvovaginal candidiasis in completed phase 3 clinical trials.