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Pronunciation |
/aɪˌbrɛksəˈfʌndʒɜːrp/ eye-BREKS-ə-FUN-jurp |
Trade names | Brexafemme |
Other names | SCY-078 |
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Routes of administration | oral, intravenous |
Drug class | Antifungal |
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Pharmacokinetic data | |
Protein binding | >99% [1] |
Metabolism | Hydroxylation ( CYP3A4) then conjugation ( glucuronidation, sulfation) [1] |
Elimination half-life | 20 hours [1] |
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Chemical and physical data | |
Formula | C44H67N5O4 |
Molar mass | 730.051 g·mol−1 |
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Ibrexafungerp, sold under the brand name Brexafemme, is an antifungal medication used to treat vulvovaginal candidiasis (VVC) (vaginal yeast infection). [1] It is taken orally (by mouth). [1] It is also currently undergoing clinical trials for other indications via an intravenous (IV) formulation. An estimated 75% of women will have at least one episode of VVC and 40 to 45% will have two or more episodes in their lifetime. [3]
Ibrexafungerp acts via inhibition of glucan synthase, which prevents formation of the fungal cell wall. [1]
Ibrexafungerp was approved for medical use in the United States in June 2021. [1] [4] It is the first non- azole oral antifungal drug to be approved by the U.S. Food and Drug Administration (FDA) for the treatment of vaginal yeast infections. [4] The FDA considers it to be a first-in-class medication. [5]
Ibrexafungerp is indicated for the treatment of adult and postmenarchal pediatric females with vulvovaginal candidiasis (VVC). [1] [4]
Ibrexafungerp is currently undergoing late-stage clinical trials for an intravenous formulation for the treatment of various fungal diseases, including life-threatening fungal infections caused primarily by Candida (including C. auris) and Aspergillus species. It has demonstrated broad-spectrum antifungal activity, in vitro and in vivo, against multidrug-resistant pathogens, including azole- and echinocandin-resistant strains. [6]
Ibrexafungerp is a triterpenoid antifungal agent. [1] It acts via inhibition of the enzyme glucan synthase, which is involved in the formation of 1,3-β-D-glucan—an essential component of the fungal cell wall. [1] The compound has concentration-dependent fungicidal activity against Candida species. [1]
Ibrexafungerp has a time to maximal concentrations of 4 to 6 hours. [1] It is metabolized by hydroxylation via CYP3A4 and subsequently by glucuronidation and sulfation. [1] The medication has an elimination half-life of approximately 20 hours. [1]