Английская Википедия:Ibrexafungerp

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Шаблон:Short description Шаблон:Use American English Шаблон:Use dmy dates Шаблон:Infobox drug

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.[2]

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][3] 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.[3] The FDA considers it to be a first-in-class medication.[4]

Medical uses

Ibrexafungerp is indicated for the treatment of adult and postmenarchal pediatric females with vulvovaginal candidiasis (VVC).[1][3]

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.[5]

Pharmacology

Pharmacodynamics

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]

Pharmacokinetics

Ibrexafungerp has a time to maximal concentrations of 4 to 6Шаблон:Nbsphours.[1] It is metabolized by hydroxylation via CYP3A4 and subsequently by glucuronidation and sulfation.[1] The medication has an elimination half-life of approximately 20Шаблон:Nbsphours.[1]

Synthesis

Файл:Ibrexafungerp synthesis.svg
Synthetic pathway of ibrexafungerp, adapted from Scheme 1 of McInturff et al. 2023.[6]

References

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Further reading

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External links

Шаблон:Antifungals Шаблон:Portal bar

Шаблон:Antiinfective-drug-stub

  1. 1,00 1,01 1,02 1,03 1,04 1,05 1,06 1,07 1,08 1,09 1,10 Ошибка цитирования Неверный тег <ref>; для сносок Brexafemme FDA label не указан текст
  2. Шаблон:Cite web
  3. 3,0 3,1 3,2 Шаблон:Cite press release
  4. Шаблон:Cite report Шаблон:PD-notice
  5. Шаблон:Cite web
  6. Шаблон:Cite journal