OVERVIEW

PRODUCT INFORMATION

REPRESENTATIVE TRADE NAMES

Ibrexafungerp – Brexafemme®

DRUG CLASS

Antifungal Agents

COMPLETE LABELING

Product labeling at DailyMed, National Library of Medicine, NIH

CHEMICAL FORMULA AND STRUCTURE

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DRUG	CAS REGISTRY NUMBER	MOLECULAR FORMULA	STRUCTURE
Ibrexafungerp	1207753-03-4	C44-H67-N5-O4

ANNOTATED BIBLIOGRAPHY

References updated: 25 January 2025

• Zimmerman HJ. Antifungal agents. In, Zimmerman HJ. Hepatotoxicity: the adverse effects of drugs and other chemicals on the liver. 2nd ed. Philadelphia: Lippincott, 1999, pp. 609-11.

  (Expert review of hepatotoxicity of antifungal agents published in 1999 before the availability of ibrexafungerp).
• Moseley RH. Antifungal agents. Antibacterial and antifungal agents. In, Kaplowitz N, DeLeve LD, eds. Drug-induced liver disease. 3rd ed. Amsterdam: Elsevier, 2013, pp. 470-3.

  (Review of hepatotoxicity of antifungal agents before the availability of ibrexafungerp or other inhibitors of β-1,3,-D glucan).
• Rogers PD, Krysan DJ. Antifungal agents. In, Brunton LL, Hilal-Dandan R, Knollman BC, eds. Goodman & Gilman's the pharmacological basis of therapeutics. 13th ed. New York: McGraw-Hill, 2018, pp. 1987-1104.

  (Textbook of pharmacology and therapeutics discusses the echinocandins (-fungins) which inhibit β-1,3-D glucan synthesis, but not ibrexafungerp).
• FDA. Multi-Discipline Review. 2021. https://www​.accessdata​.fda.gov/drugsatfda_docs​/nda/2021/214900Orig1s000MultidisciplineR.pdf

  (FDA website with product label and multidiscipline review of ibrexafungerp based upon data submitted by the sponsor in support of its approval for use in vulvovaginal candidiasis, mentions that 2 healthy subjects in phase 1 trials of a single dose of ibrexafungerp developed ALT elevations [peak 575 and 275 U/L] with mild symptoms, that resolved spontaneously, and that the rate of ALT elevations in phase 3 trials of therapy of acute vulvovaginal candidiasis was 0.7% [4/575] on ibrexafungerp vs 0.4% [1/275] on placebo, and none of the elevations was associated with symptoms or jaundice).
• Lee A. Ibrexafungerp: first approval. Drugs. 2021;81:1445-1450. [PubMed: 34313977]

  (Review of the mechanism of action, history of development, pharmacology, clinical efficacy, and safety of ibrexafungerp shortly after its approval for use in the US, mentions common adverse events of diarrhea [17%], nausea [12%], abdominal pain [11%], dizziness [3%], and vomiting [2%] and the lack of serious adverse events in registration trials; no mention of ALT elevations or hepatotoxicity).
• Ibrexafungerp (Brexafemme) for vulvovaginal candidiasis. Med Lett Drugs Ther. 2021;63:141-143. [PubMed: 34550113]

  (Concise review of the mechanism of action, clinical efficacy, safety, and costs of ibrexafungerp mentions the common adverse events of diarrhea, nausea and vomiting, abdominal pain, and dizziness, but does not mention ALT elevations or hepatotoxicity).
• Sobel R, Nyirjesy P, Ghannoum MA, Delchev DA, Azie NE, Angulo D, Harriott IA, et al. Efficacy and safety of oral ibrexafungerp for the treatment of acute vulvovaginal candidiasis: a global phase 3, randomised, placebo-controlled superiority study (VANISH 306). BJOG. 2022;129:412-420. [PMC free article: PMC9299454] [PubMed: 34676663]

  (Among 272 women with acute vulvovaginitis treated with a one day course of ibrexafungerp [300 mg twice] or placebo, clinical cure was more frequent with drug [63% vs 44%], as was mycological eradication and improvement in symptoms, and while adverse events were more frequent with ibrexafungerp [15% vs 4%], side effects were mostly mild-to-moderate nausea or diarrhea, and there were no serious adverse events; no mention of ALT elevations or hepatotoxicity).
• Schwebke JR, Sobel R, Gersten JK, Sussman SA, Lederman SN, Jacobs MA, Chappell BT, et al. Ibrexafungerp versus placebo for vulvovaginal candidiasis treatment: a phase 3, randomized, controlled superiority trial (VANISH 303). Clin Infect Dis. 2022;74:1979-1985. [PMC free article: PMC9187327] [PubMed: 34467969]

  (Among 371 women with vulvovaginal candidiasis treated with a one day course of ibrexafungerp [300 mg twice] or placebo, clinical cure rates were higher with drug [51% vs 29%], as were rates of mycological eradication and improvement in symptoms, while adverse event rates were higher with ibrexafungerp [40% vs 17%] being largely nausea and diarrhea; no mention of ALT elevations or hepatotoxicity).
• Nyirjesy P, Schwebke JR, Angulo DA, Harriott IA, Azie NE, Sobel JD. Phase 2 randomized Study of oral ibrexafungerp versus fluconazole in vulvovaginal candidiasis. Clin Infect Dis. 2022;74:2129-2135. [PMC free article: PMC9258939] [PubMed: 34555149]

  (Among 186 patients with vulvovaginal candidiasis treated with 6 different 1- or 2-day regimens of ibrexafungerp vs fluconazole, efficacy and safety results were reported for the 62 who received the recommended regimen of each agent, the clinical cure rate at 10 days was 52% vs 58% and adverse event rate 47% vs 25%; no mention of ALT elevations or hepatotoxicity).
• Goje O, Sobel R, Nyirjesy P, Goldstein SR, Spitzer M, Faught B, Larson S, et al. Oral ibrexafungerp for vulvovaginal candidiasis treatment: an analysis of VANISH 303 and VANISH 306. J Womens Health (Larchmt). 2023;32:178-186. [PMC free article: PMC9940793] [PubMed: 36255448]

  (Summary of combined results of two clinical trials of ibrexafungerp [Sobel 2022; Schwebke 2022] for acute vulvovaginal candidiasis, mentions that safety results were similar to those reported in the trials and that mild-to-moderate gastrointestinal complaints were the most common adverse events).