Ibrexafungerp
Other antifungals
Other antifungalsPregnancy: contraindicated
Contraindicated: it caused fetal harm in animals. A pregnancy test is required before each cycle and effective contraception until 4 days after the last dose.
First triterpenoid antifungal, oral, that blocks glucan synthase like the echinocandins; for vulvovaginal candidiasis. Contraindicated in pregnancy.
Quick facts
- Group
- Other antifungals
- Target
- Fungal β-1,3-D-glucan synthase (Fks1)
- Used for
- Vulvovaginal candidiasis
- Key effects
- Diarrhoea · Dizziness and headache
- Monitor
- Pregnancy test before starting
- ATC
- J02AX07
No doses: the clinician sets them by the current guideline.
Mechanism of action
Ibrexafungerp, the first triterpenoid, inhibits synthesis of the wall's β-1,3-D-glucan, like the echinocandins, but with a different molecule that is absorbed by mouth. The wall is destabilised and the fungus dies. It is fungicidal, in a concentration-dependent way, against almost all Candida species, including azole-resistant strains.
- Absorbed by mouth
- Inhibits the fungal glucan synthase
- The wall lacks β-1,3-D-glucan
- The wall is destabilised and Candida dies
Indications
- Vulvovaginal candidiasis and prevention of its recurrences in adult women and adolescents after menarche Vulvovaginal candidiasis →
Adverse effects
Common
- Diarrhoea, nausea, vomiting and abdominal pain
- Dizziness and headache
- Urinary discomfort and tiredness
Contraindications
- Pregnancy
- Use with moderate or strong CYP3A4 inducers, such as rifampicin
Key interactions
- Moderate or strong CYP3A4 inducers (rifampicin, St John's wort)
- Lower its levels; not combined.
- Strong CYP3A4 inhibitors
- Raise its levels and require a change in the regimen.
- Grapefruit and grapefruit juice
- May interact; advice is sought before having it.
What is monitored
- Pregnancy test before starting and before each monthly prevention dose
- Response of the vulvovaginal symptoms
Administration and safety
- Oral, with or without food
- To prevent recurrences it is repeated once a month for several months, with a pregnancy test before each cycle
Pregnancy and breastfeeding
Contraindicated: it caused fetal harm in animals. A pregnancy test is required before each cycle and effective contraception until 4 days after the last dose.
Nursing care
- Confirm a negative pregnancy test before each cycle
- Explain effective contraception during treatment and for 4 days after
- Review medicines and herbal products for CYP3A4 inducers and inhibitors
- Teach to report symptoms that do not improve
Pharmacokinetics
- Absorption
- Oral, with or without food.
- Metabolism
- Hydroxylation by CYP3A4, then conjugation.
- Elimination
- Mainly in the faeces.
- Half-life
- About 20 hours.
Test yourself
Think of the answer, then tap the question to see it.
How is ibrexafungerp like the echinocandins, and how is it different?
It inhibits the same wall glucan synthase, but it is a different triterpenoid molecule that is absorbed by mouth.
Which test is required before each ibrexafungerp cycle?
A pregnancy test, because it is contraindicated in pregnancy after fetal harm in animals.
Why is ibrexafungerp not combined with rifampicin?
Rifampicin induces CYP3A4, the enzyme that metabolises it, and lowers its levels.
Connections
← Back to the class: Other antifungals
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Ibrexafungerp: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026).
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Representative model, for educational purposes only.