Ibrexafungerp photo
KEY POINTS
- Ibrexafungerp (Brexafemme, SCY-078) is a triterpenoid antifungal that acts via 1, 3 B-glucan synthase inhibition
- It has a mechanism of action similar to echinocandins, but it has a unique binding site and unlike the echinocandins it has an oral formulation
- Has concentration-dependent fungicidal activity against Candida species
- Has activity against Candida FKS1 or FKS2 mutants (including echinocandin-resistant isolates of C. glabrata and C auris) and limited cross-resistance to echinocandins
- Being studied in the CARES study versus Candida auris
- Resistance has been associated with mutations in the fks-2 gene
- Retains activity against most fluconazole-resistant Candida species
- Has activity against Candida FKS1 or FKS2 mutants (including echinocandin-resistant isolates of C. glabrata and C auris) and limited cross-resistance to echinocandins
- Demonstrates in vitro activity against wild-type and azole-resistant strains of Aspergillus spp, Paecilomyces variotii, and some activity against L prolificans, but poor activity has been observed against Mucor and Fusarium spp
- On 2 June 2021, FDA-approved ibrexafungerp for the treatment of adult and post-menarchal pediatric females with vulvovaginal candidiasis (VVC)
- Current FDA approval is for oral formulation, but an injectable formulation is being studied
- Approved dose is 300 mg (as two 150 mg tablets) BID x 1 day (total course is 600 mg)
- Take with or without food
- Dose adjustments not listed in the package insert for age, renal function, or hepatic function
- Approved dose is 300 mg (as two 150 mg tablets) BID x 1 day (total course is 600 mg)
- Studied in the VANISH306 study and CANDLE study
- Current FDA approval is for oral formulation, but an injectable formulation is being studied
- Strong CYP-3A4 inhibitors increase ibrexafungerp exposure, while CYP-3A4 inducers may reduce exposure
- May require dose adjustment depending on drug-drug interactions
- The most common adverse reactions reported were diarrhea, nausea, abdominal pain, dizziness, and vomiting
- Has not been found to increase QTc to any clinically relevant extent
- Has a warning for fetal toxicity and for use in pregnancy (testing warranted prior to use, contraindicated in pregnancy)
RESOURCES
- Ibrexafungerp Package Insert
- SCYNEXIS Announces FDA Approval of BREXAFEMME® (ibrexafungerp tablets) as the First and Only Oral Non-Azole Treatment for Vaginal Yeast Infections
- Ibrexafungerp: A novel oral glucan synthase inhibitor – Med Mycol 2020
- Ibrexafungerp: A Novel Oral Triterpenoid Antifungal in Development for the Treatment of Candida auris Infections – Antibiotics 2020
- An evaluation of ibrexafungerp for the treatment of invasive candidiasis: the evidence to date – EOP 2021
- Hope on the Horizon: Novel Fungal Treatments in Development – OFID 2020
- Echinocandins for the Treatment of Invasive Aspergillosis: from Laboratory to Bedside – AAC 2019
- Ibrexafungerp: A new triterpenoid antifungal – AJHP 2022
