Rezafungin

Summary

Rezafungin (CD101) is a next-generation echinocandin antifungal agent with an extended half-life allowing once-weekly intravenous administration. It is approved for the treatment of candidemia and invasive candidiasis in adults with limited or no alternative treatment options. Its structural modification confers stability in aqueous solution and potent activity against Candida species, including some azole- and echinocandin-resistant strains.

Mechanism of Action

Non-competitive inhibitor of beta-1,3-glucan synthase, an enzyme essential for fungal cell wall synthesis. Disruption of glucan synthesis leads to osmotic instability and fungal cell death. Rezafungin has a long half-life due to its modified side chain, enabling once-weekly dosing.

Routes of Administration

Goals & Uses

• Activity against echinocandin-resistant CandidaResistant Organism CoverageLow
• Treatment of invasive candidiasisAntifungalHigh
• Treatment of candidemiaAntifungal TherapyHigh
• Antifungal prophylaxis in hematopoietic stem cell transplant recipientsProphylaxisModerate

Contraindications

• PregnancyPopulationHighPotential fetal risk or insufficient safety data
• Known hypersensitivity to rezafungin or other echinocandinsAllergyHigh

Adverse Effects

• HypokalemiaElectrolyteCommon
• AnemiaHematologicCommonLow red blood cell count or hemoglobin
• Elevated liver enzymes (ALT/AST)HepaticUncommon
• NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
• VomitingGastrointestinalCommonForceful expulsion of stomach contents
• Infusion-related reactionsHypersensitivityUncommon

Drug Interactions

• CyclosporineLow
• TacrolimusLow

Population Constraints

• Pediatric patientsAgeRelative
• Breastfeeding womenReproductiveRelative
• Pregnant womenReproductiveRelative
• Severe hepatic impairmentOrgan ImpairmentRelative

Regulatory Status

• European UnionApprovedApproved: Candidemia and invasive candidiasis in adultsEMA approved April 2023; marketed by Cidara/partner
• United StatesApprovedApproved: Candidemia and invasive candidiasis in adults with limited or no alternative treatment optionsFDA approved March 22, 2023; brand name Rezzayo; marketed by Melinta Therapeutics
• United KingdomUnknownPost-Brexit regulatory status not confirmed at time of knowledge cutoff

FDA approved in March 2023 under the brand name Rezzayo for candidemia and invasive candidiasis. EMA approved in April 2023. Developed by Cidara Therapeutics and licensed to Melinta Therapeutics in the US.

Evidence & Sources

No sources recorded yet.