Rezafungin (Rezzayo)

Rezafungin (Rezzayo) photo 

Rezafungin photo source: rezzayo.com

KEY POINTS

• Expected to be available Summer 2023, pricing to be released but expected to be expensive
• Rezafungin (Rezzayo) is an echinocandin antifungal that works by inhibiting 1,3–D-glucan synthase enzyme complex, which is present in fungal cell walls
  • Has fungicidal in vitro activity against Candida species
  • Resistance may develop due to FKS genes
  • Clinical activity has been confirmed against C. albicans, C. glabrata, C. parapsilosis, and C. tropicalis
  • Efficacy is not established for a variety of other Candida species, including C. krusei, C. auris, C. guilliermondii, and C. lusitaniae
• FDA approved March 22nd, 2023 for patients 18 years of age or older who have limited or no alternative options for the treatment of candidemia and invasive candidiasis
  • Package insert says it has not been studied for infective endocarditis, osteomyelitis, or meningitis due to Candida
• Dose as a once weekly by intravenous (IV) infusion, with an initial 400 mg loading dose, followed by a 200 mg dose once weekly thereafter
  • Has not been established for use beyond 4 weeks
  • Supplied as a 200 mg single-dose vial for reconstitution
    • Vial contains 210 mg of rezafungin acetate, equivalent to 200 mg of rezafungin
    • Vials should be stored at 20°C to 25°C (68°F to 77°F)
    • Must be diluted prior to administration
      • Avoid shaking during reconstitution to minimize foaming
      • Stable for 24 hours at 5°C to 25°C (41°F to 77°F) once reconstituted
    • 400 mg and 200 mg doses go in a total volume of 250 mL, mixed in NS, 1/2NS, or D5W
• Holds a warning for infusion-related reactions (e.g., flushing, urticaria, nausea)
  • Should be administered over 1 hour, but can be given slower if infusion reaction occurs
• Holds a warning for photosensitivity, patient counseling on sun exposure is recommended
• Holds a warning for hepatic reactions
• Adverse reactions can also include hypokalemia, pyrexia (fever), diarrhea, anemia, nausea, vomiting, hypomagnesemia, abdominal pain, constipation, and hypophosphatemia
• No major drug-drug interaction concerns
• Studies in NCT 03667690 versus caspofungin for candidemia and/or invasive candidiasis, showing similar all-cause mortality, global cure, clinical cure, and mycological eradication
• Studied in NCT 02734862 for safety

RESOURCES

Rezafungin Package Insert

Cidara Therapeutics and Melinta Therapeutics Announce FDA Approval of REZZAYO™ (rezafungin for injection) for the Treatment of Candidemia and Invasive Candidiasis

Early use of the novel antifungal rezafungin: a case series and literature review (JAC 2025)

Rezafungin versus caspofungin for treatment of candidaemia and invasive candidiasis (ReSTORE): a multicentre, double-blind, double-dummy, randomised phase 3 trial

Rezafungin Versus Caspofungin in a Phase 2, Randomized, Double-blind Study for the Treatment of Candidemia and Invasive Candidiasis: The STRIVE Trial

A phase I randomized, double-blind, single subcutaneous dose escalation study to determine the safety, tolerability, and pharmacokinetics of rezafungin in healthy adult subjects

Population Pharmacokinetics of Rezafungin in Patients with Fungal Infections

Evaluation of Rezafungin Provisional CLSI Clinical Breakpoints and Epidemiological Cutoff Values Tested against a Worldwide Collection of Contemporaneous Invasive Fungal Isolates (2019 to 2020)

Rezafungin and invasive candida infections: a new game changing antifungal?

Rezafungin: a novel antifungal for the treatment of invasive candidiasis