Evidence Grade A — Regulatory approved. 204 published studies. 11 registered clinical trials.
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Rezafungin (sold as Rezzayo) is the first once-weekly antifungal in the echinocandin class — all previous echinocandins required daily intravenous infusions. It treats serious bloodstream and deep-organ Candida infections. Its extended half-life (about 5.5 days) was achieved by chemically stabilising the molecule to prevent the breakdown that limits older drugs in this class.
Rezafungin is also known by these brand and alternate names:
204 published studies: 122 human, 4 animal, 46 in-vitro, 84 reviews
Rezafungin is marketed as Rezzayo (approved March 2023) for candidaemia and invasive candidiasis in adults with limited or no alternative treatment options. It is administered as a once-weekly intravenous infusion.
In the ReSTORE trial, rezafungin was non-inferior to daily caspofungin, the existing standard. The once-weekly dosing is the primary advance — older echinocandins require daily infusions, which is burdensome for patients and hospital resources. A second trial studying rezafungin as prophylaxis in stem cell transplant patients did not meet its primary endpoint. The echinocandin class as a whole is considered first-line for invasive Candida infections, and rezafungin's weekly dosing may expand their use in outpatient settings.
Rezafungin blocks the production of beta-(1,3)-D-glucan, a sugar polymer that is essential for fungal cell walls but absent from human cells. Without this structural component, fungal cells lose their integrity and die from osmotic stress. The drug is fungicidal (kills) against Candida species and fungistatic (stops growth) against Aspergillus. The key innovation is a chemical modification that prevents the ring-opening degradation that limits the half-life of older echinocandins.
In the ReSTORE trial, once-weekly rezafungin was non-inferior to daily caspofungin (the existing standard) for treating invasive candidiasis. The weekly dosing is the primary advance — reducing infusion frequency from daily to weekly is meaningful for both patients and hospital resources, and could enable outpatient completion of antifungal courses. A second trial studying rezafungin as preventive therapy in stem cell transplant patients did not meet its primary endpoint, limiting the drug to treatment rather than prevention. Side effects include liver enzyme elevations, infusion reactions, and low potassium. Data for Aspergillus infections and paediatric patients are limited.
PeptideTrace tracks 11 registered clinical trials for Rezafungin sourced from ClinicalTrials.gov.
Rezafungin Peritoneal Diffusion for Intra-abdominal Candidiasis
Rezafungin Prophylaxis in Liver Transplant
Pharmacokinetic Study of Rezafungin in Patients With Suspected Intra-Abdominal Candidiasis
Rezafungin for Treatment of Chronic Pulmonary Aspergillosis (CPA) in Adults With Limited Treatment Options
A Study Comparing Short-course Antifungal Therapy (SCAT) 7 Day vs Standard 14 Day Antifungal Therapy for Uncomplicated Candidemia
FDA ORIG 1
EMA Marketing Authorisation
FDA SUPPL 8
Rezafungin is a next-generation echinocandin, semisynthetic cyclic lipopeptide from anidulafungin. MW ~1,285 Da. Choline ether at C5 ornithine stabilizes against ring-opening, extending half-life to ~133 hours (~5.5 days) enabling once-weekly IV dosing (first for echinocandins). Retains canonical hexapeptide core with N-acyl lipophilic side chain. IV 400 mg Day 1, then 200 mg once weekly.
Inhibits beta-(1,3)-D-glucan synthase (catalytic Fks1p/Fks2p, regulatory Rho1p GTPase), blocking synthesis of beta-(1,3)-D-glucan polymers essential for fungal cell wall. Causes osmotic instability and fungal cell death. Fungicidal against Candida, fungistatic against Aspergillus. No CYP450-dependent target, minimal drug-drug interactions.
Marketed as Rezzayo. Approved March 22, 2023. ReSTORE (Phase III; N=187): non-inferior to caspofungin for candidemia/invasive candidiasis, global cure Day 14: 59% vs. 61%. STRIVE (Phase III) for HSCT prophylaxis did not meet primary endpoint (22.2% vs. 16.4%). Indication: candidemia and invasive candidiasis in adults with limited alternatives.
Vancomycin is marketed as Vancocin and Firvanq (approved 1958, with oral solution Firvanq approved 2018). It is the standard treatment for serious MRSA infections (bloodstream infections, endocarditis, pneumonia, bone infections) and is first-line for severe C. difficile colitis. Vancomycin requires therapeutic drug monitoring — blood levels must be checked regularly to ensure the dose is effective without causing kidney damage or hearing loss. The rise of vancomycin-resistant enterococci (VRE) and occasional vancomycin-intermediate S. aureus (VISA) strains represent ongoing challenges. Despite being nearly 70 years old, vancomycin remains irreplaceable for many serious infections, though newer alternatives like daptomycin and the lipoglycopeptides offer advantages in specific settings.
Zilucoplan is marketed as Zilbrysq (approved October 2023) for anti-acetylcholine receptor antibody-positive generalised myasthenia gravis in adults. Administered as a daily subcutaneous self-injection. In the RAISE trial, zilucoplan showed statistically significant improvements in both activities of daily living and quantitative muscle strength scores compared to placebo, with improvements evident from week one. Its key differentiator from existing complement inhibitors (eculizumab, ravulizumab) is the self-injectable format — those alternatives require hospital-based intravenous infusions. As with all complement inhibitors, patients require meningococcal vaccination before starting treatment due to increased susceptibility to meningococcal infection.
Daptomycin is marketed as Cubicin (approved September 2003). It is indicated for complicated skin and soft tissue infections and S. aureus bloodstream infections including right-sided endocarditis. Administered as a once-daily intravenous infusion. A key limitation is that daptomycin cannot be used for pneumonia — lung surfactant inactivates the drug. In the bacteraemia trial, daptomycin was non-inferior to vancomycin with significantly lower rates of kidney problems (11% versus 26%). Creatine kinase (CK) levels must be monitored during treatment, as daptomycin can cause muscle toxicity. Generics became available after patent expiry, significantly reducing cost.
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