REZZAYO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for REZZAYO (REZZAYO).
Rezafungin is an echinocandin antifungal that inhibits the synthesis of 1,3-β-D-glucan, an essential component of the fungal cell wall, leading to osmotic instability and cell death.
| Metabolism | Rezafungin is not significantly metabolized by hepatic enzymes; it undergoes slow degradation by ubiquitous peptidases and is excreted primarily unchanged in feces. |
| Excretion | Elimination primarily via feces (approximately 60% of dose) and urine (approximately 20% of dose) as unchanged drug and metabolites. |
| Half-life | Terminal elimination half-life approximately 13.3 hours in healthy subjects; at steady state, half-life ranges from 7.3 to 13.6 hours in patients with candidemia/invasive candidiasis. |
| Protein binding | Approximately 99% bound to serum albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution at steady state is approximately 48 L (0.6-0.9 L/kg for 70 kg adult), indicating extensive tissue distribution. |
| Bioavailability | Not applicable; administered only intravenously. |
| Onset of Action | Intravenous administration: therapeutic concentrations achieved within first dose; clinical response typically observed within 48-72 hours based on clinical trials. |
| Duration of Action | Dosing interval of 72 hours maintains therapeutic concentrations; duration of therapy is determined by clinical response, typically 14-28 days for invasive candidiasis. |
Intravenous: 2 mg/kg once daily, with a maximum of 200 mg per dose.
| Dosage form | POWDER |
| Renal impairment | No dose adjustment required for GFR ≥15 mL/min; not recommended for GFR <15 mL/min or dialysis. |
| Liver impairment | No dose adjustment for Child-Pugh A or B; not recommended for Child-Pugh C. |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No specific dose adjustment; use with caution due to age-related renal decline. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for REZZAYO (REZZAYO).
| Breastfeeding | No data on presence in human milk, effects on breastfed infant, or milk production. Consider developmental and health benefits of breastfeeding along with maternal need for REZZAYO and potential adverse effects on infant. |
| Teratogenic Risk | Insufficient human data in pregnant women. Animal studies show no evidence of teratogenicity at clinically relevant exposures. Risk cannot be ruled out; use only if potential benefit justifies potential risk to fetus. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to rezafungin or any echinocandin.
| Precautions | Hypersensitivity reactions (including anaphylaxis), hepatic transaminase elevations, infusion-related reactions, and risk of photosensitivity. Monitor liver function and for signs of hypersensitivity. |
Loading safety data…
| Monitor for hepatotoxicity (elevated liver enzymes, bilirubin) and hypersensitivity reactions. No specific fetal monitoring required beyond routine prenatal care. |
| Fertility Effects | No studies on fertility in humans. Animal studies show no impairment of fertility at doses up to 5 times the human exposure. |