Rezzayo (rezafungin acetate)
Antifungals-Systemic Intravenous Vial (Ea)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Rezafungin acetate is a semisynthetic lipopeptide echinocandin antifungal agent.
Rezafungin is an echinocandin antifungal agent. Like other echinocandins, rezafungin inhibits the 1,3-beta-D-glucan synthase enzyme complex, which is present in fungal cell walls but not in mammalian cells. This results in inhibition of the formation of 1,3-beta-D-glucan, an essential component of the fungal cell wall of many fungi, including Candida species (spp.).
Inhibition of 1,3-beta-D-glucan synthesis results in concentration-dependent in vitro fungicidal activity against Candida spp.; however, the clinical significance of this activity is unknown. Rezafungin is a semisynthetic lipopeptide that is synthesized from a fermentation product of Aspergillus nidulans. Echinocandins (e.g., anidulafungin, caspofungin, micafungin, rezafungin) are glucan synthesis inhibitors and differ structurally and pharmacologically from other currently available antifungal agents.
Rezafungin, anidulafungin, caspofungin, and micafungin all have concentration-dependent fungicidal activity in vitro. Fungicidal killing is correlated to AUC relative to MIC.
Rezafungin is active in vitro and in clinical infections against most isolates of C. albicans, C. glabrata, C. parapsilosis, and C. tropicalis. Although the clinical importance is not known, rezafungin also has in vitro activity against C. krusei, C. auris, C. dubliniensis, C. fabianii, C. guilliermondii, C. inconspicua, C. kefyr, C. lusitaniae, C. metapsilosis, C. orthopsilosis, C. pulcherrima, C.rugosa, and C. sojae. However, the efficacy of rezafungin in treating clinical infections caused by these fungi has not been established in adequate and well-controlled clinical trials.
Reduced susceptibility to echinocandins has been associated with specific mutations in FKS subunits of the glucan synthase enzyme. These mutations are associated with higher MICs and poor response to therapy. Rezafungin exhibits some degree of cross-resistance to all FKS mutations that confer reduced susceptibility to echinocandins.
The clinical relevance of this finding has not been fully characterized.
Following single and multiple IV dosing, peak plasma concentrations of rezafungin increase in a dose-proportional manner over the dose range of 50 to 400 mg. There is no evidence that rezafungin is hepatically metabolized and it is unlikely that rezafungin is a clinically relevant substrate of cytochrome P-450 (CYP) enzymes. Rezafungin is mainly eliminated via the feces (approximately 74.3% of parent drug); the remainder (25.7%) is eliminated in the urine primarily as inactive metabolites.
Plasma protein binding ranges from 87.5 to 93.6%. The terminal half-life of rezafungin is approximately 152 hours. Rezafungin has a prolonged half-life (approximately 133 hours) compared to other echinocandins, which allows for extended-interval dosing and provides high plasma drug concentrations throughout the course of treatment.
USES: This medication is used to treat certain fungal infections (candidemia, invasive candidiasis). Rezafungin belongs to a class of drugs known as echinocandins. It works by stopping the growth of fungi.
Generic name: rezafungin acetate
Pronunciation: (RE-za-FUN-jin)
Drug class: Antifungals-Systemic
Therapeutic class: Anti-Infective Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Rezzayo
Indications
The following indications are listed for Rezzayo:
- Candidemia
- Disseminated Candidiasis
Also known as: Disseminated Candidosis, Disseminated Moniliasis.
Dosing
No dosing information is available for this tab.
Rezafungin is administered by IV infusion. The drug should not be given by rapid IV injection.
Rezafungin acetate is commercially available as a lyophilized powder in single-dose vials containing 200 mg of rezafungin; the drug must be reconstituted and diluted prior to IV infusion.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Rezzayo 200 Mg Vial | Maintenance | Infuse 200 mg by intravenous route once weekly. |
No dosing information is available for this tab.
Drug interactions
Rezafungin does not undergo hepatic metabolism. In vitro studies indicate that rezafungin is not a substrate for cytochrome P-450 (CYP) isoenzymes or drug transporter systems. Rezafungin also is not an inhibitor or inducer of common CYP isoenzymes or drug transporters.
Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
Selected Photosensitizers/Tretinoin-Mequinol
SEVERITY LEVEL: 1-Contraindicated Drug Combination: This drug combination is contraindicated and generally should not be dispensed or administered to the same patient.
MECHANISM OF ACTION: Tretinoin, anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides are all known photosensitizers.(1)
CLINICAL EFFECTS: Concurrent use of tretinoin in patients taking anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides may increase the risk of phototoxicity.(1)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: The US manufacturer states that tretinoin-mequinol should not be administered to patients receiving photosensitizers including anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides.(1)
DISCUSSION: Because of the risk of increased photosensitivity, the US manufacturer states that tretinoin-mequinol should not be administered to patients receiving photosensitizers including anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), methotrexate, phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides.(1)
Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
Selected Photosensitizers/Aminolevulinic Acid
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Aminolevulinic acid, anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides are all known photosensitizers.(1)
CLINICAL EFFECTS: Concurrent use of aminolevulinic acid in patients taking anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides may increase the risk of phototoxicity.(1)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: The US manufacturer states that aminolevulinic acid should be avoided in patients receiving photosensitizers including anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides for 24 hours before and after administration of aminolevulinic acid.(1)
DISCUSSION: Because of the risk of increased photosensitivity, the US manufacturer states that aminolevulinic acid should be avoided in patients receiving photosensitizers including anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides for 24 hours before and after administration of aminolevulinic acid.(1)
Selected Photosensitizers/Methoxsalen
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Methoxsalen causes photosensitivity due to residual drug which is present in all parts of the skin from photopheresis. Anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides are other known photosensitizers.(1)
CLINICAL EFFECTS: Concurrent use of methoxsalen in patients taking anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides may increase the risk of phototoxicity.(1)
PREDISPOSING FACTORS: None determined.
PATIENT MANAGEMENT: The US manufacturer of methoxsalen states that concurrent use of methoxsalen with anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides should be avoided.(1)
DISCUSSION: All patients who have received methoxsalen become photosensitive. It is unknown what the risk of photosensitivity reactions is when methoxsalen is used concurrently with other photosensitizing agents.(1)
Selected Photosensitizers/Porfimer
SEVERITY LEVEL: 2-Severe Interaction: Action is required to reduce the risk of severe adverse interaction.
MECHANISM OF ACTION: Porfimer causes photosensitivity due to residual drug which is present in all parts of the skin. Anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides are other known photosensitizers.(1)
CLINICAL EFFECTS: Concurrent use of porfimer in patients taking anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides may increase the risk of phototoxicity.(1)
PREDISPOSING FACTORS: Patients with any hepatic impairment and patients with severe renal impairment have reduced drug elimination and may remain photosensitive for 90 days or longer.(1)
PATIENT MANAGEMENT: The US manufacturer of porfimer states that concurrent use of porfimer with photosensitizers including anthralin, coal tar and derivatives, fluoroquinolones, griseofulvin, organic staining dyes (such as methylene blue, rose bengal, or toluidine blue), phenothiazines, selected NSAIDs (such as diclofenac, ketoprofen, nabumetone, naproxen, piroxicam, and tiaprofenic acid), methotrexate, St. John's wort, sulfonamides, sulfonylureas, tetracyclines, and thiazides should be avoided.(1) Since the photosensitive effect of porfimer may persist for at least 30 days (and for 90 days in some patients), it would be prudent to avoid other photosensitizing agents for at least 30 days after administration of porfimer.
DISCUSSION: All patients who have received porfimer become photosensitive. It is unknown what the risk of photosensitivity reactions is when porfimer is used concurrently with other photosensitizing agents. When porfimer was used in clinical trials, photosensitivity reactions occurred in about 20% of cancer patients and in 69% of high-grade dysplasia in Barretts esophagus patients. Most of the reactions were mild to moderate erythema, but they also included swelling, pruritus, burning sensation, feeling hot, or blisters. The majority of reactions occurred within 90 days of porfimer administration.(1)
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to rezafungin or other echinocandins.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
- No disease contraindications
Adverse reactions
The most common adverse reactions (incidence >= 5%) associated with rezafungin are hypokalemia, pyrexia, diarrhea, anemia, vomiting, nausea, hypomagnesemia, abdominal pain, constipation, and hypophosphatemia.
More Frequent
- Anemia
- Hypokalemia
- Hypomagnesemia
- Hypophosphatemia
Less Frequent
- Abnormal hepatic function tests
- Disseminated intravascular coagulation
- Hypervolemia
- Kidney disease with reduction in glomerular filtration rate (GFr)
Rare or Very Rare
- Anaphylaxis
- Hypersensitivity drug reaction
More Frequent
- Acute abdominal pain
- Constipation
- Diarrhea
- Fever
- Nausea
- Vomiting
Less Frequent
- Dizziness
- Dysphagia
- Erythema
- Headache disorder
- Insomnia
- Peripheral neuropathy
- Skin photosensitivity
- Tremor
Rare or Very Rare
- Chest tightness
- Urticaria
Precautions
No enhanced messaging available.
The safety and effectiveness of rezafungin have not been established in pediatric patients.
There are no adequate and well-controlled studies of rezafungin in pregnant women to assess the drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. In animal reproduction studies, administration of rezafungin in dosages approximately 3 or 5 times the recommended human dose based on AUC comparisons resulted in no adverse embryofetal outcomes and no adverse effects on offspring growth, maturation, or measures of neurobehavioral or reproductive function.
There are no data on the presence of rezafungin or its metabolite in human milk, the effects on the breastfed infant, or the effects on milk production. Rezafungin is present in rat milk; therefore, it is likely that the drug will be present in human milk. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for rezafungin and any potential adverse effects of the drug on the breastfed infant.
The manufacturer makes no specific dosage recommendations in geriatric patients.
In phase 1 and 2 trials of rezafungin, 42% of patients were 65 years of age and older and 17% of patients were 75 years of age and older. Clinical studies of rezafungin did not include sufficient numbers of older adult patients to determine if patients 65 years of age and older respond differently than younger adult patients.
No clinically relevant effects of age (ranging from 20 to 89 years) have been observed on the pharmacokinetics of rezafungin.
ICD codes
| Code | Type | Description |
|---|---|---|
| Candidemia | ||
| B37.7 | ICD10CM | Candidal sepsis |
| Disseminated candidiasis | ||
| B37.5 | ICD10CM | Candidal meningitis |
| B37.6 | ICD10CM | Candidal endocarditis |
| B37.7 | ICD10CM | Candidal sepsis |
| B37.89 | ICD10CM | Other sites of candidiasis |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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