isavuconazonium sulfate (Rx)

Brand and Other Names:Cresemba, isavuconazole
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Dosing & Uses


Dosage Forms & Strengths


  • 186mg isavuconazonium sulfate (equivalent to 100mg isavuconazole)

injection, lyophilized powder for reconstitution

  • 372mg isavuconazonium sulfate (equivalent to 200mg isavuconazole)

Invasive Aspergillosis

Indicated for invasive aspergillosis

Has activity against most strains of the following microorganisms, both in vitro and in clinical infection: Aspergillus flavus, Aspergillus fumigatus, and Aspergillus niger

Initial: 372 mg PO/IV q8hr x6 doses (48 hr)

Maintenance: 372 mg PO/IV qDay

Invasive Mucormycosis

Indicated for invasive mucormycosis caused by Mucorales fungi such as Rhizopus oryzae and Mucormycetes species

Initial: 372 mg PO/IV q8hr x6 doses (48 hr)

Maintenance: 372 mg PO/IV qDay

Dosage Modifications

Renal impairment

  • Mild, moderate, or severe (including ESRD): No dose adjustment required

Hepatic impairment

  • Mild or moderate: No dose adjustment required
  • Severe: Not studied

<18 years: Safety and efficacy not established



Interaction Checker

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            Adverse Effects


            Nausea (27.6%)

            Vomiting (24.9%)

            Diarrhea (23.7%)

            Hypokalemia (19.1%)

            Elevated liver tests (17.1%)

            Dyspnea (17.1%)

            Abdominal pain (16.7%)

            Headache (16.7%)

            Peripheral edema (15.2%)

            Constipation (14%)

            Fatigue (10.5%)

            Insomnia (10.5%)

            Back pain (10.1%)

            Renal failure (10.1%)


            Chest pain (8.9%)

            Decreased appetite (8.6%)

            Delirium (8.6%)

            Rash (8.6%)

            Pruritus (8.2%)

            Hypotension (8.2%)

            Anxiety (8.2%)

            Acute respiratory failure (7.4%)

            Injection site reaction (6.2%)

            Dyspepsia (6.2%)

            Hypomagnesemia (5.4%)

            Cardiac disorders: Atrial fibrillation, atrial flutter, bradycardia, reduced QT interval on electrocardiogram, palpitations, supraventricular extrasystoles, supraventricular tachycardia, ventricular extrasystoles, cardiac arrest (<5%)

            Nervous system disorders: Convulsion, dysgeusia, encephalopathy, hypoesthesia, migraine, peripheral neuropathy, paraesthesia, somnolence, stupor, syncope, tremor (<5%)

            Psychiatric disorders: Confusion, hallucination, depression (<5%)

            Renal and urinary disorders: Hematuria, proteinuria (<5%)

            Respiratory, thoracic, and mediastinal disorders: Bronchospasm, tachypnea (<5%)





            Coadministration with strong CYP3A4 inhibitors or inducers

            Familial short QT syndrome; isavuconazole shortens the QTc interval in a concentration-related manner


            Hepatic adverse drug reactions (eg, elevated ALT, AST, alkaline phosphatase, total bilirubin) reported; the elevations in liver-related laboratory tests were generally reversible and did not require discontinuation of drug; cases of more severe hepatic adverse drug reactions, including hepatitis, cholestasis, or hepatic failure including death, have been reported in patients with serious underlying medical conditions (eg, hematologic malignancy) during treatment with azole antifungal agents

            Infusion-related reactions, including hypotension, dyspnea, chills, dizziness, paresthesia, and hypoesthesia, were reported; discontinue the infusion if these reaction occur

            Serious hypersensitivity and severe skin reactions (eg, anaphylaxis, Stevens-Johnson syndrome) have been reported during treatment with other azole antifungal agents

            May cause fetal harm when administered to a pregnant woman

            Drug interaction overview

            • Isavuconazole is a sensitive CYP3A4 substrate, moderate CYP3A4 inhibitor, mild P-gp inhibitor, and a mild organic cation transporter 2 (OCT2) inhibitor
            • CYP3A4 inhibitors or inducers may alter the plasma concentrations of isavuconazole
            • Caution with other drugs that cause short QT syndrome (eg, cenobamate, rufinamide)

            Pregnancy & Lactation


            Based on findings from animal studies, fetal harm may occur when administered to pregnant women

            No human data available on use in pregnant women to evaluate for a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes

            Animal studies

            • In animal reproduction studies, perinatal mortality was increased in the offspring of pregnant rats dosed orally with isavuconazonium sulfate at 90 mg/kg/day during pregnancy through the weaning period
            • In animal studies when isavuconazonium chloride was administered by oral gavage to pregnant rats and rabbits during organogenesis at exposures corresponding to less than the human maintenance dose, increases in the incidences of multiple skeletal abnormalities, including rudimentary cervical ribs and fused zygomatic arches, were observed


            • Advise female patients of reproductive potential to use effective contraception during treatment and for 28 days after the final dose


            Isavuconazole was present in the milk of lactating rats following IV administration

            Thus, drug may be present in human milk

            Therefore, breastfeeding should be discontinued during treatment

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.



            Mechanism of Action

            Triazole antifungal agent; isavuconazole is the active moiety of the prodrug isavuconazonium sulfate


            Absolute bioavailability: 98%

            Peak plasma concentration: 7,499 ng/mL (2 capsules); 20,028 (6 capsules)

            Peak plasma time: 3 hr (2 capsules); 4 hr (6 capsules)

            AUC: 121,402 hr ng/mL (2 capsules); 352,805 hr•ng/mL (6 capsules)


            Protein bound: >99%

            Vd: 450 L


            Isavuconazonium sulfate is rapidly hydrolyzed in blood to isavuconazole by esterases, predominately by butylcholinesterase to isavuconazole

            Isavuconazole is a substrate of cytochrome P450 enzymes 3A4 and 3A5

            Except for the active moiety isavuconazole, no individual metabolite observed with an AUC >10% of drug-related material

            In vivo studies indicate that CYP3A4, CYP3A5, and subsequently uridine diphosphate-glucuronosyltransferases (UGTs) are involved in the metabolism of isavuconazole


            Half-life: 130 hr

            Excretion: 46.1% feces; 45.5% urine



            IV Compatibilities

            0.9% NaCl injection

            D5W injection

            IV Preparation

            Reconstitute lyophilized powder in vial

            • Reconstitute 1 vial by adding 5 mL sterile water for injection
            • Gently shake to dissolve the powder completely
            • Visually inspect the reconstituted solution for particulate matter and discoloration; reconstituted solution should be clear and free of visible particulate

            Further dilution

            • Remove 5 mL of the reconstituted solution from the vial and add it to an infusion bag containing 250 mL (approximately 1.5 mg/mL isavuconazonium sulfate) of compatible diluent
            • The diluted solution may show visible translucent-to-white particulates of isavuconazole (which will be removed by in-line filtration)
            • Use gentle mixing or roll bag to minimize the formation of particulates
            • Avoid unnecessary vibration or vigorous shaking of the solution
            • Apply in-line filter with a microporous membrane pore size of 0.2 - 1.2 micron and in-line filter reminder sticker to the infusion bag

            IV Administration

            Do not use a pneumatic transport system

            Complete IV administration within 6 hr of dilution at room temperature (or immediately store refrigerated, see Storage)

            IV formulation must be administered via an infusion set with an in-line filter (pore size 0.2-1.2 micron)

            Infuse over a minimum of 1 hr in 250 mL of a compatible diluent, to reduce the risk for infusion-related reactions

            Do not administer as an intravenous bolus injection

            Do not infuse with other intravenous medications

            Flush IV lines with 0.9% NaCl injection or D5W prior to and after infusion

            Oral Administration

            Switching between IV and oral formulations is acceptable as bioequivalence has been demonstrated

            Loading dose is not required when switching between formulations

            Swallow oral capsules whole; do not chew, crush, dissolve, or open the capsules

            Can be taken with or without food


            Capsules: Store at 20-25ºC (68-77ºF), excursions between 15-30ºC (59-86ºF) in the original packaging to protect from moisture

            Reconstituted solution: May be stored below 25ºC for maximum 1 hr prior to preparation of the patient infusion solution

            Diluted IV solution

            • If unable to administer IV diluted solution within 6 hr of preparation, immediately refrigerate (2-8ºC [36-46ºF]) the infusion solution after dilution and complete the infusion within 24 hr
            • Do not freeze the infusion solution




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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.