Isavuconazole

CRESEMBA

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Isavuconazole ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Isavuconazole ballicule

What it isTriazole antifungal, the active form of isavuconazonium; aspergillosis and mucormycosis.

Why it mattersCovers Mucorales like posaconazole with predictable absorption and no QT prolongation.

What it changesSHORTENS QT, so it is contraindicated in familial short QT syndrome. A moderate CYP3A4 inhibitor.

Isavuconazole molecular structure (skeletal formula) — Molecular structure: Isavuconazole

FDA-approved for

aspergillosis/mucormycosis (2015)

Principal riskContraindicated in familial short QT syndrome

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger1 / 4

Weight-gain liability0 / 4

Sedation liability1 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Defining liabilityHepatotoxicity and CYP3A interactions

FDA label

Read the full label on DailyMed ↗

NO BOXED WARNINGS

FDA dosing	Population	Start	Target	Max
Invasive aspergillosis	Adults	Loading 372 mg (=200 mg isavuconazole) q8h ×6 doses (48 h)	Maintenance 372 mg QD
Invasive mucormycosis	Adults	Loading 372 mg q8h ×6 doses (48 h)	Maintenance 372 mg QD
Invasive aspergillosis/mucormycosis	Peds ≥1 yr	IV loading 15 mg/kg (<3 yr) or 10 mg/kg (≥3 yr) q8h ×6 doses	Maintenance same dose QD	372 mg per dose

Renal No adjustment needed (mild/moderate/severe incl. ESRD)

Hepatic No adjustment for mild-moderate (Child-Pugh A/B); not studied in severe (C) — use only if benefits outweigh risks, with monitoring

Start maintenance dose 12-24 h after the last loading dose

Instructions

Capsules: swallow whole; do not chew, crush, dissolve, or open; take with or without food
IV: infuse over ≥1 hour through an in-line filter (0.2-1.2 micron); do not give as a bolus; do not co-infuse other drugs
Switching between IV and oral is acceptable (bioequivalent); no loading dose needed when switching

Available strengths

cap 74.5, 186 mg
inj 40 mg/mL

Contraindications

Coadministration with strong CYP3A4 inhibitors (e.g., ketoconazole, high-dose ritonavir)
Coadministration with strong CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's wort, long-acting barbiturates)
Familial short QT syndrome

Cautions

Hepatic adverse reactions — evaluate liver tests at baseline and during therapy
Infusion-related reactions (IV) — discontinue infusion if they occur
Hypersensitivity — anaphylaxis (fatal reported) and severe skin reactions (e.g., SJS)
Embryo-fetal toxicity — advise effective contraception
Drug particulates — administer IV through an in-line filter

Adverse reactions

Nausea, vomiting, diarrhea
Headache
Elevated liver chemistry tests
Hypokalemia
Constipation
Dyspnea, cough
Peripheral edema
Back pain

Pregnancy May cause fetal harm based on animal studies (perinatal mortality, skeletal abnormalities); advise of risk and use contraception.

Lactation No human data; discontinue breastfeeding during treatment with CRESEMBA.

Cost

Isavuconazole (CRESEMBA)

Strength		#/mo	CostPlus
74.5 mg	cap	30 qd	not offered
186 mg	cap	30 qd	not offered
40 mg/mL	inj	per unit	not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Isavuconazole is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

Other forms: Isavuconazonium (CRESEMBA)

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Self-check

How does isavuconazole affect QT?
Shortens it.
Which inherited QT condition contraindicates isavuconazole?
Familial short-QT syndrome.