Zanubrutinib

BRUKINSA

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Pronunciation: zan-yoo-BROO-ti-nib (BROO-kin-sa)

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

What it isSecond-generation BTK inhibitor; CLL, mantle cell lymphoma and Waldenstrom disease.

Why this oneMore selective than ibrutinib with less atrial fibrillation, and superior progression-free survival head to head.

What limits itNeutropenia and bleeding. CYP3A4-dependent.

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

FDA-approved for

mantle cell lymphoma (2019)
CLL, Waldenstrom macroglobulinemia

FDA label

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FDA dosing	Population	Start	Target	Max
B-cell malignancies (MCL, WM, MZL, CLL/SLL, FL) — monotherapy or with obinutuzumab	adult	160 mg BID or 320 mg QD	160 mg BID or 320 mg QD	160 mg BID or 320 mg QD

Renal No adjustment needed (CLcr ≥15 mL/min); monitor if on dialysis

Hepatic Severe (Child-Pugh C): 80 mg BID; mild-moderate: no adjustment

Instructions

Take with or without food
Swallow capsules whole with water; do not open, break, or chew
Swallow tablets whole; do not chew or crush (tablets may be split in half as prescribed)
Missed dose: take same day, resume normal schedule next day

Available strengths

cap 80 mg
tab 160 mg

Cautions

Hemorrhage (including fatal/intracranial/GI)
Infections (including opportunistic; HBV reactivation)
Cytopenias (neutropenia, thrombocytopenia, anemia) — monitor CBC
Second primary malignancies (skin and non-skin) — use sun protection
Cardiac arrhythmias (atrial fibrillation/flutter)
Hepatotoxicity, including drug-induced liver injury
Embryo-fetal toxicity

Adverse reactions

Decreased neutrophil count
Decreased platelet count
Upper respiratory tract infection
Hemorrhage
Musculoskeletal pain

Pregnancy Can cause fetal harm; avoid pregnancy during and 1 week after last dose

Lactation Do not breastfeed during and for 2 weeks after last dose

Cost

Zanubrutinib (BRUKINSA)

Strength		#/mo	generic $/mo	CostPlus
160 mg	tab	60 BID		not offered
80 mg	cap	60 BID		not offered

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

Generic entry2043 est.

NO BOXED WARNINGS

Principal riskNeutropenia and bleeding

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryNot assigned — PLLR-era drug

Defining liabilityMyelosuppression and agent-specific hepatic, cardiac, pulmonary, neurologic or reproductive toxicity require oncology monitoring.

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