Acalabrutinib

CALQUENCE

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Pronunciation: a-kal-a-BROO-ti-nib (KAL-kwens)

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

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

Why this oneMore selective than ibrutinib, so less atrial fibrillation, bleeding and hypertension.

What limits itHeadache early is common. Acid-reducing drugs lower absorption of the original capsule.

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

FDA-approved for

mantle cell lymphoma (2017)
chronic lymphocytic leukemia

FDA label

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FDA dosing	Population	Start	Target	Max
MCL, CLL, or SLL (monotherapy or combination regimens)	adult	100 mg BID (q12h)	100 mg BID (q12h)	100 mg BID (q12h)

Renal Undefined

Hepatic Avoid in severe hepatic impairment; not evaluated in moderate or severe impairment.

If a dose is missed by more than 3 hours, skip it and take the next dose at the scheduled time; do not take extra capsules.

Instructions

Swallow capsules whole with water; do not open, break, or chew.
Take with or without food, approximately every 12 hours.
Hold for 3–7 days before and after surgery depending on bleeding risk.

Available strengths

cap 100 mg
tab 100 mg

Cautions

Serious and opportunistic infections (including fatal; HBV reactivation, PJP, PML)
Hemorrhage (fatal and serious; increased with antithrombotics)
Cytopenias (Grade 3/4 neutropenia, lymphopenia, anemia, thrombocytopenia)
Second primary malignancies (skin and other solid tumors) — advise sun protection
Cardiac arrhythmias (atrial fibrillation/flutter, ventricular arrhythmias)
Hepatotoxicity, including drug-induced liver injury

Adverse reactions

Most common (≥30%): upper respiratory tract infection, diarrhea, headache, musculoskeletal pain
Common Grade 3/4 labs (≥10%): neutrophil count decreased, uric acid increased, lymphocyte count decreased, platelets decreased

Pregnancy May cause fetal harm and dystocia (animal data); advise effective contraception during treatment and for 1 week after the last dose.

Lactation Advise not to breastfeed during treatment and for at least 2 weeks after the final dose.

Cost

Acalabrutinib (CALQUENCE)

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

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

Generic entry2036 est.

NO BOXED WARNINGS

Principal riskHeadache early; 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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