Ibrutinib

IMBRUVICA

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Pronunciation: eye-BROO-ti-nib (im-BROO-vi-ka)

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

Ibrutinib IMBRUVICA mascot mnemonic cartoon — Visual mnemonic: Ibrutinib mascot
**“Ibis (says) I’m a brutal nibbler”**

What it isBruton tyrosine kinase inhibitor; CLL, mantle cell lymphoma and Waldenstrom disease.

Why this oneAs the first-generation covalent BTK inhibitor, it has the deepest experience but more atrial fibrillation than newer agents.

What limits itBleeding and atrial fibrillation complicate anticoagulation. CYP3A4 interactions and treatment-emergent hypertension require review.

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

Ibrutinib prescription history

Animated chart of estimated U.S. prescriptions per year, Tyrosine kinase inhibitors (2001–2026). Ibrutinib enters in 2013 (estimated).

FDA-approved for

B-cell malignancies (2013)

Principal riskAtrial fibrillation and bleeding

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability1 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk3 / 4

Legacy pregnancy categoryD

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

FDA label

Read the full label on DailyMed ↗

NO BOXED WARNINGS

FDA dosing	Population	Start	Target	Max
CLL/SLL	Adults	420 mg QD	420 mg QD
Waldenström's macroglobulinemia	Adults	420 mg QD	420 mg QD
Chronic GVHD	≥12 yr	420 mg QD	420 mg QD
Chronic GVHD	1 to <12 yr	240 mg/m² QD	240 mg/m² QD (up to 420 mg)	420 mg

Renal Undefined

Hepatic B-cell malignancies: 140 mg QD if mild (Child-Pugh A), 70 mg QD if moderate (B), avoid if severe (C). cGVHD: reduce dose if total bilirubin >1.5–3× ULN; avoid if >3× ULN

Instructions

Take at about the same time each day with a glass of water
Swallow capsules/tablets whole; do not open, break, cut, crush, or chew
Missed dose: take same day, resume normal schedule next day; do not double up

Available strengths

cap 70, 140 mg
tab 140, 280, 420 mg
susp 70 mg/mL

Cautions

Hemorrhage (fatal bleeding reported; higher risk with anticoagulant/antiplatelet)
Infections (incl. PML, PJP; fatal and non-fatal)
Cardiac arrhythmias, cardiac failure, sudden death
Hypertension
Cytopenias (monitor CBC monthly)
Second primary malignancies (esp. skin cancers)
Hepatotoxicity, including drug-induced liver injury
Tumor lysis syndrome
Embryo-fetal toxicity

Adverse reactions

Thrombocytopenia
Diarrhea
Fatigue
Musculoskeletal pain
Neutropenia
Rash
Anemia
Bruising
Nausea
(cGVHD also) pyrexia, muscle spasms, stomatitis, hemorrhage, pneumonia, headache

Pregnancy Can cause fetal harm (animal embryofetal toxicity/malformations); advise effective contraception

Lactation No data; do not breastfeed during treatment and for 1 week after last dose

Cost

Ibrutinib (IMBRUVICA)

Strength		#/mo	CostPlus
140 mg	tab	30 qd	not offered
280 mg	tab	30 qd	not offered
420 mg	tab	30 qd	not offered
70 mg	cap	30 qd	not offered
140 mg	cap	30 qd	not offered
70 mg/mL	susp	per unit	not offered

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

Generic entry2031+ est.

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Memory aids: interaction avatars

CYP3A4 substrate

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Self-check

How does ibrutinib’s atrial-fibrillation burden compare with newer BTK inhibitors?
Higher.
Which enzyme pathway drives important ibrutinib interactions?
CYP3A4.