Drug reference

Ibrutinib

Tyrosine Kinase Inhibitor · Antineoplastic

Tyrosine Kinase InhibitorAntineoplastic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

FDA category + note

Top interactionssee all 12 →

PregnancySevereTextbookG&G 14e · p1395
AbciximabSevereDatabaseDDInter
AcalabrutinibSevereDatabaseDDInter
AdalimumabSevereDatabaseDDInter

Mechanism

Ibrutinib is a tyrosine kinase inhibitor.

Indications

Mantle cell lymphoma (specialist use only)Chronic lymphocytic leukaemia (specialist use only)Waldenstrӧm’s macroglobulinaemia (specialist use only)mantle cell lymphoma (MCL) who have received at least one prior therapymarginal zone lymphoma who have received at least one prior therapychronic lymphocytic leukemia (CLL)small lymphocytic lymphoma (SLL)Waldenström’s macroglobulinemiachronic graft-versus-host disease after failure of systemic therapySymptomatic Waldenström’s Macroglobulinemia (first-line)

Dosing

Adult: For Mantle cell lymphoma: 560 mg once daily. For Chronic lymphocytic leukaemia and Waldenstrӧm’s macroglobulinaemia: 420 mg once daily. For dose adjustments due to side-effects, consult product literature. If concurrent use of moderate inhibitors of CYP3A4, amiodarone or ciproﬂoxacin is unavoidable, reduce dose to 280 mg once daily.…

Pharmacokinetics

Half-life

4 to 6 h (elimination)

Bioavailability

doubles with food

Metabolism

CYP3A (substrate); CYP2D6 (minor)

Excretion

mainly via the feces; renal excretion is minor

Contraindications

Risk factors for QT-interval prolongation (including hypokalaemia or hypomagnesaemia)

Side effects

Common

arthralgiaastheniaconstipationcoughdiarrhoeadizzinessdyspnoeamalaisemyalgianauseapainperipheral oedemaneutropenia (>20%)pyrexia (>20%)thrombocytopenia (>20%)hemorrhage (>20%)anemia (>20%)diarrhea (>20%)nausea (>20%)musculoskeletal pain (>20%)rash (>20%)fatigue (>20%)arthralgias/myalgiasrashdiarrheadyspepsiabruising/bleedinghypertensionatrial fibrillationventricular arrhythmias

Serious

Acute kidney injury
anaphylactic reaction
differentiation syndrome
heart failure
hypotension
pericardial effusion
pericarditis
QT interval prolongation
Posterior reversible encephalopathy syndrome (PRES)
Pancreatitis
ventricular tachyarrhythmia
Hepatitis B reactivation
opportunistic infections
hypertension (onset within less than a month to 2 years)
atrial fibrillation (up to 7% of patients)
second primary malignancies (up to 16% of patients, mostly nonmelanoma skin cancers)