Ibrutinib

Cytostatic · Kinase Inhibitor

Indications

For the treatment of adult patients with: Mantle cell lymphoma (MCL) who have received at least one prior therapy. Chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL). Chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) with 17p deletion. Waldenström’s macroglobulinemia (WM). Marginal zone lymphoma (MZL) who require systemic therapy and have received at least one prior anti-CD20-based therapy. Chronic graft versus host disease (cGVHD) after failure of one or more lines of systemic therapy.

Dosage

Adults: Dose should be taken orally with a glass of water. MCL and MZL: 560 mg taken once daily. CLL/SLL, WM, and cGVHD: 420 mg taken once daily. Children: Not recommended.

Adverse Effects

The most common adverse reactions (=30%) in patients with B-cell malignancies (MCL, CLL/SLL, WM and MZL) are thrombocytopenia, diarrhea, fatigue, musculoskeletal pain, neutropenia, rash, anemia, and bruising. The most common adverse reactions (=20%) in patients with cGVHD are fatigue, bruising, diarrhea, thrombocytopenia, muscle spasms, stomatitis, nausea, hemorrhage, anemia, and pneumonia.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Precautions: Monitor for bleeding and manage. Monitor patients for fever and infections, evaluate promptly, and treat. Check complete blood counts monthly. Monitor for symptoms of arrhythmias, hypertension and manage. Other malignancies have occurred in patients, including skin cancers, and other carcinomas. Tumor Lysis Syndrome (TLS): Assess baseline risk and take precautions. Monitor and treat for TLS. Advise females of reproductive potential to use effective contraception.

Interactions

CYP3A Inhibitors, strong CYP3A Inducers.

Advice to Patient

Inform patients of the possibility of bleeding, and to report any signs or symptoms (severe headache, blood in stools or urine, prolonged or uncontrolled bleeding). Inform patients of the possibility of serious infection, and to report any signs or symptoms (fever, chills, weakness, confusion) suggestive of infection. Counsel patients to report any signs of palpitations, lightheadedness, dizziness, fainting, shortness of breath, and chest discomfort, hypertension. Inform patients that other malignancies, potential risk of tumor lysis syndrome have occurred in patients who have been treated with Ibrutinib, including skin cancers and other carcinomas. Inform the patient that Ibrutinib may need to be interrupted for medical or dental procedures.

Pharmacokinetics

Bioavailability: Absolute bioavailability in fasted condition was 2.9% and doubled when combined with a meal. Metabolism: Hepatic. Half-life elimination: 4 to 6 hours. Time to peak: 1 to 2 hours (4 hours under fed conditions [de Jong 2015]. Excretion: Faces (80%; 1% as unchanged drug); urine (<10%, as metabolites).

Compiled by Healify Pharmacy from published drug references. How we compile it →

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