Ibrutinib

What it is and how it works

Mechanism of Action Ibrutinib is a small-molecule inhibitor of Bruton’s tyrosine kinase (BTK). Ibrutinib forms a covalent bond with a cysteine residue in the BTK active site, leading to inhibition of BTK enzymatic activity. BTK is a signaling molecule of the B-cell antigen receptor (BCR) and cytokine receptor pathways. BTK’s role in signaling through the B-cell surface receptors results in activation of pathways necessary for B-cell trafficking, chemotaxis, and adhesion. Nonclinical studies show that ibrutinib inhibits malignant B-cell proliferation and survival in vivo as well as cell migration and substrate adhesion in vitro .

Mechanism class: Protein Kinase Inhibitors

Indications

is a kinase inhibitor indicated for the treatment of: Adult patients with chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) . Adult patients with chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) with 17p deletion . Adult patients with Waldenström’s macroglobulinemia (WM) . Adult and pediatric patients age 1 year and older with chronic graft versus host disease (cGVHD) after failure of one or more lines of systemic therapy . Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma IMBRUVICA is indicated for the treatment of adult patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL). 1. 2 Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma with 17p deletion IMBRUVICA is indicated for the treatment of adult patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL) with 17p deletion. 1. 3 Waldenström’s Macroglobulinemia IMBRUVICA is indicated for the treatment of adult patients with Waldenström’s macroglobulinemia (WM). 1.

Dosage and administration (summary)

and WM : 420 mg taken orally once daily . cGVHD : ◦ Patients 12 years and older: 420 mg taken orally once daily . ◦ Patients 1 to less than 12 years of age: 240 mg/m 2 taken orally once daily (up to a dose of 420 mg) . Tablets or capsules should be taken orally with a glass of water. Do not open, break, or chew the capsules. Do not cut, crush, or chew the tablets. See full prescribing information for oral suspension administration instructions . Recommended Dosage Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma and Waldenström’s Macroglobulinemia The recommended dosage of IMBRUVICA for CLL/SLL and WM is 420 mg orally once daily until disease progression or unacceptable toxicity.

Contraindications

None None

Warnings and precautions

Hemorrhage : Monitor for bleeding and manage . Infections : Monitor patients for fever and infections, evaluate promptly, and treat . Cardiac Arrhythmias , Cardiac Failure , and Sudden Death : Monitor for symptoms of arrhythmias and cardiac failure and manage . Hypertension : Monitor blood pressure and treat . Cytopenias : Check complete blood counts monthly . Second Primary Malignancies : Other malignancies have occurred in patients, including skin cancers, and other carcinomas . Hepatotoxicity, Including Drug- Induced Liver Injury : Monitor hepatic function throughout treatment .

Pregnancy

Pregnancy Risk Summary IMBRUVICA can cause fetal harm based on findings from animal studies. There are no available data on IMBRUVICA use in pregnant women to inform a drug-associated risk of major birth defects and miscarriage.

Storage and supply

Capsules The 70 mg capsules are supplied as yellow opaque capsules, marked with “ibr 70 mg” in black ink, in white HDPE bottles with a child-resistant closure: 28 capsules per bottle: NDC 57962-070-28 The 140 mg capsules are supplied as white opaque capsules, marked with “ibr 140 mg” in black ink, in white HDPE bottles with a child-resistant closur…

Source: Ibrutinib (Imbruvica) — US FDA prescribing information, 2025-10-21, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.