৳ 1,326/unit
Pack: ৳ 39,780
৳ 1,326/unit
Pack: ৳ 39,780
At a glance
Ibrutinib is a kinase inhibitor used for the treatment of Mantle Cell Lymphoma (MCL), Chronic Lymphocytic Leukemia (CLL), CLL with 17p deletion, Waldenström's Macroglobulinemia (WM), and Marginal Zone Lymphoma (MZL).
Indications
- Mantle Cell Lymphoma (MCL) - who have received at least one prior therapy
- Chronic Lymphocytic Leukemia (CLL) - who have received at least one prior therapy
- Chronic Lymphocytic Leukemia 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
Pharmacology
Ibrutinib is a small-molecule inhibitor of BTK. It 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. Ibrutinib inhibits malignant B-cell proliferation and survival in vivo.
Dosage
Adult Dose (Oral):
- Mantle Cell Lymphoma (MCL) & Marginal Zone Lymphoma (MZL): 560 mg (four 140 mg capsules) once daily
- Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL) & Waldenström Macroglobulinemia (WM): 420 mg (three 140 mg capsules) once daily
- CLL (in combination with bendamustine and rituximab): 420 mg once daily
Hepatic Impairment: Mild (Child Pugh Class A): 140 mg once daily; Moderate-to-severe (Classes B and C): Avoid use
Child Dose: Safety and efficacy not established
Side effects
Most Common (>10%):
- Diarrhea (51-63%)
- Bruising (30-54%)
- Fatigue (31-41%)
- Nausea (21-31%)
- Rash (25-27%)
- Musculoskeletal pain (27-37%)
- Headache (13-19%)
- Dizziness (14-21%)
- Upper respiratory tract infection (34-48%)
- Hemorrhage (48%)
- Neutropenia (27-29%)
- Thrombocytopenia (10-17%)
Serious: Hemorrhage, Infections, Cytopenias, Atrial Fibrillation, Hypertension, Second Primary Malignancies, Tumor Lysis Syndrome
Use in pregnancy
Use in Pregnancy: Ibrutinib can cause fetal harm; animal studies showed embryofetal toxicity including malformations; if used during pregnancy or patient becomes pregnant, apprise of potential risk to fetus.
Pregnancy Category: D — always consult a doctor before taking during pregnancy.
Precautions & warnings
Precautions:
- Monitor for bleeding
- Monitor patients for fever and infections and evaluate promptly
- Complete blood counts should be checked monthly
- Monitor for atrial fibrillation
- Second primary malignancies (including skin cancers) have occurred
- Monitor patients at risk for Tumor Lysis Syndrome (TLS)
- Embryo-Fetal Toxicity: Can cause fetal harm; advise women to avoid pregnancy
Overdose effects
Overdose: No specific experience in management of overdose; one healthy subject experienced reversible Grade 4 hepatic enzyme increases (AST and ALT) after 1680 mg dose; closely monitor patients who ingest more than recommended dosage and provide appropriate supportive treatment.
Storage conditions
Store in a dry place below 30°C, protect from light; keep out of reach of children.