Ibrucent 140: Each capsule contains Ibrutinib INN 140 mg
Ibrutinib is a small-molecule inhibitor of 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.
Ibrutinib, is a kinase inhibitor indicated for the treatment of patients with:
• Mantle cell lymphoma (MCL) who have received at least one prior therapy. Accelerated approval was granted for this indication based on overall response rate. Continued approval for this indication may be contingent upon verification of clinical benefit in confirmatory trials.
• Chronic lymphocytic leukemia (CLL) who have received at least one prior therapy
• Chronic lymphocytic leukemia with 17p deletion
• Waldenström’s macroglobulinemia (WM)
MCL: 560 mg taken orally once daily (four 140 mg capsules once daily)
CLL and WM: 420 mg taken orally once daily (three 140 mg capsules once daily)
Capsules should be taken orally with a glass of water. The capsules should not be opened, broke, or chewed
The most common adverse reactions (≥25%) in patients with B-cell malignancies (MCL, CLL, WM) were thrombocytopenia, neutropenia, diarrhea, anemia, fatigue, musculoskeletal pain, bruising, nausea, upper respiratory tract infection, and rash.
• Hemorrhage: Should be monitored for bleeding
• Infections: Patients should be monitored for fever and infections and evaluated
• Cytopenias: Complete blood counts should be checked monthly
• Atrial Fibrillation: Patients should be monitored for atrial fibrillation
• Second Primary Malignancies: Other malignancies have occurred in patients, including skin cancers, and other carcinomas
• Tumor Lysis Syndrome (TLS): Patients should be monitored at risk for TLS (e.g. high tumor burden)
• Embryo-Fetal Toxicity: Can cause fetal harm. Women should be advised of the potential risk to a fetus and to avoid pregnancy while taking the drug
Pregnancy Category D
Based on animal data, Ibrutinib can cause fetal harm when administered to a pregnant woman. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.
It is not known whether Ibrutinib is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Ibrutinib, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
The safety and effectiveness of Ibrutinib in pediatric patients have not been established.
No overall differences in safety or effectiveness were observed between elderly subjects and younger subjects. No overall differences in effectiveness were observed between these patients and younger patients. Cardiac adverse events (atrial fibrillation and hypertension), infections (pneumonia, urinary tract infection and cellulitis) and gastrointestinal events (diarrhea and dehydration) occurred more frequently among elderly patients.
CYP3A Inhibitors: Co-administration with strong and moderate CYP3A inhibitors should be avoided. If a moderate CYP3A inhibitor must be used, Ibrutinib dose should be reduced
CYP3A Inducers: Co-administration with strong CYP3A inducers should be avoided
Ibrucent 140: Each box contains 3 blister strips of 4 capsules
Ibrucent 140: Each bottle contains 90 capsules