| IMBRUVICA™ (ibrutinib) capsules, for oral use
Initial U.S. Approval: 2013
Ibrutinib is an inhibitor of Bruton's tyrosine kinase (BTK). It is a white to off-white solid with the empirical formula C25H24N6O2 and a molecular weight 440.50. Ibrutinib is freely soluble in dimethyl sulfoxide, soluble in methanol and practically insoluble in water.
| Mechanism of Action:
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.
| INDICATIONS AND USAGE:
IMBRUVICA is a kinase inhibitor indicated for the treatment of patients with mantle cell lymphoma (MCL) who have received at least one prior therapy.
This indication is based on overall response rate. An improvement in survival or disease-related symptoms has not been established
WARNINGS AND PRECAUTIONS
| ADVERSE REACTIONS
The most common adverse reactions (≥20%) in patients with MCL were thrombocytopenia, diarrhea, neutropenia, anemia, fatigue, musculoskeletal pain, peripheral edema, upper respiratory tract infection, nausea, bruising, dyspnea, constipation, rash, abdominal pain, vomiting and decreased appetite.
To report SUSPECTED ADVERSE REACTIONS, contact Pharmacyclics at 1-877-877-3536 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
CYP3A Inducers: Avoid co-administration with strong CYP3A inducers.
USE IN SPECIFIC POPULATIONS
See PACKAGE INSERT for PATIENT COUNSELING INFORMATION and Medication Guide.
| DOSAGE AND ADMINISTRATION:
560 mg taken orally once daily (four 140 mg capsules once daily.
Capsules should be taken orally with a glass of water. Do not open, break, or chew the capsules.
| Package insert data: [Accessed: Jan 2014].
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©Pharmacyclics, Inc. 2013 Issued: November 2013
Initial U.S. Approval: 2013
National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
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