Oral, once-daily dosing
IMBRUVICA® is available in two formulations, including a single tablet, once-daily option
The recommended dose for MZL is 560 mg per day, administered orally as either one 560-mg tablet or four 140-mg capsules
IMBRUVICA® tablets or capsules should be swallowed whole with water at approximately the same time each day
Do not open, break, or chew the capsules. Do not cut, crush or chew the tablets
Patients should take a missed dose of IMBRUVICA® as soon as possible on the SAME DAY, with a return to the regular schedule on the following day
If a full day of treatment is missed, patients should NOT take extra doses to make up for the missed dose
Patients should NOT take more than their prescribed dose per day
Instruct your patients to call their healthcare provider or go to the nearest hospital emergency room right away if they take too much IMBRUVICA®
Once-daily dosing is necessary to ensure inhibition of BTK enzymatic activity1
Inhibition of BTK by IMBRUVICA® has a disruptive effect on 3 key B-cell processes as shown by in vitro and in vivo studies1:
- Inhibits survival and proliferation1-6
- Inhibits adhesion1,6-11
- Modulates chemotaxis and trafficking1,5,7,9,11-14
Correlation to clinical effect has not been established.
BTK=Bruton’s tyrosine kinase, MZL=marginal zone lymphoma.
- IMBRUVICA® (ibrutinib) Prescribing Information. Pharmacyclics LLC. 2020.
- Burger JA, Buggy JJ. Bruton tyrosine kinase (BTK) inhibitor ibrutinib (PCI-32765). Leuk Lymphoma. 2013;54(11):2385-2391.
- Honigberg LA, Smith AM, Sirisawad M, et al. The Bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci USA. 2010;107(29):13075-13080.
- Cinar M, Hamedani F, Mo Z, et al. Bruton tyrosine kinase is commonly overexpressed in mantle cell lymphoma and its attenuation by ibrutinib induces apoptosis. Leuk Res. 2013;37(10):1271-1277.
- Ponader S, Chen S-S, Buggy JJ, et al. The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo. Blood. 2012;119(5):1182-1189.
- Herman SEM, Gordon AL, Hertlein E, et al. Bruton tyrosine kinase represents a promising therapeutic target for treatment of chronic lymphocytic leukemia and is effectively targeted by PCI-32765. Blood. 2011;117(23):6287-6296.
- Chang BY, Francesco M, Steggerda S, et al. Ibrutinib inhibits malignant cell adhesion and migration and reduces tumor burden in lymph node and bone marrow in a murine model of mantle cell dissemination and progression. Presented at: 104th Annual Meeting of the American Association for Cancer Research; April 6-10, 2013; Washington, DC. Abstract 923.
- Binsky I, Lantner F, Grabovsky V, et al. TAp63 regulates VLA-4 expression and chronic lymphocytic leukemia cell migration to the bone marrow in a CD74-dependent manner. J Immunol. 2010;184(9):4761-4769.
- Kurtova AV, Tamayo AT, Ford RJ, Burger JA. Mantle cell lymphoma cells express high levels of CXCR4, CXCR5, and VLA-4 (CD49d): importance for interactions with the stromal microenvironment and specific targeting. Blood. 2009;113(19):4604-4613.
- Chang BY, Francesco M, de Rooij MFM, et al. Egress of CD19+CD5+ cells into peripheral blood following treatment with the Bruton tyrosine kinase inhibitor ibrutinib in mantle cell lymphoma patients. Blood. 2013;122(14):2412-2424.
- de Rooij MFM, Kuil A, Geest CR, et al. The clinically active BTK inhibitor PCI-32765 targets B-cell receptor- and chemokine-controlled adhesion and migration in chronic lymphocytic leukemia. Blood. 2012;119(11):2590-2594.
- Kindt TJ, Goldsby RA, Osborne BA. Kuby Immunology. 6th ed. New York, NY: W.H. Freeman; 2007.
- Burger JA, Ghia P, Rosenwald A, Caligaris-Cappio F. The microenvironment in mature B-cell malignancies: a target for new treatment strategies. Blood. 2009;114(16):3367-3375.
- Davids MS, Burger JA. Cell trafficking in chronic lymphocytic leukemia. Open J Hematol. 2012;3(S1)-3. Published online February 21, 2012.