Ibrutinib (Imbruvica)
General information
Class/mechanism: Irreversible inhibitor of Bruton's tyrosine kinase (BTK), which is an enzyme that participates in the B-cell receptor (BCR) signal cascade and cytokine receptor pathways. BCR signaling is believed to promote cell proliferation, adhesion, and survival in B-cell malignancies. Inhibition of BTK interferes with the processes above, as well as B-cell chemotaxis and trafficking.[1][2][3]
[4]
Route: PO
Extravasation: n/a
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]
Additional information
- Woyach JA, Furman RR, Liu TM, Ozer HG, Zapatka M, Ruppert AS, Xue L, Li DH, Steggerda SM, Versele M, Dave SS, Zhang J, Yilmaz AS, Jaglowski SM, Blum KA, Lozanski A, Lozanski G, James DF, Barrientos JC, Lichter P, Stilgenbauer S, Buggy JJ, Chang BY, Johnson AJ, Byrd JC. Resistance mechanisms for the Bruton's tyrosine kinase inhibitor ibrutinib. N Engl J Med. 2014 Jun 12;370(24):2286-94. Epub 2014 May 28. link to original article PubMed
Diseases for which it is used
- Chronic lymphocytic leukemia (CLL) and Small lymphocytic lymphoma (SLL)
- Diffuse large B-cell lymphoma
- Follicular lymphoma
- Mantle cell lymphoma
- Marginal zone lymphoma
- Waldenström macroglobulinemia
Patient drug information
- Ibrutinib (Imbruvica) package insert[1]
- Ibrutinib (Imbruvica) patient drug information (Chemocare)[5]
- Ibrutinib (Imbruvica) patient drug information (UpToDate)[6]
History of changes in FDA indication
- 11/13/2013: FDA granted accelerated approval "for the treatment of patients with mantle cell lymphoma (MCL) who have received at least one prior therapy."
- 2/12/2014: FDA granted accelerated approval "for the treatment of patients with chronic lymphocytic leukemia (CLL) who have received at least one prior therapy."
- 7/28/2014: FDA approval expanded to include patients with chronic lymphocytic leukemia (CLL) who carry a deletion in chromosome 17 (17p deletion).
- 1/29/2015: FDA approval expanded "for the treatment of patients with Waldenström’s macroglobulinemia (WM)."
- 3/4/2016: FDA approval expanded "for the treatment of patients with chronic lymphocytic leukemia (CLL)."
- 1/18/2017: FDA accelerated approval for treatment of patients with "marginal zone lymphoma (MZL) who require systemic therapy and have received at least one prior anti-CD20-based therapy."
Also known as
CRA-032765, PCI-32765
References
- ↑ 1.0 1.1 1.2 Ibrutinib (Imbruvica) package insert
- ↑ Ibrutinib (Imbruvica) package insert (locally hosted backup)
- ↑ Imbruvica manufacturer's website
- ↑ Pharmacyclics BTK inhibitor website
- ↑ Ibrutinib (Imbruvica) patient drug information (Chemocare)
- ↑ Ibrutinib (Imbruvica) patient drug information (UpToDate)
- Drug index
- Chemotherapy
- Oral medications
- Kinase inhibitors
- BTK inhibitors
- EGFR inhibitors
- ITK inhibitors
- TEC inhibitors
- TXK inhibitors
- Chronic lymphocytic leukemia (CLL) and Small lymphocytic lymphoma (SLL) medications
- Diffuse large B-cell lymphoma medications
- Follicular lymphoma medications
- Mantle cell lymphoma medications
- Marginal zone lymphoma medications
- Waldenström macroglobulinemia medications
- Drugs FDA approved in 2013