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.
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.

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
• Waldenström macroglobulinemia

Patient drug information

• Ibrutinib (Imbruvica) package insert
• Ibrutinib (Imbruvica) patient drug information (Chemocare)
• Ibrutinib (Imbruvica) patient drug information (UpToDate)

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)."

Also known as

CRA-032765, PCI-32765