Ibrutinib (Imbruvica)

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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]

Resistance mechanisms

  1. 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

Significant side effects

  1. Review: Leong DP, Caron F, Hillis C, Duan A, Healey JS, Fraser G, Siegal D. The risk of atrial fibrillation with ibrutinib use: a systematic review and meta-analysis. Blood. 2016 Jul 7;128(1):138-40. Epub 2016 May 31. link to original article PubMed
  2. Review: Caron, F., Leong, D. P., Hillis, C., Fraser, G., & Siegal, D. (2017). Current understanding of bleeding with ibrutinib use: a systematic review and meta-analysis. Blood Advances, 1(12), 772-778. link to original article

Diseases for which it is used

Patient drug information

History of changes in FDA indication

Also known as

  • Code names: CRA-032765, PCI-32765
  • Brand name: Imbruvica


  1. 1.0 1.1 1.2 Ibrutinib (Imbruvica) package insert
  2. Ibrutinib (Imbruvica) package insert (locally hosted backup)
  3. Imbruvica manufacturer's website
  4. Pharmacyclics BTK inhibitor website
  5. Ibrutinib (Imbruvica) patient drug information (Chemocare)
  6. Ibrutinib (Imbruvica) patient drug information (UpToDate)