What is Ibrutinib (Imbruvica)?

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Last updated: May 10, 2025View editorial policy

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From the Guidelines

Ibrutinib is a highly effective treatment option for patients with Waldenström's macroglobulinemia, with an overall response rate of 91% and a major response rate of 73%, as demonstrated in a prospective study of 63 symptomatic patients 1. The typical dose of ibrutinib is 420 mg taken once daily, and it works by blocking Bruton's tyrosine kinase (BTK), an enzyme that helps certain cancer cells grow and survive. Some key points to consider when prescribing ibrutinib include:

  • Common side effects include neutropenia, thrombocytopenia, postprocedural bleeding, epistaxis, and atrial fibrillation, which were reported in a study of 63 symptomatic patients with WM 1
  • Patients should be monitored regularly for treatment effectiveness and potential side effects, with regular blood tests and follow-up appointments
  • Ibrutinib can interact with many drugs, particularly blood thinners and those metabolized by CYP3A enzymes, so it's essential to inform healthcare providers about all medications being taken
  • The estimated 2-year progression-free survival (PFS) rate was 69%, and the estimated 2-year overall survival (OS) rate was 95% in a study of 63 symptomatic patients with WM 1
  • A more recent study confirmed the efficacy and safety of ibrutinib in patients with relapsed/refractory CLL/SLL, with a median PFS of 44 months and an estimated 5-year PFS rate of 40% 1

From the FDA Drug Label

IMBRUVICA is a prescription medicine used to treat: Adults with chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) Adults with chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL) with 17p deletion. Adults with Waldenström’s macroglobulinemia (WM). Adults and children 1 year of age and older with chronic graft versus host disease (cGVHD) after failure of 1 or more lines of systemic therapy.

Ibrutinib is used to treat various conditions, including:

  • Chronic lymphocytic leukemia (CLL)/Small lymphocytic lymphoma (SLL)
  • CLL/SLL with 17p deletion
  • Waldenström’s macroglobulinemia (WM)
  • Chronic graft versus host disease (cGVHD) in adults and children 1 year of age and older 2

From the Research

Ibrutinib Overview

  • Ibrutinib is a Bruton's tyrosine kinase inhibitor used in the treatment of relapsed or refractory mantle cell lymphoma and chronic lymphocytic leukemia 3, 4, 5, 6
  • It was granted accelerated approval by the US Food and Drug Administration in November 2013 for mantle cell lymphoma and in February 2014 for chronic lymphocytic leukemia 3, 6

Efficacy

  • In a phase 2 study of 111 patients with relapsed or refractory mantle cell lymphoma, the overall response rate was 68% and the median progression-free survival was 13.9 months 3
  • In a phase 3 trial (RESONATE) comparing ibrutinib and ofatumumab for the treatment of relapsed and refractory chronic lymphocytic leukemia, ibrutinib demonstrated a significantly higher overall response rate (43% vs 4%) and improved overall survival at 12 months (90% vs 81%) 3
  • Ibrutinib has shown durable remission, improved progression-free survival, and overall survival in indolent B-cell lymphoid malignancies 3, 4, 5

Safety and Tolerability

  • Ibrutinib was well tolerated, with no dose-limiting toxicity observed 3, 4, 5
  • The most common adverse reactions included thrombocytopenia, diarrhea, neutropenia, bruising, upper respiratory tract infection, anemia, fatigue, musculoskeletal pain, peripheral edema, and nausea 6
  • In patients intolerant of ibrutinib, zanubrutinib, a next-generation BTK inhibitor, has been shown to be well tolerated and effective 7

Clinical Use

  • Ibrutinib is an effective treatment modality as a salvage therapy for mantle cell lymphoma and chronic lymphocytic leukemia, particularly in older patients who are not candidates for intensive chemotherapy and/or those with del (17p) 3, 4, 5
  • Current practice guidelines recommend ibrutinib as an upfront treatment option for patients with chronic lymphocytic leukemia and del (17p) 3

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

A review of a novel, Bruton's tyrosine kinase inhibitor, ibrutinib.

Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, 2016

Research

FDA Approval: Ibrutinib for Patients with Previously Treated Mantle Cell Lymphoma and Previously Treated Chronic Lymphocytic Leukemia.

Clinical cancer research : an official journal of the American Association for Cancer Research, 2015

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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