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ibrutinib (Imbruvica)

Indications: - treatment of mantle cell lymphoma - for patients with prior treatment failure - treatment of chronic lymphocytic leukemia - for patients with prior treatment failure - untreated older patients (>=65 years) [4] - treatment of Waldenstrom's macroglobulinemia Dosage: - 560 mg PO QD Capsules: 140 mg Adverse effects: - common - skin eruptions are seen in up to 47% of patients [7] - asymptomatic, nonpalpable, petechial rash - palpable, purpuric eruption resembling leukocytoclastic vasculitis - earlier rash onset (~15 days after initiation of drug) - thrombocytopenia, neutropenia, anemia, fatigue, musculoskeletal pain, edema, upper respiratory infection, nausea, vomiting, constipation, diarrhea, bruising, dyspnea, rash, abdominal pain, decreased appetite - other - bleeding, infections, nephrotoxicity, other malignancy - atrial fibrillation [3] - serious infections (11%) 1/3 are invasive fungal infections [3] - initial increase in lymphocyte count when used to treat CLL [5] - ibrutinib impairs ability of lymphocytes to home to lymph nodes, spleen & bone marrow - cardiotoxicity [6] - heart failure - atrioventricular block - supraventricular arrhythmias (atrial fibrillation) - hypertension [6] Mechanism of action: - Bruton tyrosine kinase (BTK) inhibitor [3]

Interactions

drug adverse effects of tyrosine kinase inhibitor(s)

General

small inhibitory antineoplastic agent (ib drug) antineoplastic tyrosine kinase inhibitor

Database Correlations

PUBCHEM correlations

References

  1. FDA News Release: Nov. 13, 2013 FDA approves Imbruvica for rare blood cancer. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm374761.htm
  2. FDA News Release: Feb. 12, 2014 FDA approves Imbruvica to treat chronic lymphocytic leukemia. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm385764.htm
  3. Varughese T, Taur Y, Cohen N et al. Serious infections in patients receiving ibrutinib for treatment of lymphoid cancer. Clin Infect Dis 2018 Aug 16; 67:687. PMID: 29509845 https://academic.oup.com/cid/article-abstract/67/5/687/4917700
  4. Ingram I Ibrutinib Alone Wins in Older CLL Patients. Adding rituximab offered no added benefit. MedPage Today. Dec 01, 2018 https://www.medpagetoday.com/meetingcoverage/ashhematology/76642 - Woyach JA, Ruppert AS, Heerema NA et al. Ibrutinib regimens versus chemoimmunotherapy in older patients with untreated CLL. N Eng J Med. Dec 1, 2018 PMID: 30501481 https://www.nejm.org/doi/full/10.1056/NEJMoa1812836
  5. Geriatric Review Syllabus, 10th edition (GRS10) Harper GM, Lyons WL, Potter JF (eds) American Geriatrics Society, 2019
  6. Jenkins K Ibrutinib Cardiotoxicity: Worse Than With Chemo? High rates of adverse events with so-called targeted therapy. MedPage Today. September 25, 2019 https://www.medpagetoday.com/hematologyoncology/leukemia/82379 - Salem JE, Manouchehri A, Bretagne M et al Cardiovascular Toxicities Associated With Ibrutinib J Am Coll Cardiol 74(13): October 2019 PMID: 31558250 http://www.onlinejacc.org/content/74/13/1667 - Bergler-Klein J Real-Life Insight Into Ibrutinib Cardiovascular Events Defining the Loose Ends. J Am Coll Cardiol 74(13): October 2019 PMID: 31558251 http://www.onlinejacc.org/content/74/13/1679
  7. Mohammed ET, Patel T Asymptomatic Purpuric Eruption on the Scalp of a Middle-aged Man. JN Learning. JAMA Oncology February 18, 2021 PMID: 33599695 https://edhub.ama-assn.org/jn-learning/module/2776412
  8. Highlights of Prescribing Information http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/205552lbl.pdf