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BTK inhibitor Ibrutinib:Brand names,Uses,Dietary instructions and Toxicity

Jul 30,2025

Bruton tyrosine kinase signaling (BTK) is critical step for B-cell development and immunoglobulin synthesis. Ibrutinib is an orally bioavailable bruton tyrosine kinase inhibitor (BTKi) and forms an irreversible covalent bound to BTK at the Cysteine-481 residue.

Ibrutinib

Brand names

Imbruvica?

Chemistry

Ibrutinib is a small molecule with the ability to form a covalent bond with Cys-481 in the ATP binding domain of BTK. The chemical name for ibrutinib is 1-{(3R)-3-[4-amino-3-(4-phenoxyphenl)-1-H-pyrazolo [3,4-d]pyrimidin-1-yl]piperidin-1-yl}prop-2-en-1-one, the molecular formula is C25H24N6O2, and the molecular weight is 440.5 g/mol. The IC50 of ibrutinib for BTK is 0.5 nM, although the drug also has activity against at least nine other kinases with a cognate cysteine, including ITK, TEC, BLK and JAK3, as well as EGF receptor and HER2 [1]. This broad activity may have therapeutic implications; for example, ibrutinib was recently found to bind covalently to ITK in T lymphocytes, thereby leading to a Th1-selective pressure.

Uses

Ibrutinib is an orally bioavailable BTKi and forms an irreversible covalent bound to BTK at Cysteine-481 residue (Herman et al., 2011, Honigberg et al., 2010). However, its binding profile is not restricted to BTK and it inhibits other kinases including interleukin-2-inducible T-cell kinase (ITK), tec protein tyrosine kinase (TEC), BMX and epidermal growth factor receptor (EGFR) (Cheng et al., 2014).[2]

Ibrutinib has been approved by FDA for the treatment of mantle cell lymphoma (MCL) at 2013 (Wang et al., 2013), for chronic lymphocytic leukemia (CLL) at 2014 (Byrd et al., 2013), for Waldenstrom's macroglobulinemia (WM) at 2015 (Treon et al., 2015) and for marginal zone lymphoma (Noy et al., 2017) and chronic graft-versus-host disease in allo-HCT at 2017 (Miklos et al., 2017).

Ibrutinib is generally well tolerated drug with rapid and durable responses but has some adverse events. The most common side effects are diarrhea, upper respiratory tract infection, bleeding, fatigue and cardiac side effects (Tang et al., 2017). These events are generally mild (grade I-II). However AF and bleeding are important and may be severe. Grade ≥ III side effects require strict monitoring. Here side effects of ibrutinib have been summarized and important points in the management of these adverse events have been reviewed.

Dietary instructions

Do not eat grapefruit or Seville oranges (sometimes used in marmalades), or drink grapefruit juice while taking this medication.

Make sure you drink plenty of water or other fluids every day while you are taking ibrutinib.

Side effects

Ibrutinib is generally well tolerated drug with rapid and durable responses but has some side events. The most common side effects are diarrhea, upper respiratory tract infection, bleeding, fatigue and cardiac side effects. These events are generally mild (grade I–II).

Toxicity

Hair and nail toxicities have been reported in 26% and 66% of the patients, respectively. Hair changes are characterized by softening and straightening. Nail changes are brittle fingernails or splitting. These changes are seen usually 6 months after ibrutinib treatment. This time is compatible with growth time of nails. Biotin supplementation may be useful (Bitar et al., 2016).

References

[1] Honigberg LA, Smith AM, Sirisawad M, et al. The bruton tyrosine kinase inhibitor PCI-32765 blocks B-cell activation and is efficacious in models of autoimmune disease and B-cell malignancy. Proc Natl Acad Sci USA. 2010;107(29):13075–13080.

[2] Paydas, Semra. “Management of adverse effects/toxicity of ibrutinib.” Critical reviews in oncology/hematology 136 (2019): Pages 56-63.

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