Ibrutinib is an antineoplastic agent used to treat chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenstrom's Macroglobulinemia. Ibrutinib is a small molecule that acts as an irreversible potent inhibitor of Burton's tyrosine kinase.
- Mechanism
- Curator reviewed · 1 reference
Ibrutinib is an inhibitor of Bruton’s tyrosine kinase (BTK). It forms a covalent bond with a cysteine residue in the active site of BTK (Cys481), leading to its inhibition. The inhibition of BTK plays a role in the B-cell receptor signaling and thus, the presence of ibrutinib prevents the phosphorylation of downstream substrates such as PLC-γ.
- Primary indication
- Ibrutinib is indicated for the treatment of the following conditions.Curator reviewed · 19 structured indications
- Formula / weight
- C25H24N6O2 · 440.507 g/mol (avg)
- First approval
- Canada, 2014 · United States, 2013 · European Union, 2016
- Code names
- CRA-032765 · JNJ-54179060 · PC-32765 · PCI-32765 · PCI-32765-00
- Brand names
Resolves to
XYFPWWZEPKGCCK-GOSISDBHSA-NSMILESNC1=NC=NC2=C1C(=NN2[C@@H]1CCCN(C1)C(=O)C=C)C1=CC=C(OC2=CC=CC=C2)C=C1What you can answer from here — as of June 15, 2026
Which drugs share a target with Ibrutinib, and which of those have an active Phase 3 trial?
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