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ibrutinib
- Development stage
- Approved
- Lead developer
- Pharmacyclics
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Ibrutinib is a small molecule, oral antineoplastic agent classified as a Bruton's tyrosine kinase (BTK) inhibitor. It acts by irreversibly binding to the cysteine residue (Cys481) in the active site of BTK, thereby inhibiting its enzymatic activity and blocking B-cell receptor signaling pathways. This inhibition disrupts processes essential for malignant B-cell proliferation, survival, adhesion, and migration. Ibrutinib is primarily indicated for the treatment of chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma (SLL), mantle cell lymphoma (MCL), Waldenström's macroglobulinemia (WM), marginal zone lymphoma (MZL), and chronic graft versus host disease (cGVHD). The drug was developed by Pharmacyclics and first approved in 2013.
- Brand names
- Imbruvica
- Other names
- PCI-32765PCI32765PCI 32765
02
Targets
JAK3 (Janus kinase 3)LCK (Proto-oncogene tyrosine-protein kinase Lck)FYN (Proto-oncogene tyrosine-protein kinase Fyn)BTK (Bruton tyrosine kinase)ITK (Interleukin 2-inducible T-cell kinase)
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