Orelabrutinib is a small molecule inhibitor of Bruton's tyrosine kinase with potential antineoplastic activity.
Uses
Orelabrutinib has been previously approved to treat patients with relapsed or refractory (R/R) mantle cell lymphoma and R/R chronic lymphocytic leukemia/small lymphocytic lymphoma.
Biological Activity
Orelabrutinib (ICP-022) is a potent, orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).
Mechanism of action
Upon administration, orelabrutinib binds to and inhibits the activity of BTK. This prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, inhibiting the growth of malignant B-cells that overexpress BTK.
