acalabrutinib

Acalabrutinib is a highly selective, second-generation small molecule inhibitor of Bruton tyrosine kinase (BTK), developed as a targeted therapy for certain B-cell malignancies. It works by covalently binding to the Cys481 residue in the BTK active site, thereby inhibiting BTK enzymatic activity and downstream signaling pathways essential for malignant B-cell proliferation and survival. Acalabrutinib demonstrates greater selectivity for BTK compared to first-generation inhibitors like ibrutinib, resulting in fewer off-target effects. It is indicated for the treatment of mantle cell lymphoma (MCL), chronic lymphocytic leukemia (CLL), and small lymphocytic lymphoma (SLL) in adults[2][3][4][6][8]. The drug was rationally designed to minimize adverse effects while maintaining potent anti-cancer efficacy[4][8]. Acalabrutinib is administered orally and marketed under the brand name Calquence.

Brand names

Calquence

Other names

acalabrutinibACP-196ACP196ACP 196Calquence