Category: pharmacological
Aliases: Calquence, ACP-196
Second-generation covalent BTK inhibitor — designed for higher BTK selectivity than ibrutinib (less off-target EGFR/ITK/TEC). Indications: CLL/SLL, mantle cell lymphoma. Lower rates of atrial fibrillation, hypertension, and bleeding vs ibrutinib in head-to-head ELEVATE-RR. CYP3A4 substrate; PPIs reduce absorption ~70% — requires acid for solubility. PK (Calquence label, SS 100 mg PO bid): Cmax 563 ng/mL (29% CV), AUC24 1843 ng·h/mL (38% CV), Tmax median 0.9 h, t½ 1 h, F 25%, Vss 101 L (52% CV), protein binding 97.5%. Short t½ explains bid dosing despite irreversible BTK binding (target turnover is what matters).
PO: 1h