btk inhibitors + venetoclax

**BTK inhibitors + venetoclax** is a combination therapy pairing Bruton's tyrosine kinase (BTK) inhibitors—such as ibrutinib, acalabrutinib, zanubrutinib, or orelabrutinib—with venetoclax, a selective BCL-2 inhibitor. BTK inhibitors covalently bind BTK to block B-cell receptor signaling critical for B-cell malignancies, while venetoclax inhibits anti-apoptotic BCL-2 to promote tumor cell death; their dual inhibition shows synergistic effects in preclinical and clinical studies. Primarily investigated for relapsed/refractory mantle cell lymphoma (MCL) and chronic lymphocytic leukemia (CLL), it achieves high overall response rates (67-92%) and complete remission rates (53-71%), often with time-limited dosing (e.g., venetoclax 200-400 mg daily after ramp-up), though continuous BTKi use is common in some regimens. Real-world data confirm efficacy in high-risk patients (e.g., TP53 mutations, high Ki-67), with 3-year PFS of 37.5% and OS of 50.8% in R/R MCL, but hematologic toxicities like neutropenia and thrombocytopenia are frequent.

Brand names

VenclextaImbruvicaCalquenceBrukinsa

Other names

venetoclax + covalent Bruton tyrosine kinase inhibitorvenetoclax + BTK inhibitor