Name of approved BTKi | Type | Study design | Pivotal study* | ORR | CRR | Adverse effects |
---|---|---|---|---|---|---|
Ibrutinib | Covalent | Phase 2 | Targeting BTK with ibrutinib in relapsed or refractory mantle cell lymphoma. N Engl J Med 369: 507–516 | 68% | 21% | Diarrhea (50%), fatigue (41%), nausea (31%), peripheral edema (28%), dyspnea (27%), constipation (25%), upper respiratory tract infection (23%), vomiting (23%), and decreased appetite (21%) |
Acalabrutinib | Covalent | Phase 2 | Acalabrutinib in relapsed or refractory mantle cell lymphoma (ACE-LY-004): a single-arm, multicenter, Phase 2 trial. Lancet 2018; 391(10121):659–667 | 81% | 40% | Headache (38%), diarrhea (31%), fatigue (27%), and myalgia (21%). Neutropenia (10%), anemia (9%), and pneumonia (5%) |
Zanubrutinib | Covalent | Phase 2 | Treatment of patients with relapsed or refractory mantle cell lymphoma with zanubrutinib, a selective inhibitor of Bruton’s tyrosine kinase. Clin Cancer Res. 2020;26(16):4216–4224 | 84% | 69% | Neutropenia (48.8%), Leukopenia (34.9%), Thrombocytopenia (32.6%) Anemia (15.1%) URI (34.9%) Rash (33.7%) Hypokalemia (16.3%) Diarrhea (15.1%) Hypertension (15.1%) Lung infection (12.8%) ALT elevation (14%) |
Pirtobrutinib | Non-covalent | Phase 2 | Pirtobrutinib in relapsed or refractory B cell malignancies (BRUIN): a phase 1/2 study. Lancet. 2021 Mar 6;397(10277):892–901 | 51% in BTK pretreated and 82% in BTK naïve patients | 13% | Fatigue (23%), diarrhea (19%), neutropenia (18%), and contusion (17%) |