Table 1.
Comparison of selected biochemical, pharmacokinetic, and pharmacodynamic properties for ibrutinib, acalabrutinib, and zanubrutinib.
| Ibrutinib | Acalabrutinib | Zanubrutinib | |
|---|---|---|---|
| FDA-approved indication(s)13,37,43 | CLL, MCL, MZL, WM, GVHD | CLL, MCL | MCL, WM, MZL |
| FDA-approved dose(s)13,37,43 | 420 or 560 mg QD | 100 mg BID | 160 mg BID or 320 mg QD |
| BTK IC50, nM 45 | 1.5 | 5.1 | 0.5 |
| TEC selectivity, fold | 6.7 | 25 | 88 |
| EGFR selectivity, fold | 3.5 | 196 | 42 |
| Half-life, hours | ~4–6 | ~0.6–2.8 | ~2–4 |
| Median BTK lymph node occupancy at trough46,47 | 420 mg QD: > 90% | 200 mg QD: 90% 100 mg BID: 95.8% |
320 mg QD: 94% 160 mg BID: 100% |
BID, twice daily; BTK, Bruton tyrosine kinase; CLL, chronic lymphocytic leukemia; EGFR, epidermal growth factor receptor; FDA, US Food and Drug Administration; GVHD, graft-versus-host disease; MCL, mantle cell lymphoma; MZL, marginal zone lymphoma; QD, once daily; TEC, tyrosine kinase expressed in carcinoma; WM, Waldenström macroglobulinemia.