Table 1.
Comparison of features and properties between ibrutinib, acalabrutinib, and zanubrutinib.
| Ibrutinib | Acalabrutinib | Zanubrutinib | |
|---|---|---|---|
| Alternative names | PCI-32765 | ACP-196 | BGB-3111 |
| Mechanism of action | C481, ATP-binding domain | C481, ATP-binding domain | C481, ATP-binding domain |
| Dosage | 420 mg, qd (CLL/SLL, WM); 560 mg, qd (MCL, MZL) | 100 mg, bid (MCL, CLL/SLL) | 160 mg, bid (MCL) |
| Pharmacodynamics | |||
| Kinetics (nM) | 54.2 | 181 | 126 |
| BTK (IC50, nM) | 1.5 | 5.1 | 0.5 |
| TEC (IC50, nM) | 10 | 126 | 44 |
| ITK (IC50, nM) | 4.9 | >1000 | 50 |
| TXK (IC50, nM) | 2 | 368 | 2.2 |
| BMX (IC50, nM) | 0.8 | 46 | 1.4 |
| EGFR (IC50, nM) | 5.3 | >1000 | 21 |
| ERBB2 (IC50, nM) | 6.4 | ~1000 | 88 |
| ERBB4 (IC50, nM) | 3.4 | 16 | 6.9 |
| BLK (IC50, nM) | 0.1 | >1000 | 2.5 |
| JAK3 (IC50, nM) | 32 | >1000 | 1377 |
| hPBMC (EC50, nM) | 0.6 | 2.9 | 0.9 |
| hWB (EC50, nM) | 5.8 | 9.2 | 2.4 |
| Pharmacokinetics | |||
| Cmax (ng/ml) | 35 | 323 | 346 |
| tmax (h) | 1–2 | 0.75 | 2 |
| AUC (ng h/ml) | 708 | 1111 | 1405 |
| Vd,ss/F | 10000 | 101 | 881 |
| t1/2 (h) | 4–6 | 0.9 | 3.31 |
| Clearance (L/h) | 62 | 159 | 182 |