Table 1.
The approved BTK inhibitors and their indications.
| Compound Number and Common Name | Trade Name | Indications | Dosage | Corporation | Stages |
|---|---|---|---|---|---|
| 1 (Ibrutinib) | Imbruvia | MCL, CLL, SLL, WM, cGVHD, etc | 420 or 560 mg/day, capsule or tablet | Pharmacyclics/Johnson | Approved (FDA: November 2013; EMA: 2014.4; JP PMDA: March 2016) |
| 5 (Zanubrutinib) [4] | Brukinsa | MCL | 80 mg bid, capsule | BeiGene | Approved (FDA: November 2019; CN NMPA: June 2020) |
| 7 (Acalabrutinib) | Calquence | MCL, CLL, SLL | 100 mg bid, capsule | Acerta Pharma | Approved (FDA: November 2017) |
| 8 (Tirabrutinib/ONO/GS-4059) | Velexbru | PCNSL | 480 mg qd, tablet | Ono Pharma | Approved (JP PMDA: 25 March 2020) |
| 11 (Olmutinib/HM-61713/BI-1482694) | Olita | NSCLC | 800 mg/day, tablet | Hanmi Pharmaceuticals | Approved (Korea: May 2016) |
| 19 (Orelabrutinib/ICP-022) | MCL, CLL, SLL | 150 mg qd, tablet | InnoCare Pharma | Approved (CN NMPA: December 2020) |
Note: MCL, mantle cell lymphoma; CLL, chronic lymphocytic leukemia; SLL, small lymphocytic lymphoma; WM, Waldenstrom’s macroglobulinemia; cGVHD, chronic graft-versus-host disease; PCNSL, primary central nervous system lymphoma; NSCLC, non-small cell lung cancer; FDA, Food and Drug Administration; EMA, European Medicines Agency; NMPA, National Medical Products Administration; PMDA, Pharmaceuticals and Medical Devices Agency.