Table 1. Activity of ALK-inhibitors emerged from completed and ongoing clinical trials.
| Drug | Study (reference) | Previous crizotinib | Crizotinib-naive | |||
|---|---|---|---|---|---|---|
| ORR | mPFS (months) | ORR | mPFS (months) | |||
| Crizotinib | Phase I (63) (PROFILE 1001) | 87/143 (60.8%) | 9.7 | |||
| Phase II (12) (PROFILE 1005) | 155/259 (59.8%) | 8.1 | ||||
| Phase III 2nd line (11) (PROFILE 1007) | 113/173 (65%) | 7.7 | ||||
| Phase III 1st line (13) (PROFILE 1014) | 128/172 (74%) | 10.9 | ||||
| Ceritinib (LDK378) | Phase I (70) (ASCEND-1) | 92/163 (56%) | 6.9 | 60/83 72% |
18.4 | |
| Phase II (71) (ASCEND-2) | 54/140 (38.6%) | 5.7 | ||||
| Phase II (72) (ASCEND-3) | 79/124 (63.7%) | 11.1 | ||||
| Alectinib (CH542480/RO5424802) | Phase I/II (73) (AF-001JP), 240/300 mg BID | 58/61 (95%) | NA | |||
| Phase I/II (74), dose escalation (AF-002JG) | 24/44 (55%) | NA | ||||
| Phase II (75) (NP28761) | 33/69 (48%) | NA | ||||
| Phase II (76) (NP28673) | 61/122 (50%) | 10.3 | ||||
| Brigatinib (AP26113) | Phase I/II (77), phase II portion (NCT01449461) | 50/70 (71%) | 13.4 | 8/8 (100%) | Not reached | |
| Lorlatinib (PF-06463922) | Phase I/II (78), dose escalation (NCT01970865) | 17/32 (53.1%) | NA | 2/2 (100%) | NA | |
| Entrectinib (RXDX-101) | Phase I/II (79), dose escalation (NCT02097810) | 2/4 (50%) | NA | |||
ALK, anaplastic lymphoma kinase; ORR, objective response rate; mPFS, median progression-free survival; NA, not available.