Table 1.
Activity of KRASG12C inhibitors in early-phase clinical trials.
| KRASG12C inhibitor | Sotorasib (AMG 510) | Adagrasib (MRTX849) | JNJ-74699157 (ARS-3248) | LY3499446 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sponsor | Amgen | Mirati Therapeutics | Janssen | Eli Lilly | ||||||||||
| Clinical Trial | Phase I/II (CodeBreaK 100) | Phase I/II (NCT03785249) *Last update: 2019 & 2020 AACR-NCI-EORTC Conference |
Phase I (NCT04006301) | Phase I/II (NCT04165031) | ||||||||||
| Patient population | KRASG12C-mutated advanced cancer | KRASG12C-mutated advanced cancer | KRASG12C-mutated advanced cancer | KRASG12C-mutated advanced cancer | ||||||||||
| Dose (mg) | All doses | 960 mg daily | All doses | 600 mg b.i.d | Terminated | Terminated | ||||||||
| NSCLC | CRC | AC | NSCLC | CRC | AC | NSCLC | CRC | AC | NSCLC | CRC | AC | NR | NR | |
| Study population (N) | 59 | 42 | 28 | 34 | 25 | 26 | 6 | 4 | 2 | 51 | 18 | 6 | NR | NR |
| ORR (%) | 32.2 | 7.1 | 14.3 | 35.3 | 12 | NR | 50 | 25 | 0 | 45 | 17 | 66 | NR | NR |
| DCR (%) | 88.1 | 73.8 | 75 | 91.2 | 80 | NR | 100 | 75 | 100 | 96 | 94 | 100 | NR | NR |
| mDOR (mo.) | 10.9 | 5.4 | NR | NR | NR | NR | NR | NR | NR | NR | NR | NR | NR | NR |
| mPFS (mo.) | 6.3 | 4 | NR | NR | NR | NR | NR | NR | NR | NR | NR | NR | NR | NR |