Table 2 FDA approved targeted agents for advanced NSCLC with corresponding clinical trials, efficacy, and safety data
From: Targeted therapy in advanced non-small cell lung cancer: current advances and future trends
Actionable mutation | FDA approved therapy (citation) | Clinical trialπ (phase) | Comparator | ORR (%) | mPFS (months) | mOS (months) | Adverse effects |
|---|---|---|---|---|---|---|---|
KRAS | Sotorasib | CodeBreaK 100 (I) | No | 32% | 6.3 | 12.5 | Diarrhea, nausea, elevated LFT’s, fatigue |
EGFR | Erlotinib | EURTAC (III) | chemotherapy | 64% | 9.7 | 22.9 | Fatigue, rash, diarrhea |
Gefitinib | NEJ002 (III) | Carboplatin/Paclitaxel | 74% | 10.8 | 27.2 | Rash, diarrhea | |
Afatinib | LUX-Lung 3 (III) | Cis/Pemetrexed | 56% | 11.1 | 28.2 | Rash, diarrhea, paronychia | |
Dacomitnib | ARCHER 1050 (III) | Gefitinib | 75% | 14.7 | 34.1 | Diarrhea, paronychia, rash | |
Osimertinib | FLAURA (III) | Erlotinib/Gefitinib | 80% | 18.9 | 38.6 | Rash, diarrhea, pneumonitis | |
ALK | Crizotinib | PROFILE 1014 (III) | Platinum/Pemetrexed | 74% | 10.9 | NR | Vision disorder, diarrhea, edema |
Certinib | ASCEND-4 (III) | Platinum/Pemetrexed | 73% | 16.6 | 51.3 | Diarrhea, nausea, vomiting | |
Alectinib | ALEXALEX (III) | Crizotinib | 83% | 25.7 | Immature | Elevated LFT’s, CPK elevation, anemia | |
Brigatinib | ALTA 1L (III) | Crizotinib | 74% | 24 | 47.6 | Elevated CPK and LFT’s | |
Ensartinibǂ | eXALT-3 (III) | Crizotinib | 75% | 25.8 | Immature | Rash, pruritis, edema | |
Lorlatinib | B7461006 (III) | Crizotinib | 76% | NR | Immature | Hyperlipidemia, edema, increased weight | |
MET Exon 14 skipping mutation | Capmatinib | GEOMETRY-mono-1 (II) | No | 41% (68%) * | 5.4 (12.4)* | NA/NA | Peripheral edema, nausea |
Tepotinib | VISION (II) | No | 46% | 8.5 | Immature | Peripheral edema | |
MET amplification | Capmatinib | GEOMETRY-mono-1 (II) | No | 29% (40%)* | 4.1 (4.2)* | NA/NA | Peripheral edema, nausea |
BRAF mutations | Dabrafenib + Trametinib | BRF113928 (II) | No | 64% (68%)* | 10.8 (10.2)* | 17.3 (18.2)* | Pyrexia, LFT elevation, HTN |
RET | Selparcatinib | LIBRETTO-001 (II) | No | 64% (85%) * | 16.5 (NR) | NR/NR | Dry mouth, diarrhea, HTN |
Pralsetinib | ARROW (II) | No | 61% (70%)* | 16.5 (13)* | NA/NA | LFT elevation, anemia | |
ROS1 | Crizotinib | PROFILE 1001 (I) | No | 72.4% | 19.3 | 51.4 | Vision disorder, nausea, edema |
Certinib | NCT01964157(II) | No | 62% (67%)* | 9.3 (19.3)* | 24 | Diarrhea, nausea, anorexia | |
Lorlatinib | NCT01970865 (I-II) | No | 41% (62%)* | 8.5 (21)* | NA | Dyslipidemia | |
Entrectinib | STARTRK-1, STARTRK-2, ALKA-372–001 (I-II) | No | 77% | 19 | NR | Weight gain, neutropenia | |
NTRK | Larotrectinib | LOXO-TRK-14001 (I-II) | No | 70% | NA | NA | LFT elevation, neutropenia, anemia |
Entrectinib | No | 70% | NA | NA | Dysgeusia, constipation, fatigue | ||
HER2 | T-DM1Ç‚ | NCT02675829 (II) | No | 44% | 5 | NA | Infusion reactions, thrombocytopenia |
T-DXdǂ | DESTINY-Lung01 (II) | No | 62% | 14 | NA | Neutropenia, anemia, ILD |