Table 1.
Targeted therapies.
| Histology | Targeted Molecule | Reagents | FDA-Approved (April 2019) |
Note |
|---|---|---|---|---|
| NSCLC | EGFR (ADC 14%, SQC 9%) |
Gefitinib (First-generation) |
Yes | Selective and reversible TKI. |
| Erlotinib (First-generation) |
Yes | Selective and reversible TKI. | ||
| Afatinib (Second-generation) |
Yes | Irreversible ErbB family blocker. | ||
| Dacomitinib (Second-generation) |
Yes | Irreversible TKI. | ||
| Osimertinib (Third-generation) |
Yes | Irreversible and also active against the resistance mutation (T790M). | ||
| Poziotinib | No | Irreversible and active against exon20 mutation and HER2 mutation. | ||
| TAK-788 | No | Active against exon20 mutation and HER2 mutation. | ||
| TAS6417 | No | Selective against exon 20 insertion mutation. | ||
| ALK (ADC 5%) |
Crizotinib(First-generation) | Yes | Multi-targeted TKI. | |
| Alectinib (Second-generation) |
Yes | Highly selective inhibitor for ALK. | ||
| Ceritinib (Second-generation) |
Yes | Highly selective inhibitor for ALK. | ||
| Brigatinib (Second-generation) |
Yes | ALK/ROS1 inhibitor. | ||
| Lorlatinib (Third-generation) |
Yes | ALK/ROS1 inhibitor. | ||
| ROS1 (ADC 1%) |
Crizotinib | Yes | ||
| Lorlatinib | No | |||
| Entrectinib | No | Inhibits ROS1, TRK and ALK. | ||
| BRAF (ADC 7%, SQC 4%) |
Dabrafenib/trametinib | Yes | Reversible ATP-competitive kinase inhibitor. | |
| RET (ADC 1%) |
Cabozantinib | No | Multi-targeted TKI. | |
| Lenvatinib | No | Multi-targeted TKI. | ||
| Vandetanib | Yes | Multi-targeted TKI. | ||
| LOXO-292 | No | Selective RET inhibitor | ||
| MET (ADC 2–4%) |
Crizotinib | No | ||
| Capmatinib | No | Reversible MET inhibitor. | ||
| Tepotinib | No | Reversible MET inhibitor. | ||
| NTRK (<1%) |
Entrectinib | No | ||
| Larotrectinib | Yes | TRK inhibitor. | ||
| PD-1 | Nivolumab | Yes | IHC: 28-8 | |
| Pembrolizumab | Yes | IHC: 22C3 | ||
| PD-L1 | Atezolizumab | Yes | IHC: SP142 | |
| Duvalumab | Yes | IHC: SP263 | ||
| SCC | DLL3 (80%) |
Rovalpituzumab tesirine | No | Antibody against DLL3 conjugated with cytotoxic reagent. |
NSCLC, non-small cell lung cancer; SQC, Squamous cell carcinoma; EGFR, epidermal growth factor receptor; ADC, adenocarcinoma; TKI, tyrosine kinase inhibitor.