Table 3.
Properties of selected orally effective small-molecule EGFR family inhibitors [4].
| Name (Trade Name) | Targets | FDA-Approved Indications or Clinical Trial Study (Year) |
|---|---|---|
| Gefitinib | EGFR | NSCLC (2003) |
| Erlotinib | EGFR | NSCLC (2004) and pancreatic cancer (2005) |
| Afatinib | ErbB1/2/4 | NSCLC (2013) |
| Osimertinib | EGFR | NSCLC (2015) |
| Dacomitinib | Pan-HER | NSCLC (2018) |
| Lapatinib | EGFR/ErbB2 | Breast cancer (2007) |
| Neratinib | ErbB2/HER2 | Breast cancer (2015) |
| Avitinib | EGFR | Phase I and II clinical trials for NSCLC |
| Olmatinib | EGFR | Phase II clinical trials for NSCLC |
| Pelitinib | EGFR | Phase I clinical trials for NSCLC and colorectal cancer |
| Pyrotinib | EGFR, ErbB2 | Gastric, breast, NSCLC |
| Brigatinib | EGFR | NSCLC, leukemia |
| Vandetinib | EGFR | NSCLC, thyroid, liver, breast, CRC |
| Icotinib | EGFR | Brain, NSCLC, pancreas, head and neck |