Table 2.
EGFR and HER2 inhibitors, target and main clinical indications or trials.
| Name (Code) Trade Name | Targets | Approved Clinical Indications or Clinical Trial Study |
|---|---|---|
| Gefitinib (ZD1389) Iressa | EGFR | NSCLC |
| Erlotinib (OSI-774) Tarceva | EGFR | NSCLC |
| Afatinib (BIBW2992) Tovok | Erb1/2/4 | NSCLC |
| Osimertinib (AZD-9291) Tagrisso | EGFR | NSCLC |
| Dacomitinib (PF299804) Visimpro | Pan-HER | NSCLC |
| Saracatinib (AZD0530) | EGFR, Src | Phase II trial (NCT00752206, NCT00607594, NCT01267266) for osteosarcoma, gastric, prostate and other solid tumors |
| Lapatinib (GW572016) Tykerb | EGFR/HER2 | Breast cancer |
| Neratinib (HKI-272) Nerlynx | HER2 | Breast cancer |
| Icotinib | EGFR | NSCLC (China) |
| Poziotinib (HM781-36B) | EGFR/HER2/HER4 | Phase II trial (NCT02979821) for NSCLC |
| Tarloxotinib (TH4000) | EGFR/HER2 | Phase II trial (NCT03805841) for NSCLC and solid tumors harboring ERBB/NRG1 gene fusions |
| Lazertinib (YH25448) | EGFR | Phase III (NCT04248829) trial for NSCLC |
| AZD3759 | EGFR | Phase II/III (NCT03653546) trial for NSCLC. |
| Pyrotinib (SHR-1258) | EGFR/HER2 | Phase I trial (NCT02500199) for HER2 positive solid tumors. |
| Avitinib (AC0010MA) | EGFR | Phase I/II (NCT02330367) clinical trial for NSCLC |
| Sapitinib (AZD8931) | EGFR/HER2/HER3 | Phase I/II trial (NCT01862003) for colorectal cancer. |
| Rociletinib (CO-1686) | EGFR | Phase III (NCT02322281) for NSCLC |
| TAS6417 | EGFR/HER2/HER3 | Phase I/IIa trial (NCT04036682) for NSCLC |
| Varlitinib (ASLAN001) | EGFR/HER2/HER4 | Phase II/III (NCT03093870, NCT03130790) for billiard tract cancer, gastric cancer and hepatocarcinoma (Phase Ib; NCT03499626) |
| Olmutinib (HM61713) | EGFR | Phase Ib (NCT04510415) and phase II (NCT03228277) clinical trials for NSCLC |
| Nazartinib (EGF816) | EGFR | Phase I/II (NCT02108964) clinical trial for NSCLC |
| Mavelertinib (PF-06747775) | EGFR | Phase II trial (NCT02349633) for NSCLC |
| Naquonitinib (ASP8273) | EGFR | Phase I (NCT02113813) trial for NSCLC |
| Ibrutinib (PCI-32765) Imbruvica | EGFR, BTK | Phase I/II (NCT02321540) trial for NSCLC, MCL, CLL. |
| EAI001 | EGFR | Preclinical |
| EAI045 | EGFR | Preclinical |