From: Tyrosine kinase inhibitors for solid tumors in the past 20 years (2001–2020)
Drug | Brand name | Manufacturer | Targets | Applications of diseases | Approved years or current phases of clinical trials |
---|---|---|---|---|---|
Gefitinib | Iressa | AstraZeneca | EGFR-sensitizing mutations | Inoperable or recurrent NSCLC | 2002§ |
1L metastatic EGFR-sensitizing mutant NSCLC | |||||
Erlotinib | Tarceva | OSI/Genentech | EGFR-sensitizing mutations | Locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen | 2004 [16] |
1L advanced EGFR-sensitizing mutant NSCLC | 2016 [16] | ||||
Combined with ramucirumab for 1L advanced EGFR-sensitizing mutant NSCLC | 2020 [191] | ||||
Icotinib | - | Shanghai Beta | EGFR-sensitizing mutations | Locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen | 2011& |
1L metastatic EGFR-sensitizing mutant NSCLC | |||||
Afatinib | Gilotrif | Boehringer Ingelheim | EGFR, HER2 | Metastatic EGFR-sensitizing mutant NSCLC | |
Advanced SqCC of Lung whose disease has progressed after treatment with platinum-based chemotherapy | 2016 [195] | ||||
1L metastatic NSCLC with non-resistant EGFR mutations (L861Q, G719X and S768I) | |||||
Dacomitinib | Vizimpro | Pfizer Inc | EGFR, HER2 | 1L metastatic EGFR-sensitizing mutant NSCLC | |
Osimertinib | Tagrisso | AstraZeneca | EGFR T790M, EGFR-sensitizing mutations | EGFR-T790M NSCLC | 2015 [25] |
1L metastatic EGFR-sensitizing mutant NSCLC | |||||
Metastatic or recurrent NSCLC with EGFR mutations other than the exon 19 deletion, L858R and T790M mutations, and exon 20 insertion | II [44] | ||||
Almonertinib | - | Jiangsu Hansoh | EGFR T790M, EGFR-sensitizing mutations | EGFR-T790M NSCLC | 2020& [32] |
1L locally advanced or metastatic pulmonary adenosquamous carcinoma | III (NCT04354961) | ||||
Investigational drugs | |||||
AST2818 (furmonertinib) | - | Shanghai Allist | EGFR T790M, EGFR-sensitizing mutations | Advanced EGFR-T790M NSCLC | |
1L locally advanced or metastatic EGFR-sensitizing mutant NSCLC | III (NCT03787992) | ||||
YH25448 (lazertinib) | - | Yuhan | EGFR T790M, EGFR-sensitizing mutations | Advanced EGFR-activating mutated NSCLC | I/II [35] |
1L locally advanced or metastatic EGFR-sensitizing mutant NSCLC | III (NCT04248829) | ||||
BPI-7711 | - | Shanghai Beta | EGFR T790M, EGFR-sensitizing mutations | EGFR-T790M advanced or recurrent NSCLC | I [36] IIb (NCT03812809) |
1L locally advanced or recurrent/metastatic EGFR-sensitizing mutant NSCLC | III (NCT03866499) | ||||
EGF816 (nazartinib) | - | Novartis | EGFR T790M, EGFR-sensitizing mutations | Advanced EGFR-mutant NSCLC | I [37] |
TAK-788 (mobocertinib) | - | Takeda | EGFR, HER2 | Metastatic NSCLC with EGFR exon 20 insertions whose disease has progressed on or after platinum-based chemotherapy | 2020/4/27 Breakthrough therapy recognition [45] |
1L locally advanced or metastatic NSCLC with EGFR exon 20 insertions | III (NCT04129502) | ||||
Poziotinib | - | Hanmi | EGFR, HER2, HER4 | ≥ 2L advanced NSCLC with EGFR exon 20 insertions | II [46] |
Tarloxotinib | - | Rain | EGFR, HER2, NRG fusion | 2L NSCLC with EGFR exon 20 insertion or HER2-activating mutation, solid tumors With NRG1/ERBB family gene fusions | [197] II (NCT03805841) |
TQB3804 | - | Jiangsu ChiaTai Tianqing | EGFR T790M, C797S, EGFR-sensitizing mutations | Osimertinib-resistant EGFR T790M/C797S mutant NSCLC | [42] I (NCT04128085) |
EAI045 | - | CSN | L858R, EGFR T790M, C797S | Combined with cetuximab for osimertinib-resistant EGFR T790M/C797S mutant NSCLC | [41] |