From: Targeted therapy in advanced non-small cell lung cancer: current advances and future trends
Drug name | Mechanism of action | Clinical trial (phase) | Study design | Disease |
---|---|---|---|---|
ERBB2(HER2) inhibitors | ||||
Ado-trastuzumab emtansine | HER2-targeted antibody–drug conjugate | NCT03784599 (1/2) | Combination with osimertinib | EGFR mutant advanced NSCLC |
Mobocertinib (TAk-788) | TKI targeting EGFR ex20ins mutations | NCT02716116 (1/2) | Combination with chemotherapy | EGFR and HER2 exon 20 insertion in advanced NSCLC |
Poziotinib | EGFR, HER2 and HER 4 inhibitors | NCT03066206 (2) | Monotherapy | EGFR exon 20 and HER2 exon 20 mutated advanced NSCLC |
trastuzumab deruxtecan | HER2-directed antibody–drug conjugate | NCT04644237 (2) | Monotherapy | HER2 mutated advanced NSCLC |
SHP2 inhibitors | ||||
JAB-3068 | SHP2 inhibitor | NCT03518554 (1) | Monotherapy | Advanced solid tumors including NSCLC |
TNO155 | SHP2 inhibitor | NCT03114319 (1) | Monotherapy and combination with Nazartinib | Advanced solid tumors including NSCLC |
Other miscellaneous target inhibitors | ||||
Aliseritib | Selective aurora A kinase inhibitor | NCT04085315 (1/2) | Combination with Osimertinib | EGFR mutant NSCLC progressing after first line TKI |
Anlotinib | VEGFR, FGFR, PDGFR, c-kit Inhibitor | NCT04165330 (1/2) | Combination with Nivolumab | Solid tumors including NSCLC |
Apatinib | VEGFR-2 Inhibitor | NCT03811054 (2) | Combination with EGFR-TKI | EGFR mutant NSCLC progressing after first line TKI |
APG-1252 | Small molecule inhibitor of BCL2 | NCT04001777 (1) | Monotherapy and combination with Osimertinib | EGFR mutant NSCLC |
BMS-986205 | IDO1 inhibitor | NCT02658890 (1/2) | Combination with Nivolumab and Ipilimumab | Advanced solid tumors including NSCLC |
Eprenetapopt (Apr-246) | Stabilizes p53 in normal, functional structure | NCT04383938 (1/2) | Combination with Pembrolizumab | Advanced solid tumors including NSCLC |
HBI-8000 | Histone deacetylase inhibitor | NCT02718066 (1/2) | Combination with Nivolumab | Advanced NSCLC |
Idelalisib | PI3K inhibitor | NCT03257722 (1/2) | Combination with Pembrolizumab | Advanced NSCLC with progression on first line therapy |
IRX4204 | Rexinoid, potent activator of RXRs | NCT02991651 (1) | Monotherapy and combination with Erlotinib | Advanced NSCLC with progression on two lines of therapy |
NC318 | IgG1 mAB specific for S15 | NCT03665285 (1/2) | Monotherapy | Advanced solid tumors including NSCLC |
Ningetinib (CT053PTSA) | Multi kinase inhibitor MET/HGFR | NCT03758287 (1/2) | Combination with Gefitinib | NSCLC with EGFR mutation and T790M negative |
Nintedanib | PDGFR, FGFR, VEGFR inhibitor | NCT03377023 (1/2) | Combination with Nivolumab and Ipilimumab | Advanced or metastatic NSCLC |
RGX-104 | Liver X receptor agonist | NCT02922764 (1) | Monotherapy or in combination with immunotherapy or chemotherapy | Advanced solid tumors including NSCLC |
Rucaparib | PARP inhibitor | NCT03845296 (2) | Monotherapy | Recurrent NSCLC |
Selinexor | Exportin 1 inhibitor | NCT03095612 (1/2) | Combination with docetaxel | Advanced KRAS mutant NSCLC with progression on first line therapy |
Selumetinib | MAPK inhibitor | NCT03392246 (2) | Combination with Osimertinib | Advanced EGFR mutant NSCLC |
Ramucirumab | VEGFR2 antagonist | NCT03909334 (2) | Combination with Osimertinib | EGFR mutant NSCLC |
Telaglenastat HCL | Glutaminase inhibitor | NCT03831932 (1/2) | Combination with Osimertinib | Advanced EGFR mutant NSCLC |
Varlilumab | Anti CD27 antibody | NCT04081688 (1) | Combination with Atezolizumab | Advanced NSCLC with progression on first line therapy |
Vorolanib | VEGFR/PDGFR inhibitor | NCT03583086 (1/2) | Combination with Nivolumab | Solid tumors including NSCLC |
ZN-c3 | WEE1 inhibitor | NCT04158336 (1/2) | Combination with Talazoparib or Pembrolizumab | Advanced solid tumors including NSCLC |
RBN-2397 | PARP7 inhibitor | NCT04053673 (1) | Monotherapy | Advanced solid tumors including NSCLC |