Summary of varied generation ALK-TKI drugs recommended for NSCLC treatment
| Drug | Month & year of approval | Circumstantial efficacy screened | Generation stage |
|---|---|---|---|
| Crizotinib | August 2011 | ALK metastatic tumors | First |
| Certinib | April 2014 | ALK metastatic tumors | Second |
| Alectinib | December 2015 | Progressed ALK metastatic tumors, exhibiting resistance to crizotinib | Second |
| November 2017 | ALK metastasis | ||
| Brigatinib | April 2017 | Progressed ALK metastatic tumors, displaying resistance to crizotinib | Second |
| Ensartinib | Could not be authentically traced | Exhibited 52% ORR in a phase II trial. A phase III trial found ensartinib better than crizotinib in systemic and intracranial diseases. ALK resistance were majorly due to G1269A, G1202R & E1210K mutations | Second |
| Lorlatinib | November 2018 | ALK metastatic tumors treated with alectinib or certinib or crizotinib & at least one more ALK inhibitor | Third |
| TPX-0131 | Currently being investigated | A compact macrocyclic inhibitor that fits well entirely in the ATP binding pocket. Efficient against compound mutations G1202R + L1198F, G1202R + L1196M, L1196M + L1198F, and G1202R + C1156F | Fourth |
| NVL-655 | Currently being investigated | A brain penetrant small molecule inhibitor with significant potential against solvent drug resistance mutations, viz. G1202R, G1202R + L1196M and G1202R + G12269A | Fourth |