From: FGFR-TKI resistance in cancer: current status and perspectives
TKI classification | TKI name | Mutation in kinase |
---|---|---|
Pan-FGFR inhibitors | TAS-120 | FGFR2(V564F) |
Multi-kinase inhibitors | TKI258 | FGFR1(N546K); FGFR2(V564I,M536I,M538I,I548V,L618M,E719G,E565,K462,N550) |
Ponatinib | FGFR1(N546K); FGFR2(V564I); FGFR4(V550 E/L) | |
E3810 | FGFR1(V561M) | |
Selective FGFR inhibitors | AZD4547 | FGFR1(V561M); FGFR2(I567, N568, V581, E584G, S587,K660E, K678M); FGFR3(V555M) |
BGJ398 | FGFR2(N550H/K, V564F, E565A, K660M, L618V, K641R) | |
PD173074 | FGFR1(V561M, N546H); FGFR3(V555M) | |
AZ12908010 | FGFR3(V555M) | |
Debio 1347 | FGFR2(N550K, K660M, L618V) | |
BLU-554 | FGFR4(V550M/L, C552) |