Future
Mutation
Location
ROS1 fusion
Active next generation inhibitor
G2032R
1
solvent front
CD74-ROS1
cabozantinib, lorlatinib, foretinib, brigatinib (in vitro)
4
cabozantinib, lorlatinib (patient)
D2033N
2
solvent front
CD74-ROS1
cabozantinib (in vitro, patient)
2
L2155S (cell line)3
n.r.
SLC34A2-ROS1
n.r.
L2026M
4
gate-keeper
CD74-ROS1
cabozantinib, brigatinib, certinib, foretinib, lorlatinib
4
S1986Y/F
5
double mutation
EZR-ROS1
lorlatinib (patient)
5
L1951
6
solvent front
cabozantinib (in vitro, pat.-derived cells)
6
ponatinib and crizotinib
1
Awad et al, NEJM 2013;
2
Drilon et al, 2015;
3
Song et al, 2015;
4
Chong et al, CCR 2016;
5
Facinetti et al., CCR 2016;
6
Katayama et al, CCR 2015; Dziadzluszko et al. JTO 2016