Lorlatinib, a 3rd generation ALK TKI, is active against all known
crizotinib-resistance mutations, including ALK G1202R
Cellular ALK phosphorylation mean IC
50
(nM)
Mutation status (EML4-
ALK)
Lorlatinib
Crizotinib
Ceritinib
Alectinib
WT (v1)
1.3
3.6
80
90
NA
41
62
24
L1196M
21
43
843
1,154
NA
70
250
113
G1269A
15
80
605
689
NA
134
NA
112
G1202R
77
113
1,003
562
>1,000
549
>10,000
362
I1151Tins
38
50
1,268
902
1,066
296
1770
126
S1206Y
4.2
3.2
626
152
NA
60
NA
29
C1156Y
1.6
15
478
406
NA
177
NA
21
F1174L
0.2
165
NA
NA
