Table 5.

Correlation of FLT3 plasma inhibitory activity, in vitro cytotoxic response, and clinical response to lestaurtinib

Patient no.
FLT3 mutation status
Residual FLT3 phosphorylation (plasma inhibitory activity), %*
MTS assay IC50, nM†
Clinical response
1   WT   22.6   40   NR  
2   WT   20.1   26   NR  
10   WT   17.6   10   NR  
15   ITD   7.2   2   HR  
18   WT   0.0   > 150   NR  
19   PM   2.0   2   HR  
22   WT   3.7   > 150   NR  
24   WT   13.3   > 150   PD  
25   PM   1.8   > 150   PD  
29
 		 WT
 		 3.7
 		 > 150
 		 PD
 
Patient no.
FLT3 mutation status
Residual FLT3 phosphorylation (plasma inhibitory activity), %*
MTS assay IC50, nM†
Clinical response
1   WT   22.6   40   NR  
2   WT   20.1   26   NR  
10   WT   17.6   10   NR  
15   ITD   7.2   2   HR  
18   WT   0.0   > 150   NR  
19   PM   2.0   2   HR  
22   WT   3.7   > 150   NR  
24   WT   13.3   > 150   PD  
25   PM   1.8   > 150   PD  
29
 		 WT
 		 3.7
 		 > 150
 		 PD
 
*

Maximal trough FLT3 plasma inhibitory activity at a lestaurtinib dose of 60 mg twice daily as measured by ex vivo bioassay.

†

Lestaurtinib concentration resulting in 50% in vitro cell death following 72-hour incubation.

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