Table 6.

Inhibition of FLT3 phosphorylation versus tandutinib plasma concentration in assessable patients with FLT3-ITD mutations by dose level and time point


Patient no., treatment

Tandutinib plasma concentration, ng/mL

FLT3 inhibition
52   
    300 mg twice daily    
        Day 1, predose   BLQ   NA  
        Day 1, 2 h   2.7   No  
        Day 1, 8 h   30.7   Yes  
        Day 3   13.5   No  
        Day 10   345.8   Yes  
73   
    525 mg twice daily    
        Day 1, predose   BLQ   NA  
        Day 1, 2 h   218.6   Yes  
        Day 1, 8 h   177.1   Yes  
        Day 3   128.3   Yes  
74   
    525 mg twice daily    
        Day 1, predose   BLQ   NA  
        Day 1, 2 h   139   Yes  
        Day 1, 8 h   25.2   No  
Day 3
 
87.3
 
No
 

Patient no., treatment

Tandutinib plasma concentration, ng/mL

FLT3 inhibition
52   
    300 mg twice daily    
        Day 1, predose   BLQ   NA  
        Day 1, 2 h   2.7   No  
        Day 1, 8 h   30.7   Yes  
        Day 3   13.5   No  
        Day 10   345.8   Yes  
73   
    525 mg twice daily    
        Day 1, predose   BLQ   NA  
        Day 1, 2 h   218.6   Yes  
        Day 1, 8 h   177.1   Yes  
        Day 3   128.3   Yes  
74   
    525 mg twice daily    
        Day 1, predose   BLQ   NA  
        Day 1, 2 h   139   Yes  
        Day 1, 8 h   25.2   No  
Day 3
 
87.3
 
No
 

BLQ indicates below limit of quantitation; NA, not applicable.

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