Table 2.

PK parameters (mean ± standard deviation) of imatinib mesylate in patients on day 1


Dose/day, mg/m2

No. of patients

tmax, h

Cmax, μg/mL

T1/2, h

AUC(0-24 h), μg.h/mL

AUC(0-∞), μg.h/mL

Vz/F, L

CI/F, L/h
260   6   3.5 ± 2.5   3.6 ± 2.0   8.9 ± 1.2   51.0 ± 34.9   60.6 ± 4.0   119 ± 83   8.9 ± 5.8  
340   8   3.7 ± 2.1   2.5 ± 0.9   9.2 ± 1.9   32.1 ± 13.0   39.6 ± 17.4   167 ± 84   12.8 ± 6.8  
440   4   5.0 ± 2.0   5.4 ± 4.3   12.8 ± 2.5   76.1 ± 54.8   103.3 ± 64.8   190 ± 213   9.3 ± 9.4  
570
 
4
 
2.9 ± 1.3
 
8.5 ± 9.2
 
14.8 ± 12.9
 
106.7 ± 113.6
 
150.7 ± 133.1
 
109 ± 88
 
5.6 ± 2.8
 

Dose/day, mg/m2

No. of patients

tmax, h

Cmax, μg/mL

T1/2, h

AUC(0-24 h), μg.h/mL

AUC(0-∞), μg.h/mL

Vz/F, L

CI/F, L/h
260   6   3.5 ± 2.5   3.6 ± 2.0   8.9 ± 1.2   51.0 ± 34.9   60.6 ± 4.0   119 ± 83   8.9 ± 5.8  
340   8   3.7 ± 2.1   2.5 ± 0.9   9.2 ± 1.9   32.1 ± 13.0   39.6 ± 17.4   167 ± 84   12.8 ± 6.8  
440   4   5.0 ± 2.0   5.4 ± 4.3   12.8 ± 2.5   76.1 ± 54.8   103.3 ± 64.8   190 ± 213   9.3 ± 9.4  
570
 
4
 
2.9 ± 1.3
 
8.5 ± 9.2
 
14.8 ± 12.9
 
106.7 ± 113.6
 
150.7 ± 133.1
 
109 ± 88
 
5.6 ± 2.8
 

PK indicates pharmacokinetics; mg/m2, milligram per square meter; No., number; tmax, h, time to reach Cmax (hours); Cmax, μg/mL, maximum mean plasma concentrations (microgram per milliliter); t1/2, h, half-life (hours); AUC(0-24h), μg.h/mL, area-under-the concentration-time curve, from time 0 to 24 hours (microgram times hour per milliliter); AUC(0-∞), μg.h/mL, area-under-the concentration-time curve, from time 0 to infinity (microgram times hour per milliliter); Vz/F, L, apparent volume of distribution during terminal phase after oral intake (liter); and CI/F, L/h, apparent total plasma clearance of drug after oral intake (liter per hour).

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