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Table 3 Geometric mean (% coefficient of variation) of telatinib and BAY 60-8246 pharmacokinetic parameters on day 14 of cycle 1

From: Phase I study of telatinib (BAY 57-9352): analysis of safety, pharmacokinetics, tumor efficacy, and biomarkers in patients with colorectal cancer

Parameter

Telatinib dose

 

600 mg bid

(n = 6)

900 mg bid

(n = 27)

1200 mg bid (n = 2)

1500 mg bid (n = 4)

(n = 6)

Telatinib

Cmax (mg/l)

0.825 (93%)

0.899 (91%) b

1.467 (33%)

Tmax (h) a

2.3 [1.1 - 4]

2.6 [0.5 - 8] b

2.5 [0.67 - 4.1]

AUC(0-tn) (mg·h/l)

5.779 (71%)

5.547 (80%) b

9.244 (31%)

AUC(0-12) (mg·h/l)

5.779 (71%)

5.761 (82%) b

9.800 (33%)

Half-life (h)

8.2 (47%)

6.8 (47%) c

8.1 (71%)

BAY 60-8246

Cmax (mg/l)

0.101 (203%)

0.095 (120%)

0.207 (85%)

Tmax (h) a

2.3 [0.6 - 4]

3.2 [0.5 - 12.2]

2.6 [0.5 - 4.1]

AUC(0-tn) (mg·h/l)

0.826 (181%)

0.634 (101%)

1.499 (93%)

AUC(0-12) (mg·h/l)

0.826 (182%)

0.636 (101%) d

1.595 (92%)

Half-life (h)

6.2 (14%) d

6.5 (48%) e

7.8 (38%) b

  1. - AUC(0-12) - area under the plasma concentration versus time curve from time 0 to 12 hours
  2. - AUC(0-tn) - area under the plasma concentration versus time curve from time 0 to last data point
  3. - Bid - bis in die, twice daily
  4. - Cmax - maximum plasma concentration
  5. - Tmax - time to reach maximum plasma concentration.
  6. a Median [range]
  7. b Sample size reduced by 1
  8. c Sample size reduced by 3
  9. d Sample size reduced by 2
  10. e Sample size reduced by 5.
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