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Table 4 Summary of afatinib pharmacokinetic parameters after multiple oral administrations of afatinib 40 and 30 mg, with letrozole 2.5 mg

From: A phase II study of afatinib, an irreversible ErbB family blocker, added to letrozole in patients with estrogen receptor-positive hormone-refractory metastatic breast cancer progressing on letrozole

Pharmacokinetic parameter (unit)

Afatinib 40 mg

Afatinib 30 mg

N

Geometric mean

Geometric CV (%)

N

Geometric mean

Geometric CV (%)

AUCtau,ss (ng*h/mL)

4

660

41.3

5

579

62.8

Cmax,ss (ng/mL)

4

43.8

42.0

5

33.9

79.4

Cpre,ss, 57 (ng/mL)

5

21.4

42.3

8

15.8

42.1

Cpre,ss, 85 (ng/mL)

4

16.9

55.7

5

17.3

46.5

tmax,ss (h)a

4

2

2–4

5

4.00

0.91–7.67

  1. AUC tau,ss area under the plasma concentration–time curve at steady state over the dosing interval, C max,ss maximum plasma concentration at steady state, C pre,ss, 57 , C pre,ss, 85 pre-dose plasma concentration on day 1 of cycles 3 and 4, respectively, CV coefficient of variation, t max,ss time to maximum plasma concentration at steady state
  2. aMedian and range