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Table 5 Associations between polymorphisms and AUC0–48 of gefitinib or O-desmethyl gefitinib

From: Pharmacokinetics of gefitinib in elderly patients with EGFR-mutated advanced non-small cell lung cancer: a prospective study

Polymorphism

Genotype

N

Gefitinib AUC0–48 (µM h)a

Pb

O-desmethyl gefitinib AUC0–48 (µM h)a

Pb

CYP3A5*3

*1/*1

1

12.1

NAc

1.94

NAc

*1/*3

6

8.62 ± 3.5

 

12.9 ± 12

 

*3/*3

11

9.73 ± 3.6

 

10.0 ± 16

 

CYP2D6*5 and *10

*1/*1

4

5.52 ± 0.61

0.00580

28.2 ± 23

0.0179

*1/*5 or *1/*10

9

9.53 ± 3.0

 

6.81 ± 4.8

 

5/*10 or *10/*10

5

12.6 ± 2.2

 

3.23 ± 2.2

 

ABCG2421C > A

C/C

8

8.49 ± 3.5

0.0692

16.5 ± 20

0.459

C/A

7

8.69 ± 2.6

 

5.14 ± 3.7

 

A/A

3

14.0 ± 1.7

 

7.43 ± 7.5

 

ABCB11236C > T

C/C

4

12.8 ± 2.6

0.0724

7.36 ± 5.9

0.670

C/T

11

7.99 ± 2.9

 

13.4 ± 18

 

T/T

3

10.6 ± 3.7

 

4.57 ± 1.6

 

ABCB12677G > T/A

G/G

1

15.3

NAc

4.36

NAc

G/T

7

8.59 ± 3.9

 

20 ± 20

 

G/A

1

7.55

 

6.79

 

T/T

6

9.33 ± 2.8

 

20 ± 20

 

T/A

3

10.6 ± 3.7

 

4.57 ± 1.6

 

ABCB1 3435C > T

C/C

1

12.2

NAc

0.00

NAc

C/T

7

9.42 ± 4.2

 

20.0 ± 20

 

T/T

10

9.27 ± 3.2

 

5.03 ± 2.9

 

ABCB1 diplotype

Any/Any

6

11.8 ± 2.9

0.0492

6.04 ± 5.4

0.640

TTT/Any

12

8.33 ± 3.2

 

12.8 ± 17

 

OATP1B1388A > G

A/A

3

8.89 ± 3.1

0.474

5.10 ± 3

0.319

A/G

7

10.8 ± 2.9

 

11.2 ± 20

 

G/G

8

8.55 ± 4.0

 

12.1 ± 11

 

OATP1B1521T > C

T/T

13

9.88 ± 3.7

NAc

8.87 ± 9.3

NAc

T/C

4

8.7 ± 3.3

 

17 ± 27

 

C/C

1

7.55

 

6.79

 

OATP1B1diplotype

*1a/*1a, *1a/*1b, or *1b/*1b

13

9.88 ± 3.7

NAc

8.87 ± 9.3

NAc

*1a/*15 or *1b/*15

4

8.70 ± 3.3

 

17.0 ± 27

 

15/*15

1

7.55

 

6.79

 
  1. N = 18
  2. AUC area under the plasma concentration–time curve from time 0 to 48 h
  3. aMean ± SD
  4. bWilcoxon or Kruskal–Wallis test
  5. cNot analyzed because of the small number of patients in a genotype (N < 3)