Table 4 Pharmacodynamic response for pFAK in pre- and post-dose tumour samples

From: A phase Ib dose-finding, pharmacokinetic study of the focal adhesion kinase inhibitor GSK2256098 and trametinib in patients with advanced solid tumours

Subject No.

Visit

pFAK (CU/μg)

Total FAK (CU/μg)

pFAK/FAK

% Change from baseline pFAK

% Change from baseline pFAK/FAK

GSK2256098 250 mg BID + trametinib 0.5mg QD

509

Baseline

112.070

1329.1

0.084

NA

NA

Day 15

13.950

585.9

0.024

–87.6

–71.763

510

Baseline

92.400

103.3

0.895

NA

NA

Day 15

60.860

245.7

0.248

–34.1

–72.310

202

Baseline

189.010

680.3

0.278

NA

NA

Day 22

30.960

762.1

0.041

–83.6

–85.378

206

Baseline

99.580

207.3

0.480

NA

NA

Day 22

50.110

59.2

0.846

–49.7

76.125

GSK2256098 500mg BID+trametinib 0.25mg QD

507

Baseline

72.750

1710.6

0.043

NA

NA

Day 15

NA

1107.3

NA

NA

NA

121

Baseline

41.680

183.7

0.227

NA

NA

Day 22

25.900

214.6

0.121

–37.9

–46.809

GSK2256098 500mg BID+trametinib 0.375mg QD

118

Baseline

79.470

268.6

0.296

NA

NA

Day 22

NA

NA

NA

NA

NA

GSK2256098 500mg BID + trametinib 0.5mg QD

200

Baseline

15.230

12.1

1.263

NA

NA

Day 22

24.600

62.0

0.397

−61.5

–68.586

  1. BID twice daily, FAK focal adhesion kinase, NA not available, pFAK phosphorylated FAK, QD once daily