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Table 3 PK parameters of conteltinib (CT-707) in different dose cohorts

From: Conteltinib (CT-707) in patients with advanced ALK-positive non-small cell lung cancer: a multicenter, open-label, first-in-human phase 1 study

PK parameter

AUCINF_obs (ng·h/mL)

AUClast (ng·h/mL)

Cmax (ng/mL)

T1/2 (h)

Tmax (h)

MRTlast (h)

Single dose in PK lead-in phase of dose-escalation phasea

Mean

SD

Mean

SD

Mean

SD

Mean

SD

Mean

SD

Mean

SD

 50 mg (n=2)

205.7

0.6

125.3

15.2

16.3

2.3

22.5

5.9

2.0

1.4

8.1

0.1

 100 mg (n=3)

1047.4

981.3

732.0

797.6

69.0

85.8

90.2

63.2

2.8

2.0

30.3

15.8

 200 mg (n=3)

3108.0

1890.6

2553.9

1616.5

139.6

123.6

83.5

6.3

2.7

0.6

47.4

4.4

 300 mg (n=3)

5109.5

1605.6

4335.8

1818.5

246.3

90.1

78.5

38.5

2.5

1.8

46.2

3.6

 450 mg (n=4)

11475.2

8250.4

9875.0

7169.1

544.3

385.3

78.7

10.3

3.3

2.2

40.5

1.4

 600 mg (n=7)

11150.6

6793.3

9644.2

6243.8

452.1

284.6

78.7

13.5

3.9

1.7

43.3

3.7

 800 mg (n=3)

11164.6

7787.7

9823.2

7130.1

421.3

259.6

77.2

9.3

3.7

0.6

42.0

4.0

Single-dose in cycle 1 day 1 of dose-expansion phaseb

Mean

SD

Mean

SD

Mean

SD

Mean

SD

Mean

SD

Mean

SD

 100 mg (n=5)

1309.9

552.3

736.7

423.4

85.5

51.0

26.7

16.7

2.7

1.5

8.9

0.9

 450 mg (n=10)

6339.7

4927.2

3055.1

849.2

327.8

122.0

23.4

19.3

2.3

1.0

9.3

1.2

 600 mg (n=10)

7153.8

4940.6

4608.9

3267.3

472.4

345.8

16.7

4.0

4.6

2.3

9.8

1.4

Cycle 1 day 28 of dose-escalation phasec

Mean

SD

Mean

SD

Mean

SD

Mean

SD

Mean

SD

Mean

SD

 50 mg (n=2)

16704.7

21404.0

683.0

205.5

42.7

4.1

352.2

446.0

1.5

0.7

11.1

0.5

 100 mg (n=3)

6110.5

5079.7

1479.9

194.0

105.6

29.9

61.1

55.7

2.7

0.6

10.6

0.1

 200 mg (n=3)

12399.1

8484.5

3573.7

1587.8

259.3

164.3

42.2

20.2

3.0

0.0

11.2

1.1

 300 mg (n=3)

19006.6

11836.7

4859.1

399.7

282.3

55.9

50.9

36.8

3.0

1.0

11.3

0.7

 450 mg (n=3)

34382.8

28835.3

8046.3

3449.6

474.0

250.9

48.6

38.2

4.3

1.5

11.6

0.6

 600 mg (n=7)

53825.9

63563.9

14023.9

8628.0

984.7

717.0

45.0

32.1

2.5

1.4

10.8

0.5

 800 mg (n=2)

27223.0

33065.7

5498.7

5665.9

304.9

302.8

52.7

30.7

3.5

0.7

11.6

0.1

Cycle 1 day 28 of dose-expansion phased

Mean

SD

Mean

SD

Mean

SD

Mean

SD

Mean

SD

Mean

SD

 100 mg (n=5)

6460.4

2881.3

1709.5

289.1

123.4

23.9

53.2

32.4

2.0

0.7

10.7

0.5

 450 mg (n=10)

15683.9

9391.2

7040.6

2456.1

491.0

176.8

26.3

11.0

3.0

1.4

10.5

0.6

 600 mg (n=10)

32508.7

20202.8

11908.9

7300.7

772.1

532.9

37.1

19.4

3.3

1.2

10.9

0.6

  1. Abbreviations: PK pharmacokinetic, AUC area under the concentration-time curve, AUCINF_obs area under the concentration-time curve from the time of dosing extrapolated to infinity, based on the last observed concentration, AUClast area under the concentration-time curve from the time of dosing to the time of the last observation, Cmax maximum concentration, Tmax time to maximum concentration, T1/2 elimination half-life, MRTlast mean residence time from the time of dosing to the time of the last measurable concentration, SD standard deviation, QD quaque die, BID bis in die
  2. aSingle-dose of conteltinib PK assessed in the PK lead-in phase of the dose-escalation phase at pre-dose and 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h, 144 h, and 168 h post-dose
  3. bSingle-dose of conteltinib PK assessed in cycle 1 day 1 of the dose-expansion phase at pre-dose and 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose
  4. cConteltinib PK assessed in cycle 1 day 28 of the dose-escalation phase at pre-dose and 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose
  5. dConteltinib PK assessed in cycle 1 day 28 of the dose-expansion phase at pre-dose and 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose
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