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Table 4 Major PK parameters of BPI-9016M, M1 and M2-2 after treatment with multiple doses of BPI-9016M for 28 days in Part A

From: Safety, efficacy and pharmacokinetics of BPI-9016M in c-MET overexpression or MET exon 14 skipping mutation patients with locally advanced or metastatic non-small-cell lung cancer: a phase Ib study

PK Parameters

300 mg QD (n = 7)

Mean (SD)

450 mg QD (n = 7)

Mean (SD)

600 mg QD (n = 7)

Mean (SD)

AUCtau (h × ng/mL)

 BPI-9016M

7680.0 (4120.0)

11,000.0 (5970.0)

10,100.0 (5350.0)

 M1

48,200.0 (20,500.0)

60,200.0 (25,100.0)

73,400.0 (19,600.0)

 M2-2

32,400.0 (12,200.0)

38,200.0 (13,500.0)

46,300.0 (10,600.0)

Cmax,ss (ng/mL)

 BPI-9016M

794.0 (370.0)

932.0 (480.0)

788.0 (394.0)

 M1

2510.0 (969.0)

3150.0 (1310.0)

3880.0 (863.0)

 M2-2

2300.0 (940.0)

2610.0 (972.0)

2730.0 (344.0)

Cmin,ss (ng/mL)

 BPI-9016M

104.0 (49.0)

168.0 (127.0)

157.0 (89.6)

 M1

1770.0 (910.0)

2100.0 (818.0)

2540.0 (601.0)

 M2-2

1030.0 (342.0)

1150.0 (373.0)

1450.0 (269.0)

Tmax,ss (h)

 BPI-9016M

3.9 (2.0)

4.0 (1.0)

3.9 (2.0)

 M1

0.0 (0.0)

1.1 (0.0)

1.0 (0.0)

 M2-2

0.0 (0.0)

0.0 (0.0)

1.0 (0.0)

T1/2 (h)

 BPI-9016M

11.2 (2.8)

11.8 (4.8)

12.7 (4.8)

 M1

19.8 (3.6)

21.7 (3.0)

21.8 (2.9)

 M2-2

21.3 (NE)

NE (NE)

NE (NE)

Ctrough (ng/mL)

 BPI-9016M

113.5 (55.0)

184.1 (131.2)

203.9 (99.2)

 M1

2294.0 (965.6)

3002.9 (1370.5)

3372.9 (615.1)

 M2-2

2112.4 (952.7)

2564.3 (966.6)

2544.3 (432.4)

CLss/F (L/h)

 BPI-9016M

50.4 (25.6)

57.6 (39.5)

83.2 (58.9)

Vz,ss/F (L)

 BPI-9016M

781.0 (357.0)

1050.0 (974.0)

1780.0 (2080.0)

MP ratio

 M1

7.0 (2.1)

6.0 (1.4)

9.1 (4.7)

 M2-2

4.9 (2.2)

4.1 (2.0)

5.7 (3.2)

  1. Data are mean (SD), unless otherwise stated. One patient in the 300 mg QD cohort had protocol violation and no exact administration time of BPI-9016M. One patient in the 600 mg QD cohort discontinued over two-week treatment of BPI-9016M due to the poor compliance. The sparse plasma PK data from other 11 patients were analyzed based on population PK analysis without PK modeling, therefore 21 patients were included in PKAS
  2. PK pharmacokinetics, AUC area under the concentration-time curve, AUCtau AUC over a dosing interval, Cmax,ss maximum plasma concentration at steady state, Cmin,ss minimum plasma concentration at steady state, Tmax,ss time to maximum plasma concentration at steady state, T1/2 terminal time of half-life, Ctrough trough concentration, CLss/F overall body clearance at steady state for extravascular dosage, Vz,ss/F total volume of drug distribution at steady state according to the terminal phase, MP ratio ratio of metabolites to parent drug calculated based on AUCtau, QD quaque die, SD standard deviation, NE not evaluable, PKAS pharmacokinetics analysis set
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BMC Cancer

ISSN: 1471-2407

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