TABLE 2.
Descriptive and statistical summary of plasma pharmacokinetics of clesacostat (PF‐05221304, Cohort 1) or ervogastat (PF‐06865571, Cohort 2) alone on Day 7 (Reference) or co‐administered on Day 14 (Test).
| Parameter | Cohort 1 | Cohort 2 | ||||
|---|---|---|---|---|---|---|
| Clesacostat 15 mg b.i.d., Day 7 | Clesacostat 15 mg + ervogastat 300 mg b.i.d., Day 14 | Ratio (%) (90% CI) a | Ervogastat 300 mg b.i.d., Day 7 | Ervogastat 300 mg + clesacostat 15 mg b.i.d., Day 14 | Ratio (%) (90% CI) a | |
| Participants (n) | 7 | 6 | NA | 9 | 9 | NA |
| T max, h | 4.00 (2.00–6.00) | 2.00 (1.50–4.00) | NA | 2.00 (1.00–4.00) | 2.00 (1.00–2.00) | NA |
| CL/F, L/h | 1.24 (26) | 1.58 (23) | NA | 34.41 (19) | 31.76 (34) | NA |
| PTR, h | 1.92 | 2.41 | NA | 94.35 | 149.7 | NA |
| AUCtau, ng*h/mL | 12,140 (26) | 9477 (23) | 80.51 (73.59, 88.09) | 8715 (19) | 9450 (34) | 108.43 (97.08, 121.10) |
| C max, ng/mL | 1337 (25) | 1128 (20) | 88.46 (79.77, 98.10) | 2386 (10) | 2580 (21) | 108.14 (97.91, 119.43) |
Note: Data are geometric mean (%CV) for all parameters except median (range) for T max.
Abbreviations: %CV, coefficient of variability; AUCtau, area under the plasma drug concentration–time curve during the dosing interval; b.i.d., twice daily; CI, confidence interval; CL/F, apparent clearance; C max, maximum plasma drug concentration; h, hour; NA, not applicable; PTR, peak‐to‐trough ratio; T max, time to maximum plasma drug concentration.
Geometric mean ratio (Day 14 [Test]/Day 7 [Reference]); ratios and 90% CIs are expressed as percentages.