Table 4. Pharmacokinetic parameters for p28 on phase I.
| Level 1 | Level 2 | Level 3 | Level 4 | Level 5 | |
|---|---|---|---|---|---|
| n=2 | n=4 | n=6 | n=6 | n=7 | |
| Dose (mg kg−1) |
0.83 |
1.66 |
2.50 |
3.33 |
4.16 |
| Dose escalation (%) |
— |
100 |
51 |
33 |
25 |
|
Cmax (μg ml−1) |
1.01 |
6.99 |
7.68 |
9.8 |
13.7 |
|
Tmax (h) |
0.17 |
0.08 |
0.08 |
0.08 |
0.08 |
|
t1/2 (h) |
0.144 |
0.054 |
0.102 |
0.107 |
0.105 |
|
t1/2α (h) |
0.144 |
0.014 |
0.019 |
0.014 |
0.010 |
|
t1/2β (h) |
NA |
0.089 |
0.053 |
0.048 |
0.035 |
|
t1/2γ (h) |
NA |
NA |
1.61 |
2.16 |
4.12 |
| AUClast (h μg per ml) |
0.24 |
1.32 |
1.93 |
2.83 |
3.70 |
| Cl (ml kg−1 per hour) |
3430 |
1259 |
1294 |
1176 |
1124 |
| Vdss (ml kg−1) | 547 | 270 | 529 | 468 | 431 |
Abbreviation: n=number of patients; NA, not available.
Pharmacokinetics parameters (Cmax=p28 maximum concentration in serum, Tmax=time to Cmax, t1/2=terminal half-life of p28, t1/2α=rapid distribution half-life, t1/2β=slow distribution half-life, t1/2γ=elimination half-life, AUClast=area-under curve, Cl=total clearance and Vdss=volume distribution at steady state) were calculated from the p28 concentrations in serum vs post-injection time. The concentration at 0 min is defined as 0 ng ml−1 Bold values indicate minimally effective dose.