Summary of PK parameters of single-agent tislelizumab following single-administration and multiple-administration to patients with advanced tumors (PK analysis set)
| Dose level | N | Cycle 1 | Cycle 4 or cycle 5 | t1/2 (day)† | ||||||
| Cmax (μg/mL) | tmax (hour) | AUCtau* (μg/mL*day) | AUC0-inf (μg /mL*day) | N | Cmax (μg/mL) | tmax (hour) | AUCtau* (μg/mL*day) | |||
| Dose escalation (part 1) | ||||||||||
| 0.5 mg/kg every 2 weeks | 3 | 13.5±3.80 | 3.46±3.12 | 84.92±35.90 | 147.9±94.42 | 3 | 23.1±11.4 | 2.76±3.24 | 178.6±102.6 | 10.7±3.90 |
| 2 mg/kg every 2 weeks | 6 | 48.3±6.89 | 2.39±0.89 | 332.2±57.33 | 613.6±107.2 | 4 | 122±25.1 | 2.71±2.59 | 1094±388.2 | 12.9±1.20 |
| 5 mg/kg every 2 weeks | 6 | 147±50.8 | 2.48±0.73 | 811.8±239.5 | 1734±1265 | 3 | 205±59.9 | 1.40±0.63 | 1682±746.2 | 15.0±14.4 |
| 10 mg/kg every 2 weeks | 6 | 278±53.7 | 2.43±1.83 | 1916±458.5 | 3777±1020 | 1 | 476 | 0.75 | 3453 | 14.5±4.04 |
| Schedule expansion (part 2) | ||||||||||
| 2 mg/kg every 2 weeks | 18 | 47.7±10.6 | 1.85±0.69 | 350.9±87.94 | 723.7±291.0 | — | — | — | — | 14.1±4.42 |
| 2 mg/kg every 3 weeks | 18 | 56.8±12.8 | 1.57±0.65 | 512.1±122.2 | 933.1±497.6 | — | — | — | — | 17.1±8.14 |
| 5 mg/kg every 2 weeks | 17 | 133±31.4 | 1.73±0.40 | 875.9±240.7 | 1724±689.4 | 1 | 360 | 0.72 | 2679 | 13.9±4.88 |
| 5 mg/kg every 3 weeks | 20 | 130±29.7 | 4.95±15.4 | 1219±287.4 | 2270±790.4 | — | — | — | — | 19.6±7.63 |
| Fixed dose (part 3) | ||||||||||
| 200 mg every 3 weeks | 12 | 77.2±13.9 | 1.40±0.82 | 674.7±173.6 | 1172±393.8 | 5 | 90.9±16.9 | 0.78±0.19 | 977.8±440.3 | 16.8±5.50 |
*Tau was defined as 14 days for every 2 weeks and 21 days for every 3 weeks; cycle: 28 days per cycle for every 2 weeks; 21 days per cycle for every 3 weeks.
†Calculated from cycle 1 data.
AUC0-inf, area under curve from time zero to infinity; AUCtau, area under curve within the dosing interval; Cmax, observed maximum concentration; PK, pharmacokinetic; t½, terminal half-life following the first dose; tmax, time to observed maximum concentration.