Table 1.

Pharmacokinetic characterization of anti-GFRA1 ADCs in rats and cynomolgus monkeys

RatCynomolgus monkey
hu-6D3.v5hu-7C9hu-6D3.v5hu-7C9
Parameters0.5 mg/kg5 mg/kg0.5 mg/kg5 mg/kg0.3 mg/kg3 mg/kg0.3 mg/kg3 mg/kg
Cmax (mg/mL)11.8 ± 1.5107 ± 8.411.8 ± 0.7132 ± 13.09.30 ± 1.193.9 ± 6.98.32 ± 0.7104 ± 4.1
AUCinf (day ·mg/mL)79.8 ± 13.4778 ± 12720.9 ± 4.1445 ± 10813.9 ± 3.06240 ± 46.18.08 ± 0.8235 ± 26.3
CL (mL/day/kg)6.4 ± 1.26.5 ± 1.224.7 ± 5.311.7 ± 2.622.4 ± 5.112.8 ± 2.137.4 ± 3.712.9 ± 1.5
Vss (mL/kg)102 ± 7.6101 ± 26.483.0 ± 5.371.8 ± 6.7107 ± 30.558.4 ± 4.7629.2 ± 1.136.3 ± 2.1
t1/2 (day)11.6 ± 2.411.2 ± 5.3NRNRNRNRNRNR
  • Abbreviations: AUCinf, area under the serum concentration-time curve extrapolated to infinity; CL, clearance; Cmax, observed maximum serum concentration; NR, not reported, due to a nonlinear pharmacokinetic profile; t1/2, half-life of the elimination phase; Vss, volume of distribution at steady state.