TABLE 1

Estimated mean PK parameters after SC and IV administration

Due to the sparse sampling paradigm, a composite concentration-time curve was used to calculate the PK parameters. There were samples from 3–4 animals per time point.

[14C]BIL[125I]BIL[14C]20-kDa PEG
RouteSCIVSCIVSCIV
Dose2 mg/kg (77 nmol/kg)0.5 mg/kg (19.4 nmol/kg)2 mg/kg (77 nmol/kg)0.5 mg/kg (19.4 nmol/kg)10 mg/kg (500 nmol/kg)
Analyte14CBILa14CBILa125IBILa125IBILa14C14C
C0 or Cmax (nM or nM eq)102955506419341.63715714151915
Tmax (h)11N.A.N.A.123N.A.N.A.10.5N.A.
t1/2 (h)b1976191545353120202165
AUC0–t (nM eq⋅h or nM⋅h)45309301680809337010301740110024,70036,000
CL (l/h per kg)N.A.N.A.0.009780.0239N.A.N.A.0.01110.0176N.A.0.0127
Vd (l/kg)N.A.N.A.1.430.030N.A.N.A.0.1760.073N.A.1.14
Bioavailability (%)7529N.A.N.A4823N.A.N.A.78N.A.
  • eq, equivalents of [14C]BIL or [125I]BIL, representing any molecules containing the radiolabeled 14C and 125I, although the exact identity is unknown; IV, intravenous; N.A., not applicable; SC, subcutaneous.

  • a Represents immunoreactive BIL.

  • b The last plasma sampling time was <2 t1/2s; therefore, the estimated mean elimination t1/2 should be interpreted with caution.