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. Author manuscript; available in PMC: 2017 Feb 10.
Published in final edited form as: J Control Release. 2016 Jun 4;235:306–318. doi: 10.1016/j.jconrel.2016.06.004

Table 4.

Comparison of pharmacokinetic parameters of dual-labeled (125I- and 111In-based) 1st generation conjugate and 2nd generation conjugates in mice.


1st generation
2nd generation
Conjugate
111In-P-EPI-125I
111In-2P-EPI-125I
125I-2P-EPI-111In
Component EPI(Tyr)-125I P(DTPA)111In EPI(Tyr)125I 2P(DTPA)111In EPI(DTPA)111In 2P(Tyr)125I
T1/2,α (h) 0.57 ± 0.07 0.50 ± 0.08 1.51 ± 0.20 1.58 ± 0.19 0.49 ± 0.13 0.47 ± 0.16
T1/2,β (h) 9.63 ± 11.47 9.20 ± 1.68 29.79 ± 1.62 31.52 ± 2.01 28.40 ± 2.03 31.11 ± 2.19
AUC (% ID h/mL) 260.72 ± 24.64 324.25 ± 36.98 1135.00 ± 43.81 1473.97 ± 65.83 1604.36 ± 95.44 1628.32 ± 97.28
CL (mL/h) 0.38 ± 0.03 0.30 ± 0.03 0.08 ± 0.003 0.06 ± 0.003 0.06 ± 0.003 0.06 ± 0.004
MRT (h) 13.01 ± 1.96 12.46 ± 2.25 41.85 ± 2.21 43.95 ± 2.73 40.71 ± 2.89 44.69 ± 13.15
Vss (mL) 4.99 ± 0.31 3.84 ± 0.29 3.68 ± 0.08 2.98 ± 0.08 2.53 ± 0.05 2.74 ± 0.06

T1/2,α = initial half-life; T1/2,β = terminal half-life; AUC = total area under the blood concentration versus time curve; %ID = percentage of injected dose; CL = total body clearance; MRT = mean residence time; Vss = steady-state volume of distribution. Data are presented as mean ± standard deviation (n = 5).