Table 2. Pharmacokinetic Parameters of Intravenously Administered 68Ga-labeled Anti-miR-15b RNA Oligonucleotides and Control Tracers in Healthy Adult Ratsa.
tracer | AUC0→∞ (min × g/mL) | ClT (mL/min × g) | kel (mL/min × g) | t1/2 (min) | Cmax (mL/g) | Tmax (s) |
---|---|---|---|---|---|---|
[68Ga]Ga-NOTA-anti-miR-15b | 120.0 ± 3.6 | 0.0083 ± 0.0003 | 0.0231 ± 0.0030 | 30.4 ± 3.9 | 23.6 ± 1.6 | 5.0 ± 0.0 |
[68Ga]Ga-NOTA(mod)-anti-miR-15b | 125.6 ± 14.9 | 0.0080 ± 0.0010 | 0.0209 ± 0.0031 | 33.7 ± 5.5 | 18.3 ± 6.8 | 25.0 ± 26.5 |
[68Ga]Ga-DOTA-anti-miR-15b | 229.7 ± 128.1 | 0.0057 ± 0.0032 | 0.0155 ± 0.0056 | 48.7 ± 15.2 | 16.8 ± 3.1 | 17.5 ± 12.6 |
[68Ga]Ga-NOTA-anti-miR-15b(scr) | 101.8 ± 5.6 | 0.0098 ± 0.0005 | 0.0257 ± 0.0021 | 27.1 ± 2.2 | 15.4 ± 1.7 | 10.0 ± 5.8 |
[68Ga]Ga-NOTA-anti-miR-15b(2SBS) | 68.6 ± 6.6 | 0.0147 ± 0.0015 | 0.0220 ± 0.0016 | 31.7 ± 2.2 | 8.6 ± 0.9 | 79.5 ± 17.5 |
[68Ga]Ga-NOTA-anti-miR-34 | 92.3 ± 21.1 | 0.0112 ± 0.0024 | 0.0201 ± 0.0024 | 34.9 ± 4.5 | 14.4 ± 5.8 | 30.5 ± 6.0 |
[68Ga]Ga-NOTA-T6 | 100.2 ± 13.7 | 0.0101 ± 0.0013 | 0.0329 ± 0.0066 | 21.7 ± 4.4 | 17.3 ± 3.9 | 7.5 ± 5.0 |
[68Ga]Ga-NOTA | 100.0 ± 15.7 | 0.0102 ± 0.0017 | 0.0323 ± 0.0083 | 22.4 ± 5.3 | 18.6 ± 2.4 | 12.5 ± 5.0 |
AUC0→∞ = area under the curve; ClT = total clearance; kel = elimination rate constant; t1/2 = plasma half-life; Cmax = maximum concentration; Tmax = time of maximum concentration.