Table 2.
Plasma nicotine and receptor occupancy before and after treatment with 3′-AmNic-rEPA.
| # | Ab (μg/mL) | IV nic (mg) | % Occupancy | AUC t0–∞ (ng. min/ml) | Cmax (ng/mL) | Tmax (min) | Cl (mL/min) | VD (L) | Half life (min) | |||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| T1 | T2 | T1 | T2 | T1 | T2 | T1 | T2 | T1 | T2 | T1 | T2 | T1 | T2 | |||
| 1 | 59.8 | 1.66 | 56.9 | 56.2 | 920 | 1994 | 9.7 | 9.3 | 20.0 | 10.0 | 1804 | 833 | 233511 | 154433 | 90 | 129 |
| 2* | 45.3 | 1.90 | 54.4 | 30.3 | 742 | 1165 | 4.8 | 7.5 | 30.0 | 30.0 | 2560 | 1630 | 351398 | 213721 | 95 | 91 |
| 3 | 85.4 | 2.76 | 65.5 | 51.5 | 2496 | 2979 | 9.1 | 22.3 | 30.0 | 10.0 | 1106 | 926 | 263278 | 141204 | 165 | 106 |
| 4 | 64.6 | 1.86 | 56.6 | 49.7 | 1514 | 2413 | 15.5 | 46.1 | 10.0 | 10.0 | 1228 | 771 | 78755 | 132457 | 44 | 119 |
| 5 | 75.9 | 1.46 | 46.4 | 47.6 | 1421 | 2622 | 10.7 | 20.1 | 10.0 | 20.0 | 1027 | 557 | 172453 | 75759 | 116 | 94 |
| 6 | 127.9 | 1.75 | 66.6 | 59.6 | 2097 | 3994 | 10.0 | 34.2 | 30.0 | 10.0 | 835 | 438 | 295992 | 159289 | 246 | 252 |
| 7 | 64.6 | 1.35 | 39.1 | 31.5 | 4001 | 15718 | 8.3 | 28.4 | 20.0 | 30.0 | 337 | 86 | 161987 | 46904 | 333 | 378 |
| 8 | 41.7 | 1.62 | 60.3 | 62.7 | 1489 | 2083 | 8.0 | 8.5 | 5.0 | 10.0 | 1088 | 778 | 261298 | 177543 | 166 | 158 |
| 9 | 65.0 | 1.70 | 59.5 | 49.7 | 1205 | 1524 | 11.8 | 15.0 | 5.0 | 5.0 | 1411 | 1115 | 151182 | 154616 | 74 | 96 |
| 10** | NA | 1.74 | 52.8 | 49.1 | ||||||||||||
| 11 | 129.2 | 1.39 | 48.0 | 56.2 | 1337 | 2625 | 7.6 | 20.1 | 10.0 | 20.0 | 1040 | 530 | 216448 | 72835 | 144 | 95 |
| Mean | 1.9 | 54.9 | 49.1 | 1722 | 3712 | 9.6 | 21.2 | 17.0 | 15.5 | 1244 | 766 | 218630 | 132876 | 147 | 152 | |
| SD (±) | 75.9 | 0.5 | 8.7 | 10.1 | 951 | 4291 | 2.8 | 12.4 | 10.3 | 9.0 | 596 | 418 | 79657 | 52169 | 87 | 93 |
| Sig | F=5.2, p=.05 | t=−1.8, p=.10 | t=−3.5, p=.01 | t=0.1, p=.41 | t=5.6, p=.00 | t=4.2, p=.002 | t=0.34, p=.74 | |||||||||
Subject was not able to abstain from tobacco smoking for the required period.
Poor venous access during and post IV nicotine challenge for subject #10 thus no nicotine plasma levels obtained on either scan day.
AUC – area under plasma nicotine concentration time curve, Cmax – maximal concentration of plasma nicotine, Tmax – time to reach Cmax, Cl – clearance of nicotine, VD – volume of distribution. Pre – data from SPECT scan day prior to treatment with 3′-AmNic-rEPA; Post – data from SPECT scan day after treatment with 3′-AmNic-rEPA. SD – standard deviation.
Ab (μg/mL) – antibody concentration levels on scan day 2.
T1 – at time 1 (before immunization); T2 – at time 2 (after immunization)