Table 2.
Plasma pharmacokinetic parameters for total radioactivity, omacetaxine, and its metabolite 4′-DMHHT following a single subcutaneous dose of 1.25 mg/m2 (95 μCi) 14C-omacetaxine (N = 6)
| Cmax (ng/mL)a | tmax (h) | AUC0-t (ng.h/mL)b | AUC0-inf. (ng.h/mL)b | t1/2 (h) | Vz/F (L) | CL/F (L/h) | M:P ratio (AUC0-inf) | |
|---|---|---|---|---|---|---|---|---|
| TRA | ||||||||
| Mean | 30.9 | 0.6c | 262 | 292 | 11.3 | ND | ND | ND |
| SD | 6.1 | 0.3–1.0c | 127 | 134 | 2.5 | ND | ND | ND |
| Omacetaxine | ||||||||
| Mean | 28.6 | 0.48c | 180 | 188 | 14.6 | 268 | 14.4 | ND |
| SD | 6.5 | 0.3–0.5c | 75.4 | 79.9 | 5.5 | 59.3 | 6.2 | ND |
| 4′-DMHHT | ||||||||
| Mean | 3.5 | 3.98c | 45.3 | 49.6 | 10.7 | ND | ND | 0.27 |
| SD | 1.3 | 0.2–8.1c | 33.0 | 34.1 | 2.9 | ND | ND | 0.14 |
AUC 0-t area under the plasma concentration-time curve from time zero to time of the last quantifiable concentration,, AUC 0-inf area under the plasma concentration-time curve from time zero to infinity, CL/F total plasma clearance, C max maximum observed plasma concentration, M:P metabolite-parent, NA not applicable, ND not determined, SD standard deviation, t 1/2 terminal elimination half-life, t max time to maximum observed plasma concentration, TRA total radioactivity, V z /F apparent volume of distribution
aUnits are ng-eqv/g for TRA
bUnits are ng-eqv∙h/g for TRA
cMedian/range values presented