TABLE 3.
Comparison of preclinical and clinical data of paclitaxel nanoformulations
| ABI-007(Abraxane®) | Taxol® | |
|---|---|---|
| Preclinical data in rats | ||
| Dose (mg/kg) | 5 | 5 |
| t1/2(h) | 11.42 | 7.24 |
| Tmax (h) | 0.033 | 0.033 |
| Cmax (μg/ml) | 4.0 | 11.8 |
| AUC∞ (μg·h/ml) | 4.59 | 5.85 |
| Vz (L/kg) | 18.33 | 8.75 |
| CL (L/h/kg) | 1.112 | 0.837 |
| Clinical data | ||
| Dose | 260 mg/m2, 30 min (n = 14) | 175 mg/m2, 3 h (n = 12) |
| MTD | 300 mg/m2 | 240 mg/m2 |
| t1/2(h) | 21.6 (17.2) | 20.5 (14.6) |
| Tmax (h) | 0.36 (45.2) | 2.65 (27.6) |
| Cmax (ng/ml) | 22,968.6 (112.5) | 3543.3 (57.2) |
| AUC∞ (ng·h/ml) | 14,778.6 (45.3) | 12,602.7 (21.0) |
| Vz (L/m2) | 663.8 (48.1) | 433.4 (31.1) |
| Cl (L/h/m2) | 21.13 (43.8) | 14.76 (31.8) |
Note: The data presented here has been compiled from the article published by Sparreboom et al. (2005). Preclinical: ABI-007 and Taxol were given i.v. to Harlan Sprague–Dawley male rats (n = 10). An i.v. bolus of either [3H] ABI-007 or [3H] Taxol at a PTX dose of 5 mg/kg was administered. Blood PTX concentration was determined from extracted blood pooled from 10 rats, plotted versus time, and fitted using noncompartmental analysis. Two methods were used for blood PTX quantitation: radioactivity and HPLC. The data from HPLC is presented here. Clinical: ABI-007 (Abraxane®) 260 mg/m2 over 0.5 h or Taxol® 175 mg/m2 over 3 h were randomized to give patients with advanced solid tumors. Data are presented as mean values (% coefficient of variation).