Table 3

Preclinical antitumor activity of BMS-247550 and paclitaxel versus paclitaxel-resistant tumors

TumorBMS-247550Paclitaxel
Route, scheduleOD1 (mg/kg)LCK2,3GD3,4 (days)LCK2,4,5GD3,4 (days)
Human tumors—in nude mice
 Pat-7i.v. q2d×54.8–6.32.9 ± 1.429.9 ± 3.80.8 ± 0.59.7 ± 45
 A2780Taxi.v. q2d×56.32.5230.87.5
 HCT116/VM46i.v. q2d×54.8–6.32.4330.557.0
i.v. q4d×3162.026.8ND6ND6
 Pat-21i.v. q4d×3 (2 courses)101.694.70.315.7
 Pat-26i.v. q4d×3131.223.50.48.5
Human tumors—in nude rats
 Pat-7i.v. q8d×23>5 (4:6 cures)>462.2 (No cures)21.5 (No cures)
Murine tumor
 M5076i.v. q4d×3241.011.50.34
  • 1 OD, MTD.

  • 2 LCK, gross LCK.

  • 3 LCKs and GDs are for OD or MTD, if inactive.

  • 4 GD, delay (in days) of tumor growth to specified volume (500 or 1000 mm3).

  • 5 LCK are for paclitaxel OD (dose ranged from 24–36 mg/kg, i.v. q2d×5), or highest dose tested, if inactive.

  • 6 ND, not determined.