Atiratecan (TP300; 47 mg/kg; IV; once per week for 3 weeks) shows more than 50% of tumor growth inhibition in all nine models, regardless of the expression of BCRP[1].
Atiratecan (24 mg/kg; IV; once per week for 6 weeks) in combination with capecitabine results in synergistic eVects in the HCT116 human colon cancer and NCI-N87 human gastric cancer xenograft models and an additive eVect in the WiDr human colon cancer xenograft model which is BCRP-positive and CPT-11-insensitive[1].
The eVective dose range of Atiratecan is between 0.30 and 47 mg/kg (MTD/ED50=157). The toxic dose is 63 mg/kg for Atiratecan[1].
| Animal Model: | Five-week-old male athymic nude mice (CAnN.CgFoxn1nu/CrlCrlj)[1] |
| Dosage: | 47 mg/kg (the maximum tolerated dose; MTD) |
| Administration: | IV; once per week for 3 weeks |
| Result: | Showed more than 50% of tumor growth inhibition in all models, regardless of the expression of BCRP.
|
