LP-261 (oral gavage; 4 mg/kg; single dose) displays rapid adsorption by the oral route (Tmax=2.0 h), the terminal half-life of 1.4 h ( 0.2 h indicated a moderate rate of elimination in rat, and the volume of distribution (Vss) is 1.25 L/kg[1].LP-261 (oral gavage; 15 or 50 mg/kg; twice daily; 28 days) at 50mg/kg results in an approximately tumor volume of 130 mm3 versus 3769 mm3 in the vehicle treated group, this represents a 96% reduction in mean tumor volume. Meanwhile, LP-261 at 15 mg/kg leads to a 41% inhibition after 28 days in this mouse model[1].
| Animal Model: | Human tumor xenograft model (Injected with NCI-H522 human non-small-cell) in NCr-nu mice[1] |
| Dosage: | 15 or 50 mg/kg |
| Administration: | Oral gavage; 15 or 50 mg/kg; twice daily; 28 days |
| Result: | Had potent anti-tumor efficacy at high dosage and exhibited no significant changes in body weights. |
