Pharmacology
MK-0457 is a potent pan-Aurora kinase inhibitor used for the treatment of Non-Small-Cell Lung cancer.
Efficacy
| Animal Model | Administration | Dosage | Formulation | Description |
|---|---|---|---|---|
| HeyA8 and SKOV3ip1 tumor mice models[1] | intraperitoneal injection twice daily for 2 days | 50 mg/kg | 1:1 PEG300/PBS | MK-0457 combined with docetaxel results in the greatest efficacy in reducing tumor burden, eliciting a >90% reduction in tumor weight |
| MIA PaCa-2 xenograft mice model[2] | twice a day intraperitoneally (b.i.d. i.p.) for 13 d | 75 mg/kg | 50% PEG 300 in 50 mM phosphate buffer | MK-0457 causes profound inhibition of tumor growth |
Pharmacokinetics and Pharmacodynamics
Toxicity
To be updtaed.
References
[1] Lin YG, et al. Clin Cancer Res, 2008, 14(17), 5437-5446.
[2] Harrington EA, et al. Nat Med, 2004, 10(3), 262-267.
