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MedKoo product information:
Description of Trametinib: Trametinib is an orally bioavailable inhibitor of mitogen-activated protein kinase kinase (MEK MAPK/ERK kinase) with potential antineoplastic activity. Trametinib specifically binds to and inhibits MEK 1 and 2, resulting in an inhibition of growth factor-mediated cell signaling and cellular proliferation in various cancers. MEK 1 and 2, dual specificity threonine/tyrosine kinases often upregulated in various cancer cell types, play a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway that regulates cell growth. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
Current developer: GSK
Antitumor activities: . Trametinib (JTP-74057) strongly inhibited MEK1/2 kinase activities, but did not inhibit another 98 kinase activities. Treatment by JTP-74057 resulted in growth inhibition accompanied with upregulation of p15INK4b and/or p27KIP1 in most of the colorectal cancer cell lines tested. Daily oral administration of JTP-74057 for 14 days suppressed tumor growth of HT-29 and COLO205 xenografts in nude mice. Notably, tumor regression was observed only in COLO205 xenografts, and COLO205 was much more sensitive to JTP-74057-induced apoptosis than HT-29 in vitro. Treatment with an Akt inhibitor enhanced the JTP-74057-induced apoptosis in HT-29 cells. Finally, JTP-74057 exhibited an additive or a synergistic effect in combination with the standard-of-care agents, 5-fluorouracil, oxaliplatin or SN-38. JTP-74057, a highly specific and potent MEK1/2 inhibitor, exerts favorable antitumor activities in vitro and in vivo. Sensitivity to JTP-74057-induced apoptosis may be an important factor for the estimation of in vivo efficacy, and sensitivity was enhanced by an Akt inhibitor. These results suggest the usefulness of JTP-74057 in therapeutic applications for colorectal cancer patients. (source: Int J Oncol. 2011 Jul;39(1):23-31).
1: Jing J, Greshock J, Holbrook JD, Gilmartin AG,
Zhang X, McNeil E, Conway T, Moy C, Laquerre S, Bachman KE, Wooster R,
Degenhardt Y. Comprehensive Predictive Biomarker Analysis for MEK
Inhibitor GSK1120212. Mol Cancer Ther. 2011 Dec 14. [Epub ahead of
print] PubMed PMID: 22169769.
(Keyword; CAS#; MedKoo code#)
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