January 19, 2011Open Access

GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition

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Resumen

GSK1120212 combines high potency, selectivity, and long circulating half-life, offering promise for successfully targeting the narrow therapeutic window anticipated for clinical MEK inhibitors.

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Gilmartin et al. (Wed,) studied this question.

synapsesocial.com/papers/69deb7f3499d77a496b0c965 https://doi.org/https://doi.org/10.1158/1078-0432.ccr-10-2200

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1Safety and efficacy results from the first-in-human study of the oral MEK 1/2 inhibitor GSK1120212.2010 · 121 citations
2Multicenter Phase II Study of the Oral MEK Inhibitor, CI-1040, in Patients With Advanced Non-Small-Cell Lung, Breast, Colon, and Pancreatic Cancer2004 · 639 citations
3Identification of the sites in MAP kinase kinase‐1 phosphorylated by p74raf‐1.1994 · 551 citations
4Phase I Pharmacokinetic and Pharmacodynamic Study of the Oral MAPK/ERK Kinase Inhibitor PD-0325901 in Patients with Advanced Cancers2010 · 250 citations
5MEK1 mutations confer resistance to MEK and B-RAF inhibition2009 · 634 citations

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