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A single 2 mg (2 mg/10mL) oral dose of \[14C\]GSK1120212 containing approximately 79 μCi of radioactivity will be delivered as a solution.

The 2 mg dose is based on clinical data from the ongoing FTIH study in which subjects have been dosed daily for greater than 21 days, as well as preclinical toxicity data.

GSK1120212

GSK Clinical Trials

GSK1120212 is a reversible and highly selective allosteric inhibitor of MEK1 and MEK2 activation and kinase activity currently being developed for the treatment of malignant melanoma. This is a Phase I, open-label, non-randomized, single-dose study designed to characterize the absorption, distribution, metabolism, and elimination (ADME) of a single oral dose of MEK inhibitor \[14C\]GSK1120212 as a solution in male subjects with solid tumor malignancies. A sufficient number of subjects will be enrolled to complete approximately four evaluable subjects. Following completion of the study, subjects may elect to continue dosing with GSK1120212 in the rollover study, MEK114375.

Study to Investigate the Absorption, Distribution, Metabolism and Elimination of [14C]GSK1120212

An Open-label Mass Balance Study to Investigate the Absorption, Distribution, Metabolism and Elimination of a Single Oral Dose of MEK Inhibitor [14C]GSK1120212 in Male Subjects With Solid Tumors

• Total and relative excretion of radioactivity in urine and feces following a single, 2 mg oral solution dose of \[14C\]GSK1120212

AUC(0- t), AUC(0-∞), Cmax, tmax and t1/2

Characterize and quantify metabolites of GSK1120212 in plasma, urine and feces (studied separately under a DMPK protocol).

Assess percentage of drug-related material that covalently bonds to plasma proteins (studied separately under a DMPK protocol)

Blood:plasma ratio of total drug-related material (radioactivity)

Plasma GSK1120212 concentrations AUC(0-t), AUC(0-∞), Cmax, tmax, and t1/2

Study title	NCT ID	Conditions	Interventions	Eligibility	Organization
Study to Investigate the Absorption, Distribution, Metabolism and Elimination of [14C]GSK1120212	NCT01387204	Cancer	GSK1120212	18 Years -	GlaxoSmithKline
Study to Investigate the Absorption, Distribution, Metabolism and Elimination of [14C]GSK1120212	NCT01387204	Cancer	GSK1120212	18 Years -	GlaxoSmithKline
Study to Investigate the Absorption, Distribution, Metabolism and Elimination of [14C]GSK1120212	NCT01387204	Cancer	GSK1120212	18 Years -	GlaxoSmithKline

Spots Global Cancer Trial Database for radiolabeled adme