GSK Investigational Site
Tacoma, Washington, 98418, United States
NCT Number: NCT01387204
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.
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Inclusion criteria
Exclusion criteria
11.2. Receiving enzyme inducing anti-epileptic drugs (EIAEDs). 12. History of acute coronary syndromes (including myocardial infarction and unstable angina), coronary angioplasty, or stenting within the past 6 months. 13. QTcB greater than or equal to 480 msec. 14. History or evidence of current clinically significant uncontrolled arrhythmias.
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.
Time frame: 11 days
Time frame: 11 days
AUC(0- t), AUC(0-∞), Cmax, tmax and t1/2
Time frame: 11 days
Characterize and quantify metabolites of GSK1120212 in plasma, urine and feces (studied separately under a DMPK protocol).
Time frame: 11 days
Assess percentage of drug-related material that covalently bonds to plasma proteins (studied separately under a DMPK protocol)
Time frame: 11 days
Blood:plasma ratio of total drug-related material (radioactivity)
Time frame: 11 days
Plasma GSK1120212 concentrations AUC(0-t), AUC(0-∞), Cmax, tmax, and t1/2
Time frame: From dosing on Day 1 to Follow-up
Number of adverse events (AEs)
Time frame: Screening, Day -1, Day 1, Day 5, and Follow-up
Changes from baseline
Time frame: Screening, Day 1 pre-dose, 24 hours, Day 11 and Follow-up
Changes from baseline
Time frame: Screening, Day -1, and Day 11
Changes from baslines
GlaxoSmithKline
Industry
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
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View the official ClinicalTrials.gov record (opens in a new tab)This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.
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