The purpose of this study is to explore the potential dose response relationship between the pharmacokinetics of GSK2141795 and \[18F\] FDG PET pharmacodynamic markers of glucose metabolism in tumor tissue. Three to six subjects will be enrolled in each cohort and dosed with repeat escalating doses of GSK2141795. \[18F\] FDG PET imaging and optional tumor biopsies will be done prior to initiation of dosing and sequentially at select time points during the first five weeks of dosing. The maximal dose of a given schedule evaluated in this study will not exceed the maximal tolerated dose established in the first-time-in-human trial PCS112689 for the same schedule.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
36
GSK2141795 is an oral, low nanomolar pan-AKT kinase inhibitor that demonstrates activity in hematologic and solid tumor cell lines. It also delays tumor growth in a dose dependent manner in solid tumor xenograft mouse models
GSK Investigational Site
London, United Kingdom
The amount of GSK2141795 in the blood (ng/ml) from baseline
Time frame: 6 months
The net unidirectional uptake of FDG (Ki) from baseline
Time frame: 6 months
The change in size of tumor from baseline (RECIST Criteria)
Time frame: 6 months
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