The purpose of this study is to test the safety of a new drug and to look at how the drug is handled by your body. This is the first time the drug will be given to people, the drug has been safely given to animals over many days at higher doses than will be given in the study. The study will be done in healthy men and woman to determine what effects, good or bad, it has on thier health. This study will find out: If the drug has any side effects after one dose of the drug is given? How much of the drug gets into the bloodstream, and how long does the body take to get rid of it? If the drug causes any changes to a substance that is in skin, hair or blood.
This study represents the first administration of the focal adhesion kinase (FAK) inhibitor GSK2256098 to humans to evaluate the safety, pharmacokinetics (PK), pharmacodynamics (PD), and preliminary food effect following single oral doses in adult healthy subjects before proceeding to studies in subjects with cancer that will be given at higher doses over an extended period of time. FAK is a protein in the body that is important in cancer development. Objectives of the study will be to characterize the safety of single doses of GSK2256098; to characterize the single dose PK of GSK2256098 in the presence and absence of food; to examine the dose proportionality of GSK2256098 PK parameters following single dose administration; and to characterize the effect of single doses of GSK2256098 on phospho-FAK (pFAK) tyrosine 397 (Y397) levels in skin and hair follicles. Dose- and concentration-effect relationships for various safety parameters will be explored as appropriate.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
SINGLE
Enrollment
38
focal adhesion kinase inhibitor given as a single dose
Placebo to be used as comparator for GSK2256098
GSK Investigational Site
Melbourne, Victoria, Australia
To characterize the safety of single doses of GSK2256098 in adult healthy subjects
Time frame: within 10-14 days following administration of study drug
To characterize the single dose pharmacokinetics of GSK2256098 in blood and urine in adult healthy subjects
Time frame: 14 days after administration of study drug
To examine the dose proportionality of GSK2256098 pharmacokinetic parameters following single dose administration in healthy subjects
Time frame: 14 days
To explore dose- and concentration-effect relationships for various safety parameters, if appropriate
Time frame: 14 days
To estimate the effect of high fat/calorie meal on the pharmacokinetics, safety, and tolerability of a single dose of GSK2256098.
Time frame: 14 days
To explore and potentially identify small molecules or cytokines in plasma which may serve as biomarkers for future studies
Time frame: 14 days
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