GSK2485852 is a Hepatitis C NS5B site IV non-nucleoside polymerase inhibitor being developed for the treatment of chronic HCV infection. HBI115040 is the first administration of GSK2485852 in humans to establish the initial safety, tolerability, pharmacokinetic, and antiviral profile. The study design is a fusion of single and repeat dosing cohorts in HCV infected subjects to evaluate the safety, pharmacokinetics, and antiviral activity of GSK2485852. HBI115040 describes a Phase I, randomized, double-blind, placebo-controlled, dose escalation fusion study to determine the safety, tolerability, pharmacokinetic, and antiviral profile of GSK2485852 in single doses (Part 1), repeat doses (Part 2), and ritonavir co-administration (Part 3) in chronically infected HCV subjects. The study will also explore the effect of a moderate (30%) fat meal on pharmacokinetic endpoints in HCV subjects in Part 1.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
TRIPLE
Enrollment
27
single dose
single dose
single dose
Repeat dose, once daily for 3 days
Repeat dose, twice daily for 3 days
Repeat dose, TIDfor 3 days
Repeat dose, twice daily for 3 days
single dose, day 1
single dose, day 1
single dose daily for 3 days
GSK Investigational Site
Anaheim, California, United States
GSK Investigational Site
Orlando, Florida, United States
GSK Investigational Site
Lenexa, Kansas, United States
GSK Investigational Site
Las Vegas, Nevada, United States
GSK Investigational Site
Willingboro, New Jersey, United States
Safety parameters: adverse events; telemetry; absolute values and changes over time of hematology, clinical chemistry, urinalysis, vital signs (blood pressure, heart rate), and electrocardiogram (ECG) parameters
Time frame: up to 7 days
GSK2485852 PK parameters following single dose administration: AUC(0-inf), AUC(0-t), AUC(0-24), Cmax, tmax, C24, t1/2, tlag, and CL/F
Time frame: 24 hours
GSK2485852 PK parameters following repeat dose administration: AUC(0-τ), Cτ, Cmax, tmax, t1/2, and CL/F
Time frame: 72 hours
HCV RNA viral load reduction from baseline
Time frame: 24 to 72 h
HCV RNA change from baseline to nadir
Time frame: up to 72 h
Time course of HCV viral load at baseline, during dosing with GSK2485852, and > or = 14 days after GSK2485852 dosing
Time frame: up to 14 days
GSK2485852 PK parameters: AUC(0-24), Cmax, tmax and tlag following a single dose with and without moderate fat/calorie meal.
Time frame: 24 h
GSK2485852 accumulation ratio (R)
Time frame: 72 h
GSK2485852 time invariance in non-food cohorts
Time frame: 72 hours
GSK2485852 dose proportionality after single or repeat dosing in non-food cohorts
Time frame: up to 72 h
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