The study will evaluate the hypothesis that at doses and plasma concentrations which affect pharmacodynamic markers of activity at the chemokine receptors, CCR2 and CCR5, the compound is safe and well tolerated. It will also evaluate the hypothesis that the pharmacokinetic profile is robust and consistent with a once or twice a day therapeutic administration.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
DOUBLE
Enrollment
27
Oral solution, placebo, single dose
Oral solution, 1mg, single dose
Oral solution, 3mg, single dose
Pfizer Investigational Site
New Haven, Connecticut, United States
Safety and toleration: adverse events, supine and standing vital sign measurements, telemetry, 12-lead ECGs, blood and urine tests
Time frame: 0-3 days
Plasma pharmacokinetics: Cmax, Tmax, AUClast, AUCinf, AUC0-24, CL/F, Vz/F and T1/2
Time frame: 0-4 days
Urinary pharmacokinetics: Aet (mount excreted in urine), Aet% and CLr
Time frame: 0-2 days
p-ERK inhibition in human monocytes
Time frame: 0-3 days
Change in circulating monocytes
Time frame: 0-3 days
Change from baseline in plasma MCP-1
Time frame: 0-3 days
MIP 1B stimulated CCR5 receptor internalization
Time frame: 0-3 days
MCP-1 stimulated CCR5 receptor internalization
Time frame: 0-3 days
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Oral solution, 10mg, single dose
Oral solution, 30mg, single dose
Oral solution, 100mg, single dose
Oral solution, 300mg, single dose
Oral solution, 600mg, single dose
Oral solution, 900mg, single dose
Oral solution, up to 900mg, single dose after food
Oral solution, placebo, single dose after food