Healthy male and female volunteers will be given SQ109 300mg daily for 14 days to assess the safety and tolerability and pharmacokinetics.
This is a Phase 1C randomized, placebo controlled, double-blinded, in-patient trial of a single oral dose of 300 mg of SQ109 given daily for 14 consecutive days to evaluate the safety, tolerability and pharmacokinetics of SQ109 in normal healthy male and female subjects 18-45 years of age. Each subject will receive 300 mg of SQ109 or placebo.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
TRIPLE
Enrollment
10
Quintiles Phase I Services - Overland Park
Overland Park, Kansas, United States
Safety & tolerability via: physical exams, color and visual acuity tests, funduscopic exams, neurological exams, vital signs, electrocardiograms, routine clinical labs (includes chemistry, hematology, coagulation and urinalysis data), and adverse events.
Time frame: Days 1-14, 16-18, 21 and 28
Pharmacokinetics of SQ109: Serial blood samples prior to and following single/multiple doses: AUC(0-t): area under the concentration time curve to the last time with concentration greater than or equal to the validated limit of quantitation of the assay
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on day 1.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: AUC(0-infinity): area under the concentration time curve to infinity
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on day 1.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: AUC(0-24): area under the concentration time curve to 24 hours
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on days 1, 5, & 14.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: t1/2: apparent terminal half-life
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on days 1 & 14.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: CL/F: apparent oral clearance
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on days 1, 5, & 14.
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Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: Vz/F: apparent volume of distribution
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on days 1, 5, & 14.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: Cmin: observed minimum concentration
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on days 5, & 14.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: Cavg: calculated average concentration during the dosing interval
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on days 5, & 14.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: Tmax: Time of maximum concentration (Cmax)
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on days 1, 5, & 14.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: AUC(0-tau) Area under the concentration time curve to the end of the dosing interval, 24 hours
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on days 1, 5, & 14.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: RCmax: Accumulation ratio for Cmax estimated as Cmax (Day 14) / Cmax (Day 1)
Time frame: Before and after dosing on days 1-14. Serial PK after dosing on days 1 & 14.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: Tmin: Time to minimum concentration (Cmin)
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on days 1, 5, & 14.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: Linearity Index: AUC(0-tau) (Day 14) / AUC(0-infinity)(Day 1)
Time frame: Before and after dosing on days 1-14. Serial PK after dosing on days 1 & 14.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: RAUC : Accumulation ratio for AUC estimated as AUC0-tau (Day 14)/ AUC(0-24)(Day 1)
Time frame: Before and after dosing on days 1-14. Serial PK after dosing on days 1 & 14.
Pharmacokinetics of SQ109: Serial blood samples for measurement of plasma levels of SQ109 prior to and following single/multiple doses: Cmax: observed maximum concentration
Time frame: Before and after dosing on days 1-14, then on days 16-21 & 28. Serial PK after dosing on days 1, 5, & 14.