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Study to Determine the Safety, Tolerability, and Pharmacokinetic (PK) Profile of EGT0001474 in Healthy Volunteers

Phase 1
Completed
Conditions
Safety and Tolerability of EGT0001474 in Healthy Volunteers
Interventions
Drug: Placebo
Registration Number
NCT00854113
Lead Sponsor
Theracos
Brief Summary

This study evaluated the safety, tolerability and pharmacokinetics of single or multiple doses of EGT0001474.

Detailed Description

EGT0001474 is an inhibitor of human sodium dependent glucose co-transporter II being developed for the treatment of Type II Diabetes mellitus.

This is a singe center, Phase-1, double blinded,placebo controlled, dose escalation study of single and multiple ascending doses of EGT0001474 in healthy male and female subjects.

In part-1, subjects were randomized to receive single doses of EGT0001474 at 2.5-150 mg or placebo in the ratio of 3:1. In part-2, subjects were randomized to receive 14 daily doses of EGT0001474 at 10, 50 and 150 mg or placebo in the ratio of 4:1. When the various doses were analysed, the maximum dose 150 mg was found to be tolerable. Although there was no serious adverse events, mild adverse events were observed.

This study provided information on human safety, tolerability, PK and pharmacodynamic effects of EGT0001474.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
78
Inclusion Criteria
  • Male or female volunteers between the ages of 18 and 55 years inclusive.
  • In good health.
  • Female subjects must be surgically sterilized or postmenopausal.
  • Body mass index (BMI) between 18 kg/m2 and 30 kg/m2 inclusive.
  • Non-smoker.
  • Negative drug and alcohol screens.
Exclusion Criteria
  • Abnormal ECG
  • Sitting blood pressure above 140/90 mmHg on 2 evaluations at least 10 minutes apart at screening
  • Treatment with an investigational drug within 30 days or 7 half-lives, whichever is longer.
  • Previous treatment with EGT0001474.
  • History of drug abuse.
  • Febrile illness within 5 days prior to the first dose of study medication.

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
PlaceboPlaceboPlacebo
EGT0001474EGT0001474Ascending doses of EGT0001474
Primary Outcome Measures
NameTimeMethod
CmaxPart-1 (Single dose) measured in 1 day and part 2 (multiple doses) measured in 14 days

Pharmacokinetics results. Cmax -Maximum plasma drug concentration

TmaxPart-1 (Single dose) measured in 1 day and part 2 (multiple doses) measured in 14 days

Pharmacokinetics results. Time to maximum plasma drug concentration (Tmax) was calculated for each groups

AUC 0-tPart-1 (Single dose) measured in 1 day and part 2 (multiple doses) measured in 14 days

Pharmacokinetics results. AUC 0-t - Are under plasma concentration-time curve from time 0 time t.

t1/2Part-1 (Single dose) measured in 1 day and part 2 (multiple doses) measured in 14 days

Pharmacokinetics results.t 1/2 - apparent terminal half life

AUC 0 -24Part-1 (Single dose) measured in 1 day and part 2 (multiple doses) measured in 14 days

Pharmacokinetics results. Area under the plasma concentration-time curve from time 0 to 24 hours post-dose.

Terminal Rate Constant.Part-1 (Single dose) measured in 1 day and part 2 (multiple doses) measured in 14 days

Pharmacokinetics results. Terminal rate constant was estimated by linear regression of logarithmic transformed concentration versus time data

CL/FPart-1 (Single dose) measured in 1 day and part 2 (multiple doses) measured in 14 days

Pharmacokinetics results. Apparent oral clearance

VZ/FPart-1 (Single dose) measured in 1 day and part 2 (multiple doses) measured in 14 days

Pharmacokinetic results. Apparent volume of distribution

Secondary Outcome Measures
NameTimeMethod

Trial Locations

Locations (1)

Covance Clinical Research Unit

🇺🇸

Madison, Wisconsin, United States

Covance Clinical Research Unit
🇺🇸Madison, Wisconsin, United States
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