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Safety and Pharmacokinetic Study of S-Equol in Healthy Volunteers

Phase 1
Completed
Conditions
Healthy
Interventions
Drug: Placebo
Registration Number
NCT00787007
Lead Sponsor
Ausio Pharmaceuticals, LLC
Brief Summary

The purpose of this study is 1) to test the safety of S-equol in healthy volunteers and 2) to see how quickly S-equol enters the bloodstream, is distributed in the body, and broken down and removed, when taken with food or without food.

Detailed Description

The study is a double blind, randomized, placebo-controlled, dose-escalation study of the safety and tolerability of single doses of S-equol up to 320 mg in healthy male and female adult subjects. Approximately 8 qualified volunteers will be selected at each dose level and randomly assigned to receive S-equol or placebo, in the fasted state. For the 20 mg dose group, subjects will complete two treatment periods, one in the fasted state, and one in the fed state.

A safety review of study results for each dose group will occur when Day 8 follow-up visit safety data are available, and prior to enrollment/dosing of the next subsequent dose group. Given favorable safety review of a dose group's experience, the subsequent dose group will be enrolled/dosed at least 10 days after the previous group's dosing.

Pharmacokinetic evaluations consist of determination of plasma and urine concentrations of free and total conjugated S-equol at various time points. Safety evaluations include physical examination,vital signs, ECG, serum chemistry, hematology, and urinalysis, 12-lead telemetry, and assessment of clinical signs and symptoms.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
60
Inclusion Criteria
  • Healthy male and female volunteers aged 18 to 65 years, inclusive
  • Female subjects must be non-pregnant and non-lactating; surgically sterile, post-menopausal or be using an acceptable non-hormonal method of birth control
  • Must not have used any hormonal agents or devices within 4 weeks prior to enrollment
  • In good health as determined by a physician
  • BMI between 18 and 30, inclusive
  • Normal clinical laboratory test results
  • Negative drug and alcohol toxicology screens
  • Negative HIV antibody and hepatitis panel screening results
  • For men over 44 years of age, PSA ≤ 2.0 ng/mL
  • For women over 44 years of age, normal mammography and pelvic ultrasound
  • Protein C and Protein S activity levels above the lower limit of normal
  • Negative for Factor V Leiden.
Exclusion Criteria
  • History of any chronic, subacute or acute condition of clinical significance
  • Total bilirubin level >0.9, conjugated bilirubin >0.4, or unconjugated bilirubin >0.8
  • Fasting cholesterol level >280 mg/dL; fasting triglyceride level >1.5 x ULN
  • History of thromboembolic events or estrogen-dependent benign or malignant neoplasm
  • Resting systolic blood pressure >140 mm Hg or <90 mm Hg, or diastolic blood pressure >90 mm Hg or <60 mm Hg
  • Resting pulse >100 beats/minute or <45 beats/minute
  • Abnormal 12-lead ECG or telemetry results
  • Subject is unwilling or unable to comply with study rules
  • History of sudden cardiac death in the immediate family, or a personal history of cardiac disease, treated hypertension, congestive heart failure, or unexplained syncope
  • History of cancer, other than basal cell carcinoma or stage 1 squamous cell carcinoma, that has not been successfully treated
  • Use of any prescription or over-the-counter medication within 1 week prior to Day -1 or anticipates the need for any medication during the course of the study
  • History or intolerance to estrogen medication
  • History of substance abuse, drug addiction, or alcoholism within 3 years
  • Inability to abstain from alcohol, caffeine, Yerba mate tea, or from grapefruit, grapefruit juice or flavonoid-rich foods from 48 hours prior to the administration of study medication and throughout the duration of the study.
  • History of smoking or any use of a tobacco or nicotine containing product within 6 months
  • Donated blood or blood products within 30 days
  • Mental instability or inability to be compliant with the protocol
  • Subject has received an investigational test substance within 60 days or anticipates receiving any investigational test substance other than S-equol during the course of this study
  • Subject has been previously enrolled in this study

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
7Placeboplacebo capsule
2S-equol20 mg, fasted and fed
1S-equol10 mg
3S-equol40 mg
4S-equol80 mg
5S-equol160 mg
6S-equol320 mg
Primary Outcome Measures
NameTimeMethod
To evaluate the safety and tolerability of ascending, single oral doses of S-equol, administered in fasted and fed states, in healthy male and female volunteers.Continuous
Secondary Outcome Measures
NameTimeMethod
To evaluate the single dose pK profile of S-equol in the fed and fasted state. To compare the pK profiles of younger and older and male and female volunteers.Variable

Trial Locations

Locations (1)

Charles River

🇺🇸

Tacoma, Washington, United States

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