Safety and Pharmacokinetic Study of S-Equol in Healthy Volunteers

Ausio Pharmaceuticals

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: S-equol; Drug: Placebo

Study type: Interventional

Funder types: Industry

Identifiers

NCT00787007

AUS-CT01

Details and patient eligibility

About

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.

Full 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.

Enrollment: 60 patients

Sex: All

Ages: 18 to 65 years old

Volunteers: Accepts Healthy Volunteers

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

Trial design

Primary purpose: Basic Science

Allocation: Randomized

Interventional model: Parallel Assignment

Masking: Double Blind

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60 participants in 7 patient groups, including a placebo group

1

Experimental group

Description:

10 mg

Treatment:

Drug: S-equol

2

Experimental group

Description:

20 mg, fasted and fed

Treatment:

Drug: S-equol

3

Experimental group

Description:

40 mg

Treatment:

Drug: S-equol

4

Experimental group

Description:

80 mg

Treatment:

Drug: S-equol

5

Experimental group

Description:

160 mg

Treatment:

Drug: S-equol

6

Experimental group

Description:

320 mg

Treatment:

Drug: S-equol

7

Placebo Comparator group

Description:

placebo capsule

Treatment:

Drug: Placebo