A Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Food-Effect of KQ-791

NCT02370043 | Completed Phase 1 Results

• 1 other identifier: KQ-791-01
• Study Type: interventional
• Target: 19
• Locations: 1 country
• Sites: 2

Brief Summary

The purpose of this study is to assess the safety, tolerability, and the effect of food on KQ-791. Each participant may receive up to 3 single doses of KQ-791 (at up to 3 different dose levels) and 1 placebo dose over the course of the study. Up to 6 escalating dose levels may be studied, in two distinct groups or cohorts.

Conditions

Healthy Volunteers; Insulin Resistance

Outcome Measures

Primary Outcomes (1)

• Number of Participants With One or More Serious Adverse Events (SAEs) Considered by the Investigator to be Related to Study Drug

  Baseline to study completion (up to 11 weeks)

Secondary Outcomes (19)

• Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Non-Zero Concentration (AUC0-t)

  Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mg

• Area Under the Concentration-Time Curve From Time Zero to 24-hour Post-Dose (AUC0-24)

  Pre-dose and 0.5, 1, 2, 4, 6, 8,10, and 24 hours post-dose

• Area Under the Concentration-Time Curve From Time Zero to Infinity (AUC0-inf)

  Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mg'

• Maximum Observed Drug Concentration (Cmax)

  Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mg

• Residual Area

  Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mg

Study Arms (3)

KQ-791

EXPERIMENTAL

Escalating doses of KQ-791, starting at 15 milligrams

Drug: KQ-791

KQ-791 (after meal)

EXPERIMENTAL

Single dose of KQ-791 in capsule form, after a meal

Drug: KQ-791 (after meal)

Placebo

PLACEBO COMPARATOR

Single dose of placebo matching KQ-791 dose

Drug: Placebo

Interventions

KQ-791 DRUG

Capsules administered orally while fasting, in up to 3 periods

KQ-791

KQ-791 (after meal) DRUG

Single dose of KQ-791 in capsules, after a meal, in 1 period

KQ-791 (after meal)

Placebo DRUG

Capsules, administered orally, in 1 period

Placebo

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Male or non-childbearing potential female, which includes post-menopausal female (absence of menses for 12 months prior to drug administration, bilateral oophorectomy or hysterectomy with bilateral oophorectomy at least 6 months prior to drug administration) or surgically sterile female (hysterectomy or tubal ligation at least 6 months prior to drug administration)
• Body Mass Index (BMI) greater than or equal to (≥) 27.0 and less than or equal to (≤) 35.0 kilogram per square meter (kg/m2)
• Healthy as defined by:
• absence of clinically significant illness and surgery within last 4 weeks. Participants vomiting within 24 hours pre-dose will be evaluated for upcoming illness/disease
• the absence of clinically significant history of neurological, endocrine, cardiovascular, pulmonary, hematological, immunologic, psychiatric, gastrointestinal, renal, hepatic, or metabolic disease
• Male participants who are not vasectomized for at least 6 months, and who are sexually active with non-sterile female partner (sterile female partners include post-menopausal females and surgically sterile females) must be willing to use one of the following acceptable contraceptive methods throughout the study and for 90 days after the last study drug administration:
• simultaneous use of a condom, and for the female partner hormonal contraceptives (used since at least 4 weeks) or intra-uterine contraceptive device (placed since at least 4 weeks)
• simultaneous use of a male condom, and for his female partner, a diaphragm with intravaginally applied spermicide
• Some degree of insulin resistance, as shown by:
• fasting blood glucose ≥95.4 and ≤126 milligrams per deciliter (mg/dL) (equivalent to 5.3 to 7.0 millimoles per liter (mmol/L), respectively) and
• fasting triglycerides ≤ 4.0 mmol/L, and/or
• Low-Density Lipoprotein Cholesterol (LDL-C) ≤ 6.0 mmol/L
• Capable of consent
• Non-smoker (no use of tobacco products within the last 3 months)

You may not qualify if:

• Positive test for hepatitis B, hepatitis C, or Human Immunodeficiency Virus (HIV)
• Evidence of clinically significant hepatic or renal impairment, including Alanine Aminotransferase (ALT) above 1.5x Upper Limit of Normal (ULN), Aspartate Aminotransferase (AST) above 2x ULN, total bilirubin above 2x ULN (total bilirubin accepted up to 2x ULN if direct bilirubin is within normal limits), or Estimated Glomerular Filtration Rate (eGFR) less than (\<) 90 milliliters per minute (mL/minute)
• Positive urine drug screen
• History of significant allergic reactions (e.g. angioedema) to any drug.
• Use of any drugs known to induce or inhibit hepatic drug metabolism within the last 30 days
• Positive pregnancy test
• Any reason which, in the opinion of the qualified investigator (QI) would prevent the subject from participating in the study
• Clinically significant electrocardiogram (ECG) abnormalities at screening, or clinically significant personal or family history (in a first-degree relative) of heart diseases, including:
• Confirmed corrected QT (QTcF) interval greater than (\>) 450 milliseconds (msec) for men and women
• Bundle branch blocks and other conduction abnormalities other than mild first degree atrio-ventricular block
• Irregular rhythms other than sinus arrhythmia or occasional, rare supraventricular ectopic beats
• History of unexplained syncope
• Family history of unexplained sudden death or sudden death due to long QT syndrome
• T-wave configurations are not of sufficient quality for assessing QT interval
• Clinically significant vital sign abnormalities (systolic blood pressure lower than 90 or over 150 mmHg, diastolic blood pressure lower than 50 or over 95 mmHg, or heart rate less than 50 or over 100 beats per minute (bpm))

Sponsors & Collaborators

• Kaneq Bioscience Limited: lead

Study Sites (2)

Inventiv

Montreal, Quebec, H3X 2Hp, Canada

Location

inVentiv

Québec, G1P 0A2, Canada

Location

MeSH Terms

Conditions

Insulin Resistance

Interventions

Postprandial Period

Condition Hierarchy (Ancestors)

Hyperinsulinism; Glucose Metabolism Disorders; Metabolic Diseases; Nutritional and Metabolic Diseases

Intervention Hierarchy (Ancestors)

Digestive System Physiological Phenomena; Digestive System and Oral Physiological Phenomena

Results Point of Contact

• Title: Dr. Gosse Bruinsma
• Organization: Kaneq Bioscience Limited

gosse.bruinsma@kaneqbioscience.ca

1-613-800-0955

Study Officials

• Email: daniel.bouthillier@Kaneq.ca

  Kaneq Bioscience

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Purpose: BASIC SCIENCE
• Intervention Model: CROSSOVER
• Sponsor Type: OTHER
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 18, 2015
• First Posted: February 24, 2015
• Study Start: February 1, 2015
• Primary Completion: July 1, 2015
• Study Completion: July 1, 2015
• Last Updated: November 26, 2019
• Results First Posted: October 30, 2019

Record last verified: 2019-11

Locations

CA (2)