Mode
Text Size
Log in / Sign up
Phase 1 Completed N=19 Randomized Double-blind Basic Science

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

Healthy Volunteers · Insulin Resistance
Source: ClinicalTrials.gov NCT02370043 ↗
Enrolled (actual)
19
Serious AEs
0.0%
Results posted
Oct 2019
Primary outcomePrimary: Number of Participants With One or More Serious Adverse Events (SAEs) Considered by the Investigator to be Related to Study Drug — 0; 0; 0; 0 participants

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.

Outcome Measures

OutcomeResultp-value
PRIMARY
Number of Participants With One or More Serious Adverse Events (SAEs) Considered by the Investigator to be Related to Study Drug
0; 0; 0; 0; 0; 0
SECONDARY
Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Non-Zero Concentration (AUC0-t)
34699.23; 95223.95; 358380.52; 110566.98; 721393.21; 1207610.37
SECONDARY
Area Under the Concentration-Time Curve From Time Zero to 24-hour Post-Dose (AUC0-24)
3410.02; 12251.48; 33151.96; 16718.65; 60448.26; 113891.92
SECONDARY
Area Under the Concentration-Time Curve From Time Zero to Infinity (AUC0-inf)
40581.44; 128600.49; 387934.16; 120230.35; 776014.78; 1311488.40
SECONDARY
Maximum Observed Drug Concentration (Cmax)
188.65; 637.51; 1857.08; 923.51; 3238.86; 5828.97
SECONDARY
Residual Area
4.59; 11.51; 3.58; 13.23; 4.25; 4.53
SECONDARY
Time to Observed Cmax (Tmax)
4; 5; 4; 8; 5.01; 8
SECONDARY
Elimination Half-Life (T1/2 el)
200.67; 196.45; 214.42; 76.86; 219.71; 197.77
SECONDARY
Elimination Rate Constant (Kel)
0.0035; 0.0035; 0.0032; 0.0090; 0.0032; 0.0035
SECONDARY
Apparent Body Clearance (Cl/F)
0.3696; 0.4666; 0.5027; 1.6219; 0.7732; 0.9150
SECONDARY
Apparent Volume of Distribution (Vd/F)
107.01; 132.23; 155.49; 179.83; 245.08; 261.06
SECONDARY
Area Under the Concentration-time Curve From Time Zero to Infinity (AUC0-inf) in Fed Versus Fasting State
0.32
SECONDARY
Area Under the Concentration-time Curve From Time Zero to the Last Non-Zero Concentration (AUC0-t) in Fed Versus Fasting State
0.31
SECONDARY
Maximum Observed Drug Concentration (Cmax) in Fed Versus Fasting State
0.50
SECONDARY
Time to Maximum Drug Concentration (Tmax) in Fed Versus Fasting State
3
SECONDARY
Amount of Drug Excreted in Urine
37.72; 155.51; 381.35; 224.51; 739.07; 1796.43
SECONDARY
Cumulative Urinary Excretion From Time Zero to Time t (Ae0-t)
90.60; 350.68; 859.41; 421.70; 1893.11; 3793.47
SECONDARY
Maximum Rate of Urinary Excretion (Rmax)
5.13; 21.09; 49.05; 25.53; 123.11; 206.83
SECONDARY
Time of Rmax Urinary Excretion (TRmax)
5.93; 5.93; 5.91; 9.88; 5.88; 9.90
SECONDARY
Renal Clearance (Clr)
0.0266; 0.0286; 0.0259; 0.0252; 0.0313; 0.0333

Eligibility Criteria

Inclusion Criteria

  • 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)

Exclusion Criteria

  • Any clinically significant abnormality or abnormal laboratory test results (other than glucose,triglycerides and LDL-C levels described in inclusion criterion)
  • 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 ( ) 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))
  • History of significant alcohol abuse within one year prior to screening or regular use of alcohol within six months prior to the screening (regular use of more than three units of alcohol per day for males and more than two units of alcohol per day for females [1 unit = 150 (milliliter) mL of wine, 360 mL of beer, or 45 mL of 40% alcohol]) or positive alcohol breath test
  • History of significant drug abuse within the last year or use of soft drugs (such as marijuana) within 3 months prior, or hard drugs (such as cocaine, phencyclidine (PCP) and crack) within the last year
  • Participation in a clinical trial involving the administration of an investigational or marketed drug within the last
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT02370043). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.

Back to search