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A Study of Omarigliptin (MK-3102) in Participants With Impaired Renal Function (MK-3102-009)

Phase 1
Completed
Conditions
Chronic Renal Insufficiency
Type 2 Diabetes Mellitus
Interventions
Registration Number
NCT01407276
Lead Sponsor
Merck Sharp & Dohme LLC
Brief Summary

This is a 2-part study in participants with renal impairment and matched healthy participants to investigate the effect of impaired renal function on the plasma and urine levels of omarigliptin (MK-3102) after taking a single 3 mg dose by mouth.

Detailed Description

In Part I, three panels of 6 participants each will be enrolled with varying degrees of renal disease (mild, moderate, or severe renal impairment) based on their estimated glomerular filtration rate (eGFR). Each of these panels will be matched with a corresponding panel of equal number of healthy, age-, race-, BMI- and gender-matched control participants. All panels will receive a single oral dose of 3-mg omarigliptin, followed by plasma sampling and urine collection. In Part II, 6 participants with end stage renal disease (ESRD) requiring hemodialysis will receive a single 3-mg oral dose of omarigliptin immediately following hemodialysis (HD) (Period 1) and 2 hours prior to HD (Period 2).There will be approximately 1 month between Period 1 and Period 2. A corresponding panel of equal number, healthy matched control subjects (age, race, BMI, gender) will also receive a single 3 mg dose by mouth. Omarigliptin dose administration will be followed by plasma sampling for both panels.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
49
Inclusion Criteria

Impaired Renal Function Subjects:

  • Females of reproductive potential must have a negative pregnancy test and agree to use 2 methods of birth control
  • Diagnosis of renal insufficiency based on estimated glomerular filtration rate (eGFR) calculated using the Modification of Diet in Renal Disease (MDRD) equation

Healthy Subjects:

  • Females of reproductive potential must have a negative pregnancy test and agree to use 2 methods of birth control;
  • In general good health
Exclusion Criteria

Impaired Renal Function Subjects:

  • Is mentally or legally incapacitated
  • Has rapidly fluctuating renal function or has demonstrated or suspected renal artery stenosis
  • History of significant endocrine (other than Type 2 diabetes), gastrointestinal, cardiovascular, hematological, immunological, respiratory, or genitourinary diseases
  • History of stroke, chronic seizures or major neurological disease
  • Uncontrolled Type 2 diabetes or history of Type 1 diabetes or ketoacidosis
  • History of cancer (Some exceptions apply)
  • Regular user of barbiturates or sleep aides
  • Consumes excessive amounts of alcohol (more than 2 drinks/day)
  • Consumes excessive amounts of caffeinated beverages (more than 6/day)
  • Has had major surgery or has lost or donated 1 unit of blood within 4 weeks
  • Has a history of significant multiple and/or severe allergies
  • Current or history of illicit drug abuse
  • Nursing mothers

Healthy Subjects:

  • Is mentally or legally incapacitated;
  • Has a history of stroke, chronic seizures, or major neurological disorder
  • Renal impairment
  • History of clinically significant endocrine, gastrointestinal, cardiovascular, hematological, immunological, respiratory, or genitourinary diseases
  • Hypoglycemia, glucose intolerance, Type 1 or Type 2 diabetes, or ketoacidosis
  • History of cancer (Some exceptions apply)
  • Regular user of barbiturates or sleep aides
  • Consumes excessive amounts of alcohol (more than 2 drinks/day)
  • Consumes excessive amounts of caffeinated beverages (more than 6/day)
  • Has had major surgery or has lost or donated 1 unit of blood within 4 weeks
  • Has a history of significant multiple and/or severe allergies
  • Current or history of illicit drug abuse
  • Nursing mothers

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Part 1: Mild Renal Impairment (Panel A)Omarigliptin-
Part 1: Control to Match Panel A (Panel B)Omarigliptin-
Part 1: Moderate Renal Impairment (Panel C)Omarigliptin-
Part 1: Control to Match Panel E (Panel F)Omarigliptin-
Part 2: End-stage Renal Disease needing hemodialysis (Panel G)Omarigliptin-
Part 2: Control to Match Panel G (Panel H)Omarigliptin-
Part 1: Severe Renal Impairment (Panel E)Omarigliptin-
Part 1: Control to Match Panel C (Panel D)Omarigliptin-
Primary Outcome Measures
NameTimeMethod
Area Under the Concentration-time Curve From Time 0 to Infinity (AUC0-∞) of OmarigliptinPre-dose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 (Panel G only), 96, 168, 240, and 336 hours post-dose

AUC0-∞ is a measure of the mean concentration levels of drug in the plasma after the dose.

Maximum Concentration (Cmax) of OmarigliptinPre-dose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 (Panel G only), 96, 168, 240, and 336 hours post-dose

Cmax is a measure of the maximum amount of drug in the plasma after the dose is given.

Concentration at 168 Hours Post-dose (C168h) of Omarigliptin168 hours post-dose

C168h is a measure of the plasma drug concentration 168 hours post-dose.

Apparent Volume of Distribution (Vd/F) of OmarigliptinUp to 336 hours post-dose

Vd/F is defined as the distribution of a medication between the plasma and the rest of the body after the dose. It is the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of the drug.

Area Under the Concentration-time Curve From Time 0 to 168 Hours Post Dose (AUC0-168h) of OmarigliptinPre-dose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 (Panel G only), 96, and 168 hours post-dose

AUC0-168h is a measure of the total amount of drug in the plasma from the dose to 168 hours after the dose.

Apparent Terminal Half-life (t1/2) of OmarigliptinPre-dose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 (Panel G only), 96, 168, 240, and 336 hours post-dose

T1/2 is the time required for the maximum concentration of a drug in the plasma to decrease by 50%.

Apparent Total Body Clearance (CL/F) of OmarigliptinUp to 336 hours post-dose

CL/F is a calculation of the rate at which a drug is removed from the body via renal, hepatic, and other clearance pathways, expressed as volume (milliliters) per unit of time (minutes).

Renal Clearance (CLr) of OmarigliptinUp to 336 hours post-dose

CLr is a calculation of the rate at which a drug is removed from the body via renal clearance pathways, expressed as volume (milliliters) per unit of time (minutes). CLr was only determined for Panels A-F.

Fraction of Dose Excreted Unchanged in Urine Through 48 Hours Post-dose (fe48h) of OmarigliptinUp to 48 hours post-dose

fe48h is expressed as percentage of omarigliptin not metabolized and excreted in urine. fe48h was only determined for Panels A-F.

Cumulative Amount of Drug Excreted in Urine Over 48 Hours (Ae0-48h) of OmarigliptinUp to 48 hours post-dose

Ae0-48h is a measure of the cumulative amount of drug excreted in the urine for 48 hours post-dose. Ae0-48h was only determined for Panels A-F.

Time to Maximum Concentration (Tmax) of OmarigliptinPre-dose and 0.5, 1, 2, 4, 6, 8, 12, 24, 48, 72 (Panel G only), 96, 168, 240, and 336 hours post-dose

Tmax is a measure of the time to reach the maximum drug plasma concentration post-dose.

Secondary Outcome Measures
NameTimeMethod
Number of Participants Experiencing an Adverse Event (AE)From pre-dose to 14 days post-dose (Up to Day 15)

An AE was defined as any unfavorable and unintended change in the structure (signs), function (symptoms), or chemistry (laboratory data) of the body temporally associated with any use of a Sponsor product, whether or not considered related to the use of the product.

Number of Participants Withdrawn From StudyUp to Day 15
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