This study evaluated the safety, tolerability and pharmacokinetic (PK) effects of enlicitide chloride in participants with moderate renal impairment (RI) to those of healthy matched control participants. Moderate RI was defined as the estimated glomerular filtration rate (eGFR) ≥30 and \<60milliliter/minute/1.73meters\^2 (ml/min/1.73m\^2). There is no formal hypothesis.
Study Type
INTERVENTIONAL
Allocation
NON_RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
18
10 mg capsule administered orally
Velocity Clinical Research, Hallandale Beach ( Site 0002)
Hallandale, Florida, United States
Alliance for Multispecialty Research, LLC ( Site 0001)
Knoxville, Tennessee, United States
Area Under the Concentration-Time Curve From Time 0 to Infinity (AUC0-Inf) of MK-0616
Blood samples were collected at pre-specified timepoints to determine the AUC0-inf of MK-0616. AUC0-inf was defined as the area under the concentration-time curve of MK-0616 from time zero to infinity.
Time frame: Predose and 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120, 168, 240, and 336 hours postdose
Area Under the Concentration- Time Curve From Time 0 to Last Measurable Concentration (AUC0-last) of MK-0616.
Blood samples were collected at pre-specified timepoints to determine the AUC0-last of MK-0616. AUC0-last was defined as the area under the concentration-time curve of MK-0616 from time zero to last measurable concentration.
Time frame: Predose and 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120, 168, 240, and 336 hours postdose
Maximum Plasma Concentration (Cmax) of MK-0616
Blood samples were collected at pre-specified time points to determine the Cmax of MK-0616. Cmax was defined as the maximum concentration of MK-0616 reached.
Time frame: Predose and 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120, 168, 240, and 336 hours postdose
Time to Maximum Plasma Concentration (Tmax) of MK-0616
Blood samples were collected at pre-specified timepoints to determine the Tmax of MK-0616. Tmax was defined as time to the maximum concentration of MK-0616 reached.
Time frame: Predose and 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120, 168, 240, and 336 hours postdose
Apparent Terminal Half-life (t1/2) of MK-0616
Blood samples were collected at pre-specified timepoints to determine the t1/2 of MK-0616. t1/2 was defined as the time required to divide the MK-0616 plasma concentration by two after reaching pseudo-equilibrium, following a single dose of MK-0616.
Time frame: Predose and 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120, 168, 240, and 336 hours postdose
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Apparent Clearance (CL/F) of MK-0616
Blood samples were collected at pre-specified timepoints to determine the CL/F of MK-0616. CL/F was the apparent total clearance of MK-0616 in plasma over time, assessed as the rate at which MK-0616 was removed from the plasma.
Time frame: Predose and 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120, 168, 240, and 336 hours postdose
Apparent Volume of Distribution (Vz/F) of MK-0616
Blood samples were collected at pre-specified timepoints to determine the Vz/F of MK-0616. Vz/F was the apparent volume of distribution of MK-0616 between the plasma and the rest of the body, after dose, assessed as the total volume of MK-0616 that would need to be uniformly distributed to achieve the desired plasma drug concentration.
Time frame: Predose and 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120, 168, 240, and 336 hours postdose
Number of Participants Who Experienced an Adverse Event (AE)
An AE was any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. An AE can therefore be any unfavourable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a study intervention. Number of participants who experienced an AE were reported.
Time frame: Up to approximately 14 days
Number of Participants Who Discontinued From the Study Due to an AE
An AE was any untoward medical occurrence in a clinical study participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. An AE can therefore be any unfavourable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a study intervention. Number of participants who discontinued from the study due to an AE were reported.
Time frame: Up to approximately 14 days
Amount Recovered in Urine From 0 to 24 Hours (Ae0-24) of MK-0616
Urine samples were collected at pre-specified time points to determine the AE0-24 of MK-0616. Ae0-24 was defined as the amount of MK-0616 recovered in urine from time 0-24 hours.
Time frame: Predose and at 0, 4, 8, 12 and 24 hours postdose
Fraction of Dose Recovered in Urine (Fe) of MK-0616
Urine samples were collected at pre-specified time points to determine the Fe of MK-0616. Fe was defined as the fraction of dose of MK-0616 recovered in urine.
Time frame: Predose and at 0, 4, 8, 12, 24, 36 and 48 hours postdose
Renal Clearance (CLr) of MK-0616
Urine samples were collected at pre-specified time points to determine the CLr of MK-0616. was defined as the time it takes for the MK-0616 to be completely removed by the kidneys.
Time frame: Predose and 4, 8, 12, 24, 36, and 48 hours postdose
Percent Change From Baseline in Free Proprotein Convertase Subtilisin Kexin 9 (PCSK9)
Urine samples were collected at pre-specified time points (baseline and 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48 and 336 hours postdose) to evaluate the reduction in free PCSK9 from baseline to up to 336 hours postdose after administration of MK-0616. The percent change from baseline in free PCSK9 was reported.
Time frame: Baseline (Predose) and up to 336 hours post dose