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Trial · Interventional

CompletedPhase 1Results postedRegistry data

A Study of Enlicitide Chloride (MK-0616 Oral PCSK9 Inhibitor) in Participants With Moderate Renal Impairment (MK-0616-007)

NCTNCT05070390 (opens ClinicalTrials.gov in a new tab)Other id0616-007Other idMK-0616-007
Open at ClinicalTrials.govAsk about this trial

Overview

Status
Completed
Phase
Phase 1
Enrollment
18 participants (actual)
Sponsor
Merck Sharp & Dohme LLC · Industry
Design
Not randomized · Open label (no masking)
Countries
1 country

United States

Start
16 Nov 2021
Primary completion
3 May 2023
Completion
3 May 2023
First posted
7 Oct 2021
Last update posted
19 Aug 2026
Conditions
Moderate Renal Impairment

Timeline

1 trial · 1 completed · 1 with posted results

  • Completed
  • Ongoing
  • Not yet recruiting
  • Stopped
  • Estimated dates (est.)
  • Results posted
2021202220232024
  1. Ph 1

    A Study of Enlicitide Chloride (MK-0616 Oral PCSK9 Inhibitor) in Participants With Moderate Renal Impairment (MK-0616-007)

    NCT05070390

    16 Nov 2021 to 3 May 2023

Registry summary

Text and fields below are the sponsor's entries at ClinicalTrials.gov, shown as posted.

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.

Interventions

  • Enlicitide ChlorideDrug

Arms2

  • Experimental

    Panel A - Moderate Renal Impairment (RI)

    Single dose of enlicitide chloride 10 mg

  • Experimental

    Panel B - Healthy Controls

    Single dose of enlicitide chloride 10 mg

Primary outcomes7

Outcomes the sponsor listed as primary.

  1. Area Under the Concentration-Time Curve From Time 0 to Infinity (AUC0-Inf) 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

    Registry description

    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.

  2. Area Under the Concentration- Time Curve From Time 0 to Last Measurable Concentration (AUC0-last) 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

    Registry description

    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.

  3. Maximum Plasma Concentration (Cmax) 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

    Registry description

    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.

  4. Time to Maximum Plasma Concentration (Tmax) 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

    Registry description

    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.

  5. Apparent Terminal Half-life (t1/2) 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

    Registry description

    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.

  6. Apparent Clearance (CL/F) 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

    Registry description

    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.

  7. Apparent Volume of Distribution (Vz/F) 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

    Registry description

    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.

Secondary outcomes(6)

  1. Number of Participants Who Experienced an Adverse Event (AE)

    Time frame · Up to approximately 14 days

    Registry description

    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.

  2. Number of Participants Who Discontinued From the Study Due to an AE

    Time frame · Up to approximately 14 days

    Registry description

    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.

  3. Amount Recovered in Urine From 0 to 24 Hours (Ae0-24) of MK-0616

    Time frame · Predose and at 0, 4, 8, 12 and 24 hours postdose

    Registry description

    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.

  4. Fraction of Dose Recovered in Urine (Fe) of MK-0616

    Time frame · Predose and at 0, 4, 8, 12, 24, 36 and 48 hours postdose

    Registry description

    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.

  5. Renal Clearance (CLr) of MK-0616

    Time frame · Predose and 4, 8, 12, 24, 36, and 48 hours postdose

    Registry description

    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.

  6. Percent Change From Baseline in Free Proprotein Convertase Subtilisin Kexin 9 (PCSK9)

    Time frame · Baseline (Predose) and up to 336 hours post dose

    Registry description

    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.

Posted results

Values are shown as posted at ClinicalTrials.gov, with their units. PepBank has not converted, pooled or compared them.

Primary outcome results

Primary outcomeGeometric mean· 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 Infinity (AUC0-Inf) of MK-0616

GroupValue (hour*nmol/Liter)
Panel A - Moderate Renal Impairment (RI)453
Panel B - Healthy Controls369
Primary outcomeGeometric mean· 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.

GroupValue (hour*nmol/Liter)
Panel A - Moderate Renal Impairment (RI)312
Panel B - Healthy Controls192
Primary outcomeGeometric mean· 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

GroupValue (nmol/Liter)
Panel A - Moderate Renal Impairment (RI)5.80
Panel B - Healthy Controls4.00
Primary outcomeMedian· 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

GroupValue (Hour)
Panel A - Moderate Renal Impairment (RI)2.00
Panel B - Healthy Controls4.66
Primary outcomeGeometric mean· 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

GroupValue (Hour)Spread
Panel A - Moderate Renal Impairment (RI)55.144.1
Panel B - Healthy Controls48.832.0
Primary outcomeGeometric mean· Predose and 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120, 168, 240, and 336 hours postdose

Apparent Clearance (CL/F) of MK-0616

GroupValue (Liter/hour)
Panel A - Moderate Renal Impairment (RI)14.2
Panel B - Healthy Controls17.5
Primary outcomeGeometric mean· 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

GroupValue (Liter)
Panel A - Moderate Renal Impairment (RI)1130
Panel B - Healthy Controls1230
Secondary and other outcome results(1)
Secondary outcomeCount of participants· Up to approximately 14 days

Number of Participants Who Experienced an Adverse Event (AE)

GroupValue (Participants)
Panel A - Moderate Renal Impairment (RI)3
Panel B - Healthy Controls2

Adverse events, as posted

Adverse events as posted: participants affected out of participants at risk, by group
GroupDeathsSerious eventsOther events
Panel A - Moderate RIParticipants with moderate renal impairment (RI) received a single dose of MK-616 10mg orally on Day 1.0 / 100 / 103 / 10
Panel B - Healthy ControlsHealthy matched control participants received a single dose of MK-0616 10 mg orally on Day 1.0 / 80 / 82 / 8

Each cell reads participants affected / participants at risk, as the registry posted them.

Registry data comes from ClinicalTrials.gov. Study results come from studies, not from the registry. How PepBank works

Studies0

Studies that cite this trial.

No study cites this trial.

Eligibility

Who could join, as posted.

Sex
All
Age
from 18 Years up to 75 Years
Healthy volunteers
Accepted
Inclusion and exclusion criteria, as posted
Inclusion Criteria: * Good health based upon medical history, physical examination, vital signs, laboratory safety tests, and electrocardiograms (ECG) performed before randomization * Body mass index (BMI) ≥18 kg/m\^2 and ≤40 kg/m\^2 * Male participants must agree to the following during the intervention period and for at least 90 days after the last dose of study intervention: Refrain from donating sperm, PLUS either be abstinent from heterosexual intercourse as their preferred and usual lifestyle (abstinent on a long-term and persistent basis) and agree to remain abstinent, or use acceptable contraception per study protocol * Female participants must be of non-childbearing potential * Moderate RI participants: Baseline estimated glomerular filtration rate (eGFR) ≥30 and \<60 mL/min/1.73 m\^2 based on the Modification of Diet in Renal Disease (MDRD) equation * Moderate Renal Impairment (RI) participants: No clinically significant change in renal status at least 1 month prior to dosing and not currently receiving or has not previously been on hemodialysis * Healthy Matched Controls: eGFR ≥80 mL/min/1.73 m\^2 based on the MDRD equation Exclusion Criteria: * Healthy Matched Controls: history of clinically significant endocrine, GI, cardiovascular, hematological, hepatic, immunological, renal, respiratory, genitourinary, or major neurological (including stroke and chronic seizures) abnormalities or diseases * Mentally or legally incapacitated, has significant emotional problems at the time of prestudy (screening) visit or expected during the conduct of the study or has a history of clinically significant psychiatric disorder of the last 5 years. Participants who have had situational depression may be enrolled in the study at the discretion of the investigator * History of cancer, with the exception of adequately treated nonmelanomatous skin carcinoma or carcinoma in situ of the cervix or other malignancies that have been successfully treated with appropriate follow up and therefore unlikely to recur for the duration of the study * History of significant multiple and/or severe allergies * Positive for hepatitis B surface antigen (HBsAg), hepatitis C antibodies or human immunodeficiency virus (HIV) * History of major surgery, donated or lost 1 unit of blood (approximately 500 mL) within 4 weeks prior to the prestudy (screening) visit * Moderate RI participants: Does not agree to follow the smoking restrictions as defined by the study * Healthy Matched Controls: History of smoking and/or has used nicotine or nicotine-containing products (eg, nicotine patch and electronic cigarette) within 3 months of screening * Received any nonlive vaccine starting from 14 days prior to study intervention or is scheduled to receive any nonlive vaccine through 30 days following study intervention with the exception of Corona virus disease (COVID-19) vaccine administration. Study intervention must be given at least 72 hours following or at least 48 hours prior to any COVID-19 vaccination * Consumes greater than 3 servings of alcoholic beverages per day * Consumes excessive amounts, defined as greater than 6 servings (1 serving is approximately equivalent to 120 mg of caffeine) of coffee, tea, cola, energy drinks, or other caffeinated beverages per day * Regular user of cannabis, any illicit drugs or has a history of drug (including alcohol) abuse within approximately 3 months

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