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Trial · Interventional

CompletedPhase 1Results postedRegistry data

Enlicitide Decanoate (MK-0616 Oral PCSK9 Inhibitor) Renal Impairment Study (MK-0616-020)

NCTNCT05934292 (opens ClinicalTrials.gov in a new tab)Other id0616-020Other idMK-0616-020
Open at ClinicalTrials.govAsk about this trial

Overview

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

United States

Start
20 Jul 2023
Primary completion
19 Jan 2024
Completion
19 Jan 2024
First posted
6 Jul 2023
Last update posted
30 Sept 2026
Conditions
Hypercholesterolaemia

Timeline

1 trial · 1 completed · 1 with posted results

  • Completed
  • Ongoing
  • Not yet recruiting
  • Stopped
  • Estimated dates (est.)
  • Results posted
202320242025
  1. Ph 1

    Enlicitide Decanoate (MK-0616 Oral PCSK9 Inhibitor) Renal Impairment Study (MK-0616-020)

    NCT05934292

    20 Jul 2023 to 19 Jan 2024

Registry summary

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

The primary objective of the study is to compare the plasma pharmacokinetics (PK) of enlicitide decanoate following a single 20 mg dose in participants on a background of statin therapy with varying degrees of renal impairment (moderate, severe, end stage renal disease \[ESRD\]) to those of healthy mean matched control participants on a background of statin therapy. There is no formal hypothesis.

Interventions

  • Enlicitide DecanoateDrug

Arms4

  • Experimental

    Panel A: Moderate Renal Impairment (RI)

    Participants receive Enlicitide Decanoate 20 mg tablet single dose orally on Day 1

  • Experimental

    Panel B: Severe RI

    Participants receive Enlicitide Decanoate 20 mg tablet single dose orally on Day 1

  • Experimental

    Panel C: End-Stage Renal Disease (ESRD) on Hemodialysis (HD)

    Participants receive Enlicitide Decanoate 20 mg tablet orally on Day 1 and Day 16.

  • Experimental

    Panel D: Healthy Controls

    Participants receive Enlicitide Decanoate 20 mg tablet single dose orally on Day 1.

Primary outcomes7

Outcomes the sponsor listed as primary.

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

    Time frame · Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

    Registry description

    AUC0-inf was a measure of the total amount of drug in the plasma from the dose administration extrapolated to infinity. Blood for plasma samples was collected at pre-specified timepoints to determine the AUC0-inf of enlicitide decanoate for Panel A, B, C, and D participants. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C ESRD - enlicitide decanoate pre-hemodialysis and Panel C ESRD - enlicitide decanoate post-hemodialysis to report AUC0-inf. Per protocol, mean AUC0-inf was reported.

  2. AUC From Time 0 to Last Measurable Concentration (AUClast) of Enlicitide Decanoate

    Time frame · Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

    Registry description

    AUClast was defined as the area under the concentration-time curve of enlicitide decanoate from time zero to last measurable concentration. Blood for plasma samples was collected at pre-specified timepoints to determine the AUClast of enlicitide decanoate in Panel A, B, C, and D participants. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C ESRD - enlicitide decanoate pre-hemodialysis and Panel C ESRD - enlicitide decanoate post-hemodialysis to report AUClast. Per protocol, mean AUClast was reported.

  3. Maximum Plasma Concentration (Cmax) of Enlicitide Decanoate

    Time frame · Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

    Registry description

    Cmax was defined as the maximum or peak concentration of enlicitide decanoate observed after its administration. Blood for plasma samples was collected at pre-specified time points to determine the Cmax of enlicitide decanoate in Panel A, B, C and D participants. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis to report Cmax. Per protocol, mean Cmax was reported.

  4. Time to Maximum Plasma Concentration (Tmax) of Enlicitide Decanoate

    Time frame · Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

    Registry description

    Tmax was defined as the time required for a study drug to reach maximum concentration in plasma. Blood for plasma samples was collected at pre-specified time points to determine the Tmax of enlicitide decanoate in Panel A, B, C and D participants. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis to report Tmax. Per protocol, mean Tmax was reported.

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

    Time frame · Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

    Registry description

    Half-life (t1/2) was defined as the time required for plasma drug concentration of enclitide decanoate to decrease by 50% from peak. Blood for plasma samples was collected at pre-specified time points to determine the t1/2 of enlicitide decanoate in Panel A, B, C and D participants. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis to report t1/2. Per protocol, mean t1/2 was reported.

  6. Apparent Clearance (CL/F) of Enlicitide Decanoate

    Time frame · Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

    Registry description

    CL/F was the apparent total clearance of enlicitide decanoate in plasma over time. Blood for plasma samples was collected at pre-specified timepoints to determine the CL/F of enlicitide decanoate for Panel A, B, C, and D participants. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis to report CL/F. Per protocol, mean CL/F was reported.

  7. Apparent Volume of Distribution (Vz/F) of Enlicitide Decanoate

    Time frame · Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

    Registry description

    Vz/F was the apparent volume of distribution of enlicitide decanoate between the plasma and the rest of the body, after dose, assessed as the total volume of enlicitide decanoate that would need to be uniformly distributed to achieve the desired plasma drug concentration. Blood for plasma samples was collected at pre-specified time points to determine the Vz/F of Enlicitide Decanoate in Panel A, B, C, and D participants. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis to report Vz/F. Per protocol, mean Vz/F was reported.

Secondary outcomes(10)

  1. Panel C: Dialysate Clearance (CLd) of Enlicitide Decanoate

    Time frame · Predose and 0, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, and 48 hours postdose

    Registry description

    CLd was the measure of the amount of enlicitide decanoate cleared from plasma via dialysis. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis. Urine samples were to be collected for Panel C participants to determine mean CLd.

  2. Panel C: Dialysate Concentration (Cd) of Enlicitide Decanoate

    Time frame · Predose and 0, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, and 48 hours postdose

    Registry description

    Cd was the measure of the concentration of enlicitide decanoate in dialysate. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis. Urine samples were to be collected for Panel C participants to determine mean Cd.

  3. Panel C: Amount of Enlicitide Decanoate Excreted (AEd) in Dialysate

    Time frame · Predose and 0, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, and 48 hours postdose

    Registry description

    AEd was the measure of the amount of enlicitide decanoate excreted in the dialysate. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis. Urine samples were to be collected for Panel C participants to determine mean AEd.

  4. Panel C: Percentage of Dose (%Dose) of Enlicitide Decanoate Excreted in Dialysate

    Time frame · Predose and 0, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, and 48 hours postdose

    Registry description

    %Dose was the percentage of the dose of enlicitide decanoate excreted in the dialysate. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis. Urine samples were to be collected for Panel C participants to determine %Dose.

  5. Amount of Enlicitide Decanoate Excreted in Urine From 0 to 24 Hours (AE0-24) After Administration of Enlicitide Decanoate

    Time frame · Predose and 0, 0.5, 1, 1.5, 2, 4, 8, 12, and 24 hours postdose

    Registry description

    AE0-24 was the measure of the amount of enlicitide decanoate excreted at 0 to 24 hours. Urine samples were to be collected to determine the AE0-24 after administration of enlicitide decanoate for Panels A, B, C, and D. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis to report AE0-24. Per protocol, mean AE0-24 was reported.

  6. Percentage of Unchanged Enlicitide Decanoate Excreted in Urine (Fe)

    Time frame · Predose and 0, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, and 48 hours postdose

    Registry description

    Fe was the measure of the percentage of unchanged enlicitide decanoate excreted in the urine. The percentage of enlicitide decanoate that was excreted unchanged in urine over the 24-hr collection interval (Fe) was calculated as 100 times the ratio of Ae0-24 and dose. Urine samples were to be collected to determine the Fe after administration of enlicitide decanoate for Panels A, B, C, and D. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis to report Fe.

  7. Renal Clearance (CLr) of Enlicitide Decanoate

    Time frame · Predose and 0, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, and 48 hours postdose

    Registry description

    CLr was the measure of how quickly enlicitide decanoate was removed from the plasma by the kidney and excreted in urine. Urine samples were to be collected to determine the CLr after administration of enlicitide decanoate for Panels A, B, C, and D. Per protocol, Panel C ESRD on HD arm was separated into two arms: Panel C enlicitide decanoate pre-hemodialysis and Panel C enlicitide decanoate post-hemodialysis to report CLr. Per protocol, mean CLr was reported.

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

    Time frame · Up to approximately 30 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 unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a study intervention. The number of participants who experienced an AE were reported.

  9. Panels A, B, and D: Number of Participants Who Discontinued From the Study Due to an AE

    Time frame · Up to approximately 30 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 unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a study intervention. The number of Panel A, B, and D participants who discontinued study treatment due to an AE were reported.

  10. Panel C: Number of Participants Who Discontinued From the Study Treatment Due to an AE

    Time frame · Up to approximately 30 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 unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease (new or exacerbated) temporally associated with the use of a study intervention. The number of Panel C participants who discontinued study treatment due to an AE were 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 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

Area Under the Concentration-Time Curve From Time 0 to Infinity (AUC0-Inf) of Enlicitide Decanoate

GroupValue (hr*nmol/Liter)
Panel A: Moderate Renal Impairment (RI)733
Panel B: Severe RI554
Panel C: ESRD - Enlicitide Decanoate Pre-Hemodialysis850
Panel C: ESRD - Enlicitide Decanoate Post-Hemodialysis570
Panel D: Healthy Controls487
Primary outcomeGeometric mean· Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

AUC From Time 0 to Last Measurable Concentration (AUClast) of Enlicitide Decanoate

GroupValue (hr*nmol/Liter)
Panel A: Moderate Renal Impairment (RI)735
Panel B: Severe RI362
Panel C: ESRD - Enlicitide Decanoate Pre-Hemodialysis649
Panel C: ESRD - Enlicitide Decanoate Post-Hemodialysis538
Panel D: Healthy Controls456
Primary outcomeGeometric mean· Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

Maximum Plasma Concentration (Cmax) of Enlicitide Decanoate

GroupValue (nmol/Liter)
Panel A: Moderate Renal Impairment (RI)9.56
Panel B: Severe RI5.8
Panel C: ESRD - Enlicitide Decanoate Pre-Hemodialysis8.73
Panel C: ESRD - Enlicitide Decanoate Post-Hemodialysis9.08
Panel D: Healthy Controls9.72
Primary outcomeMedian· Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

Time to Maximum Plasma Concentration (Tmax) of Enlicitide Decanoate

GroupValue (hours)
Panel A: Moderate Renal Impairment (RI)16
Panel B: Severe RI2.75
Panel C: ESRD - Enlicitide Decanoate Pre-Hemodialysis18.01
Panel C: ESRD - Enlicitide Decanoate Post-Hemodialysis1.00
Panel D: Healthy Controls1.0
Primary outcomeGeometric mean· Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

Apparent Terminal Half-life (t1/2) of Enlicitide Decanoate

GroupValue (hours)Spread
Panel A: Moderate Renal Impairment (RI)81.570.4
Panel B: Severe RI56.432.7
Panel C: ESRD - Enlicitide Decanoate Pre-Hemodialysis53.636.9
Panel C: ESRD - Enlicitide Decanoate Post-Hemodialysis75.662.9
Panel D: Healthy Controls4660.8
Primary outcomeGeometric mean· Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

Apparent Clearance (CL/F) of Enlicitide Decanoate

GroupValue (Liter/hr)
Panel A: Moderate Renal Impairment (RI)17.6
Panel B: Severe RI23.3
Panel C: ESRD - Enlicitide Decanoate Pre-Hemodialysis15.2
Panel C: ESRD - Enlicitide Decanoate Post-Hemodialysis22.6
Panel D: Healthy Controls26.5
Primary outcomeGeometric mean· Predose and 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, 48, 72, 120, 168, and 240 hours postdose

Apparent Volume of Distribution (Vz/F) of Enlicitide Decanoate

GroupValue (Liter)
Panel A: Moderate Renal Impairment (RI)2070
Panel B: Severe RI1890
Panel C: ESRD - Enlicitide Decanoate Pre-Hemodialysis1170
Panel C: ESRD - Enlicitide Decanoate Post-Hemodialysis2470
Panel D: Healthy Controls1760
Secondary and other outcome results(1)
Secondary outcome· Predose and 0, 0.5, 1, 1.5, 2, 4, 8, 12, 24, 36, and 48 hours postdose

Panel C: Dialysate Clearance (CLd) of Enlicitide Decanoate

GroupValue
Panel C: ESRD - Enlicitide Decanoate Pre-Hemodialysisnot posted
Panel C: ESRD - Enlicitide Decanoate Post-Hemodialysisnot posted

Adverse events, as posted

Adverse events as posted: participants affected out of participants at risk, by group
GroupDeathsSerious eventsOther events
Panel A: Moderate Renal Impairment (RI)Participants received Enlicitide Decanoate 20 mg tablet single dose orally on Day 1.0 / 80 / 82 / 8
Panel B: Severe RIParticipants received Enlicitide Decanoate 20 mg tablet single dose orally on Day 1.0 / 80 / 82 / 8
Panel C: End-Stage Renal Disease (ESRD) on Hemodialysis (HD)Participants received Enlicitide Decanoate 20 mg tablet orally on Day 1 and Day 16.0 / 91 / 90 / 9
Panel D: Healthy ControlsParticipants received Enlicitide Decanoate 20 mg tablet single dose orally on Day 1.0 / 80 / 80 / 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 85 Years
Healthy volunteers
Accepted
Inclusion and exclusion criteria, as posted
Inclusion Criteria: * Be in good health with the exception of renal impairment (RI) and hypercholesterolemia for participants in Panels A, B, and C. Participants with RI that have stable, chronic medical or psychiatric conditions, including but not limited to hypertension, hypercholesterolemia, diabetes mellitus, hyper- or hypothyroidism, gout, and chronic anxiety or depression may be included at the discretion of the investigator * Body Mass Index (BMI) ≥ 18 kg/m\^2 and ≤ 40 kg/m\^2, inclusive * Be on a stable dose of any statin therapy defined as: no changes to dose or type of statin therapy for at least 2 months prior to Screening and participant anticipates no changes to statin therapy throughout the study until the poststudy visit Exclusion Criteria: * History or presence of renal artery stenosis * Had a functioning renal transplant in the past 5 years and is taking transplant medication * Participants in panels A, B and D: Has rapidly fluctuating renal function as determined by historical measurements * Has a history gastrointestinal disease which might affect food and drug absorption, as determined by the investigator, or has had gastric bypass or similar surgery * History of cancer (malignancy) * History of significant multiple and/or severe allergies, or has had an anaphylactic reaction or significant intolerability to prescription or nonprescription drugs or food * Has received an anti-proprotein convertase subtilisin/kexin type 9 (PCSK9) small molecule treatment, monoclonal antibody, or short interfering RNA (siRNA) or RNA interference (ie, Inclisiran) within 12 months prior to Screening * Participants with RI (Panels A, B, and C): Taking medications to treat chronic medical conditions and/or conditions associated with renal disease, if participant has not been on a stable regimen for at least 1 month (other than statins, which require a stable dose for at least 2 months) prior to administration of the initial dose of study intervention, and/or is unable to withhold the use of the medication(s) within 4 hours prior to and 4 hours after administration of study intervention * Participated in another investigational study within 4 weeks prior to the prestudy (screening) visit * Consumes greater than 3 servings of alcoholic beverages per day * Consumes excessive amounts, defined as greater than 6 servings of caffeinated beverages per day

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