A Phase 1 interventional study of Preladenant in Chronic Hepatic Impairment, sponsored by Merck Sharp & Dohme LLC. Completed. Open to participants aged 18 Years to 70 Years, including healthy volunteers. Per ClinicalTrials.gov, last updated 2018-09-24.
Sponsored by Merck Sharp & Dohme LLC · Phase 1, Interventional, and Treatment
The purpose of this study is to compare the pharmacokinetics (PK) of preladenant after administration of a single 5 mg oral dose of preladenant in participants with hepatic impairment and healthy volunteers. Part 1 of this study compares healthy volunteers with participants with mild hepatic impairment. Part 2 compares healthy volunteers with participants with moderate hepatic impairment. Healthy volunteers in each part of this study are to be matched with participants with hepatic impairment by race, age, gender, and body mass index (BMI). The primary hypotheses are that in participants with mild or moderate HI, the area under the concentration-time curve from time 0 extrapolated to time of the last quantifiable concentration (AUC0-t) of preladenant is similar to that observed in matched healthy volunteers, so that the mean ratio of hepatic impaired/healthy is contained within the interval [0.50, 2.00].
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Key Inclusion Criteria for Healthy Participants Groups:
Key Inclusion Criteria for Hepatic Impaired Groups:
Key Exclusion Criteria
Participants with mild chronic liver disease enrolled in Part 1 received one 5-mg preladenant tablet, orally, on Day 1.
Drug: Preladenant
Healthy volunteers with normal hepatic function matched to participants with mild chronic liver disease by race, age, BMI, and gender, enrolled in Part 1 received one 5-mg preladenant tablet, orally, on Day 1.
Drug: Preladenant
Participants with moderate chronic liver disease enrolled in Part 2 received one 5-mg preladenant tablet, orally, on Day 1.
Drug: Preladenant
Healthy volunteers with normal hepatic function matched to participants with moderate chronic liver disease by race, age, BMI, and gender, enrolled in Part 2 received one 5-mg preladenant tablet, orally, on Day 1.
Drug: Preladenant
After at least an 8 hours overnight fast, one 5-mg preladenant tablet, is administered orally, on Day 1.
Also known as: SCH 420814, MK-3814, Adenosine 2a Antagonist
Area Under the Plasma Concentration-time Curve From Time 0 Extrapolated to Time of the Last Quantifiable Concentration (AUC 0-t) of Preladenant After a Single Dose of Preladenant
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the AUC 0-t of preladenant.
Time frame: Pre-dose up to 72 hours postdose
Maximum Observed Plasma Concentration (Cmax) of Preladenant After a Single Dose of Preladenant
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the Cmax of preladenant.
Time frame: Pre-dose up to 72 hours postdose
AUC 0-t of Preladenant Metabolite SCH 434748 After a Single Dose of Preladenant
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the AUC 0-t of SCH 434748.
Time frame: Pre-dose up to 72 hours postdose
Cmax of Preladenant Metabolite SCH 434748 After a Single Dose of Preladenant
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the Cmax of SCH 434748.
Time frame: Pre-dose up to 72 hours postdose
AUC 0-t of Preladenant Metabolite SCH 446637 After a Single Dose of Preladenant
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the AUC 0-t of SCH 446637.
Time frame: Pre-dose up to 72 hours postdose
Cmax of Preladenant Metabolite SCH 446637 After a Single Dose of Preladenant
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the Cmax of SCH 446637.
Time frame: Pre-dose up to 72 hours postdose
AUC 0-t of Preladenant Calculated Using Free Drug Concentration After a Single Dose of Preladenant
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the AUC 0-t of preladenant calculated using free drug concentration.
Time frame: Pre-dose up to 72 hours postdose
Cmax of Preladenant Calculated Using Free Drug Concentration After a Single Dose of Preladenant
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the Cmax of preladenant calculated using free drug concentration.
Time frame: Pre-dose up to 72 hours postdose
| Milestone | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 |
|---|---|---|---|---|
| Started | 12 | 12 | 9 | 9 |
| Completed | 12 | 12 | 9 | 9 |
| Not completed | 0 | 0 | 0 | 0 |
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the AUC 0-t of preladenant.
| hr*ng/mL | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 |
|---|---|---|---|---|
| Area Under the Plasma Concentration-time Curve From Time 0 Extrapolated to Time of the Last Quantifiable Concentration (AUC 0-t) of Preladenant After a Single Dose of Preladenant | 97.864 (33.181 to 304.594) | 91.014 (27.457 to 171.810) | 300.667 (81.081 to 571.197) | 115.715 (16.816 to 352.507) |
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the Cmax of preladenant.
| ng/mL | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 |
|---|---|---|---|---|
| Maximum Observed Plasma Concentration (Cmax) of Preladenant After a Single Dose of Preladenant | 39.380 (15.900 to 61.500) | 30.171 (5.890 to 73.200) | 56.997 (8.950 to 109.00) | 39.735 (4.130 to 113.00) |
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the AUC 0-t of SCH 434748.
| hr*ng/mL | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 |
|---|---|---|---|---|
| AUC 0-t of Preladenant Metabolite SCH 434748 After a Single Dose of Preladenant | 28.505 (17.858 to 60.434) | 15.395 (0.156 to 45.462) | 60.486 (17.213 to 96.253) | 25.288 (6.399 to 149.982) |
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the Cmax of SCH 434748.
| ng/mL | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 |
|---|---|---|---|---|
| Cmax of Preladenant Metabolite SCH 434748 After a Single Dose of Preladenant | 10.503 (5.280 to 20.400) | 6.784 (0.624 to 21.400) | 13.983 (4.530 to 52.700) | 9.936 (2.970 to 54.500) |
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the AUC 0-t of SCH 446637.
| hr*ng/mL | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 |
|---|---|---|---|---|
| AUC 0-t of Preladenant Metabolite SCH 446637 After a Single Dose of Preladenant | 38.262 (18.636 to 87.772) | 24.612 (0.149 to 84.837) | 170.215 (55.366 to 491.013) | 35.421 (10.783 to 70.257) |
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the Cmax of SCH 446637.
| ng/mL | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 |
|---|---|---|---|---|
| Cmax of Preladenant Metabolite SCH 446637 After a Single Dose of Preladenant | 12.691 (6.470 to 29.100) | 10.004 (0.595 to 24.000) | 21.761 (9.840 to 45.600) | 10.993 (4.910 to 21.400) |
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the AUC 0-t of preladenant calculated using free drug concentration.
| hr*ng/mL | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 |
|---|---|---|---|---|
| AUC 0-t of Preladenant Calculated Using Free Drug Concentration After a Single Dose of Preladenant | 1.605 (0.547 to 6.396) | 1.211 (0.261 to 3.295) | 6.792 (1.133 to 15.708) | 1.681 (0.202 to 6.757) |
For healthy and HI participants blood samples were collected at pre-dose (0 hour) and at 0.50, 1, 2, 4, 6, 12, 16, 24, 30, 36, and 48 hours postdose. Blood samples were also collected for HI participants only at 60 and 72 hours postdose in order to determine the Cmax of preladenant calculated using free drug concentration.
| ng/mL | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 |
|---|---|---|---|---|
| Cmax of Preladenant Calculated Using Free Drug Concentration After a Single Dose of Preladenant | 0.646 (0.223 to 1.412) | 0.401 (0.130 to 1.129) | 1.288 (0.255 to 2.787) | 0.577 (0.050 to 2.184) |
Collected over Up to 7 days. Non-serious events are listed at a 5% frequency threshold.
| Group | Deaths | Serious | Other |
|---|---|---|---|
| Mild Hepatic Impaired (HI) Part 1 | — | 0/12 (0%) | 2/12 (16.7%) |
| Healthy to Match Mild HI Part 1 | — | 0/12 (0%) | 0/12 (0%) |
| Moderate HI Part 2 | — | 0/9 (0%) | 1/9 (11.1%) |
| Healthy to Match Moderate HI Part 2 | — | 0/9 (0%) | 1/9 (11.1%) |
| Event | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 |
|---|---|---|---|---|
| ToothacheGastrointestinal disorders | 0/12 | 0/12 | 0/9 | 1/9 |
| DyskinesiaNervous system disorders | 0/12 | 0/12 | 1/9 | 0/9 |
| ConstipationGastrointestinal disorders | 1/12 | 0/12 | 0/9 | 0/9 |
| HeadacheNervous system disorders | 1/12 | 0/12 | 0/9 | 0/9 |
Randomized participants
| Age, Continuous(Years) | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 | Total |
|---|---|---|---|---|---|
| Mean | 55.3 ± 6.5 | 52.3 ± 7.1 | 52.2 ± 4.8 | 50.1 ± 3.3 | 52.7 ± 5.9 |
| Sex: Female, Male(Participants) | Mild Hepatic Impaired (HI) Part 1 | Healthy to Match Mild HI Part 1 | Moderate HI Part 2 | Healthy to Match Moderate HI Part 2 | Total |
|---|---|---|---|---|---|
| Female | 0 | 0 | 4 | 4 | 8 |
| Male | 12 | 12 | 5 | 5 | 34 |
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Plan to share: Yes — https://www.merck.com/clinical-trials/pdf/ProcedureAccessClinicalTrialData.pdf
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