Pharmacokinetics
Conditions
Brief summary
The purpose of this randomized, double-blind, placebo-controlled study is to evaluate the safety, pharmacokinetics and pharmacodynamics of rising, single oral doses MK-1064 in healthy, young, male participants. The primary pharmacokinetic hypothesis is that at least one dose of MK-1064 that is generally safe and well tolerated produces an average MK-1064 plasma concentration from 0 to 4 hours of ≥2.2 μM. Since this is an early Phase I assessment of MK-1064 in humans, the study protocol allows for modifications to the outlined dose, dosing regimen and/or clinical or laboratory procedures, if required to address study objectives and/or to ensure appropriate safety monitoring of participants.
Detailed description
Two panels (Panels A and B), will receive alternating single rising oral doses of MK-1064/placebo (i.e., order of administration will be Panel A 5 mg, Panel B 10 mg, Panel A 25 mg, Panel B 50 mg, and continuing in this alternating sequence). Following dosing for a given treatment period, a minimum of 3 days will elapse before administration of the next scheduled dose. After administration of each dose, safety and tolerability will be reviewed. The decision to proceed to the next Panel/Period in the alternating sequence will be contingent on acceptable safety and tolerability data from the preceding Panels/Periods.
Interventions
DRUGMK-1064
Dose for each period administered as oral MK-1064 tablets (1, 10 and 50 mg strengths)
DRUGPlacebo
Dose for each period administered as oral placebo tablets matching active MK-1064 tablets
Sponsors
Merck Sharp & Dohme LLC
Study design
Allocation
RANDOMIZED
Intervention model
PARALLEL
Primary purpose
TREATMENT
Masking
DOUBLE (Subject, Investigator)
Eligibility
Sex/Gender
MALE
Age
18 Years to 45 Years
Healthy volunteers
Yes
Inclusion criteria
* Body Mass Index (BMI) ≤31 kg/m\^2 * In good health based on medical history, physical examination, vital sign measurements, and laboratory safety tests * Nonsmoker and has not used nicotine or nicotine-containing products for at least approximately 6 months
Exclusion criteria
* Mentally or legally incapacitated, significant emotional problems at screening or expected during the conduct of the study or history of a clinically significant psychiatric disorder within the last 10 years * History of any persistent sleep abnormality (including difficulty falling asleep, difficulty staying asleep) lasting for 3 months or more, or history of obstructive sleep apnea, restless legs syndrome, or narcolepsy of any duration * Participant has experienced poor quality sleep (including difficulty falling asleep, difficulty staying asleep) for at least 4 of 7 nights per week in the past 30 days prior to screening * Participant works a night shift and is not able to avoid night shift work a minimum of 1 week before each treatment period * Participant has traveled across 3 or more time zones (transmeridian travel) in the last 2 weeks prior to study * Unwilling or unable to consume a standard high fat breakfast * History of clinically significant endocrine, gastrointestinal, cardiovascular, hematological, hepatic, immunological, renal, respiratory, or genitourinary abnormalities or diseases * History of seizures, epilepsy, stroke, peripheral neuropathy, or other clinically significant neurological disease or cognitive impairment * History of cancer * History of cataplexy * Participant is unable to refrain from or anticipates the use of any medication, including prescription and non-prescription drugs or herbal remedies, beginning approximately 2 weeks prior to administration of the initial dose of study drug and throughout the study * Participant consumes \>3 servings of alcohol a day * Participant consumes \>6 caffeine servings a day * Participant has had major surgery, donated or lost 1 unit of blood (approximately 500 mL) or participated in another investigational study within 4 weeks prior to screening * History of significant multiple and/or severe allergies or has had an anaphylactic reaction or significant intolerability to prescription or non-prescription drugs or food * Is currently a regular user of any illicit drugs or has a history of drug (including alcohol) abuse within 2 years of screening * Is a regular user of sedative-hypnotic agents
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Number of Participants Who Experienced One or More Adverse Events (AEs) | Up to 14 days after the last dose of study drug (Up to approximately 60 days) | An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of study drug, whether or not considered related to the use of study drug. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a pre-existing condition which is temporally associated with the use of study drug, is also an AE. |
| Number of Participants Who Discontinued Study Due to an AE | Up to 14 days after the last dose of study drug (Up to approximately 60 days) | An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of study drug, whether or not considered related to the use of study drug. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a pre-existing condition which is temporally associated with the use of study drug, is also an AE. |
| Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064 | Pre-dose and 0.5, 1, 2, 3 and 4 hours post-dose | AUC0-4hr is the area under the plasma concentration-time curve from time 0 to 4 hours post-dose. This is a measure of the average amount of study drug (MK-1064) in the blood plasma over a period of 4 hours after the dose. |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064 | Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post dose (all Periods); 72 hours post-dose (Periods 3 and 4 only) | AUC0-last is the area under the plasma concentration-time curve from time zero to time of last measurable concentration. It is is a measure of the amount of study drug (MK-1064) in the blood plasma from pre-dose until the last measurable concentration of study drug could be determined. |
| Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 | Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post dose (all Periods); 72 hours post dose (Periods 3 and 4 only) | t1/2 is the elimination half-life of study drug. t1/2 is the time it takes for half of the study drug (MK-1064) in the blood plama to dissipate. |
| Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 | Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post dose (all Periods); 72 hours post dose (Periods 3 and 4 only) | Cmax is the maximum (peak) concentration of study drug (MK-1064) observed in blood plasma. |
| Time to Cmax (Tmax) Following Single Doses of MK-1064 | Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post dose (all Periods); 72 hours post dose (Periods 3 and 4 only) | Tmax is the amount of time to reach maximum (peak) plasma drug concentration following drug administration. |
Participant flow
Recruitment details
Healthy male participants aged 18-45 years (inclusive) were recruited for this study.
Participants by arm
| Arm | Count |
|---|---|
| Panel A: MK-1064 Panel A: Eight (8) participants were included in this panel. Within each of up to 5 treatment periods, 6 participants were randomly assigned to receive single oral doses of MK-1064 and 2 participants were randomly assigned to receive single oral doses of matching placebo. MK-1064 was administered in rising single doses of 5, 25, 100 and 200 mg over Periods 1-4, in the morning with participants in a fasted condition. In Period 5, a single MK-1064 dose of 25 mg or placebo was administered to participants in the morning following a standard high-fat breakfast. Dosing periods alternated with Panel B. There was to be a minimum 7-day washout between treatment periods for any given participant. | 8 |
| Panel B: MK-1064 Panel B: Eight (8) participants were included in this panel. Within each of up to 5 treatment periods, 6 participants were randomly assigned to receive single oral doses of MK-1064 and 2 participants were randomly assigned to receive single oral doses of matching placebo. MK-1064 was administered in rising single doses of 10, 50, 150 and 250 mg over Periods 1-4, in the morning with participants in fasted condition. In Period 5, a single MK-1064 dose of 50 mg or placebo was administered to participants in the evening after a 4-hour fast. Dosing periods alternated with Panel A. There was to be a minimum 7 day wash-out between treatment periods for any given participant. | 8 |
| Total | 16 |
Baseline characteristics
| Characteristic | Panel A: MK-1064 | Panel B: MK-1064 | Total |
|---|---|---|---|
| Age, Categorical <=18 years | 0 Participants | 0 Participants | 0 Participants |
| Age, Categorical >=65 years | 0 Participants | 0 Participants | 0 Participants |
| Age, Categorical Between 18 and 65 years | 8 Participants | 8 Participants | 16 Participants |
| Sex: Female, Male Female | 0 Participants | 0 Participants | 0 Participants |
| Sex: Female, Male Male | 8 Participants | 8 Participants | 16 Participants |
Adverse events
| Event type | EG000 affected / at risk | EG001 affected / at risk | EG002 affected / at risk | EG003 affected / at risk | EG004 affected / at risk | EG005 affected / at risk | EG006 affected / at risk | EG007 affected / at risk | EG008 affected / at risk | EG009 affected / at risk | EG010 affected / at risk |
|---|---|---|---|---|---|---|---|---|---|---|---|
| deaths Total, all-cause mortality | — / — | — / — | — / — | — / — | — / — | — / — | — / — | — / — | — / — | — / — | — / — |
| other Total, other adverse events | 4 / 6 | 5 / 6 | 5 / 6 | 5 / 6 | 5 / 6 | 5 / 6 | 6 / 6 | 6 / 6 | 3 / 6 | 3 / 6 | 5 / 16 |
| serious Total, serious adverse events | 0 / 6 | 0 / 6 | 0 / 6 | 0 / 6 | 0 / 6 | 0 / 6 | 0 / 6 | 0 / 6 | 1 / 6 | 0 / 6 | 0 / 16 |
Outcome results
Primary
Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064
AUC0-4hr is the area under the plasma concentration-time curve from time 0 to 4 hours post-dose. This is a measure of the average amount of study drug (MK-1064) in the blood plasma over a period of 4 hours after the dose.
Time frame: Pre-dose and 0.5, 1, 2, 3 and 4 hours post-dose
Population: All participants who received ≥1 dose of MK-1064.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Panel A: MK-1064 5 mg | Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064 | 0.77 µmol*hr/L | Standard Deviation 0.13 |
| Panel B: MK-1064 10 mg | Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064 | 1.01 µmol*hr/L | Standard Deviation 0.42 |
| Panel A: MK-1064 25 mg | Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064 | 2.99 µmol*hr/L | Standard Deviation 0.41 |
| Panel B: MK-1064 50 mg | Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064 | 5.51 µmol*hr/L | Standard Deviation 2.29 |
| Panel A: MK-1064 100 mg | Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064 | 9.75 µmol*hr/L | Standard Deviation 1.31 |
| Panel B: MK-1064 150 mg | Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064 | 10.28 µmol*hr/L | Standard Deviation 3.42 |
| Panel A: MK-1064 200 mg | Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064 | 20.12 µmol*hr/L | Standard Deviation 9.03 |
| Panel B: MK-1064 250 mg | Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064 | 22.70 µmol*hr/L | Standard Deviation 7.98 |
| Panel A: MK-1064 25 mg (Fed) | Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064 | 1.61 µmol*hr/L | Standard Deviation 0.25 |
| Panel B: MK-1064 50 mg (Night) | Average Plasma Concentration From Time Zero to 4 Hours (Area Under the Plasma Drug Concentration-time Curve From Time Zero to 4 Hours [AUC0-4hr]) Following Single Doses of MK-1064 | 5.16 µmol*hr/L | Standard Deviation 2.6 |
Primary
Number of Participants Who Discontinued Study Due to an AE
An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of study drug, whether or not considered related to the use of study drug. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a pre-existing condition which is temporally associated with the use of study drug, is also an AE.
Time frame: Up to 14 days after the last dose of study drug (Up to approximately 60 days)
Population: All participants who received ≥1 dose of study drug.
| Arm | Measure | Value (NUMBER) |
|---|---|---|
| Panel A: MK-1064 5 mg | Number of Participants Who Discontinued Study Due to an AE | 0 Participants |
| Panel B: MK-1064 10 mg | Number of Participants Who Discontinued Study Due to an AE | 0 Participants |
| Panel A: MK-1064 25 mg | Number of Participants Who Discontinued Study Due to an AE | 0 Participants |
| Panel B: MK-1064 50 mg | Number of Participants Who Discontinued Study Due to an AE | 0 Participants |
| Panel A: MK-1064 100 mg | Number of Participants Who Discontinued Study Due to an AE | 0 Participants |
| Panel B: MK-1064 150 mg | Number of Participants Who Discontinued Study Due to an AE | 0 Participants |
| Panel A: MK-1064 200 mg | Number of Participants Who Discontinued Study Due to an AE | 0 Participants |
| Panel B: MK-1064 250 mg | Number of Participants Who Discontinued Study Due to an AE | 0 Participants |
| Panel A: MK-1064 25 mg (Fed) | Number of Participants Who Discontinued Study Due to an AE | 0 Participants |
| Panel B: MK-1064 50 mg (Night) | Number of Participants Who Discontinued Study Due to an AE | 0 Participants |
| Panels A & B: Placebo | Number of Participants Who Discontinued Study Due to an AE | 0 Participants |
Primary
Number of Participants Who Experienced One or More Adverse Events (AEs)
An AE is defined as any unfavorable and unintended change in the structure, function, or chemistry of the body temporally associated with the use of study drug, whether or not considered related to the use of study drug. Any worsening (i.e., any clinically significant adverse change in frequency and/or intensity) of a pre-existing condition which is temporally associated with the use of study drug, is also an AE.
Time frame: Up to 14 days after the last dose of study drug (Up to approximately 60 days)
Population: All participants who received ≥1 dose of study drug.
| Arm | Measure | Value (NUMBER) |
|---|---|---|
| Panel A: MK-1064 5 mg | Number of Participants Who Experienced One or More Adverse Events (AEs) | 4 Participants |
| Panel B: MK-1064 10 mg | Number of Participants Who Experienced One or More Adverse Events (AEs) | 5 Participants |
| Panel A: MK-1064 25 mg | Number of Participants Who Experienced One or More Adverse Events (AEs) | 5 Participants |
| Panel B: MK-1064 50 mg | Number of Participants Who Experienced One or More Adverse Events (AEs) | 5 Participants |
| Panel A: MK-1064 100 mg | Number of Participants Who Experienced One or More Adverse Events (AEs) | 5 Participants |
| Panel B: MK-1064 150 mg | Number of Participants Who Experienced One or More Adverse Events (AEs) | 5 Participants |
| Panel A: MK-1064 200 mg | Number of Participants Who Experienced One or More Adverse Events (AEs) | 6 Participants |
| Panel B: MK-1064 250 mg | Number of Participants Who Experienced One or More Adverse Events (AEs) | 6 Participants |
| Panel A: MK-1064 25 mg (Fed) | Number of Participants Who Experienced One or More Adverse Events (AEs) | 3 Participants |
| Panel B: MK-1064 50 mg (Night) | Number of Participants Who Experienced One or More Adverse Events (AEs) | 3 Participants |
| Panels A & B: Placebo | Number of Participants Who Experienced One or More Adverse Events (AEs) | 5 Participants |
Secondary
Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064
t1/2 is the elimination half-life of study drug. t1/2 is the time it takes for half of the study drug (MK-1064) in the blood plama to dissipate.
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post dose (all Periods); 72 hours post dose (Periods 3 and 4 only)
Population: All participants who received ≥1 dose of MK-1064.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Panel A: MK-1064 5 mg | Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 | NA hr | — |
| Panel B: MK-1064 10 mg | Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 | NA hr | — |
| Panel A: MK-1064 25 mg | Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 | NA hr | — |
| Panel B: MK-1064 50 mg | Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 | NA hr | — |
| Panel A: MK-1064 100 mg | Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 | 11.1 hr | Standard Deviation 5 |
| Panel B: MK-1064 150 mg | Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 | 6.8 hr | Standard Deviation 3.2 |
| Panel A: MK-1064 200 mg | Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 | 7.5 hr | Standard Deviation 1.6 |
| Panel B: MK-1064 250 mg | Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 | 8.6 hr | Standard Deviation 2.7 |
| Panel A: MK-1064 25 mg (Fed) | Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 | NA hr | — |
| Panel B: MK-1064 50 mg (Night) | Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 | NA hr | — |
Secondary
Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064
AUC0-last is the area under the plasma concentration-time curve from time zero to time of last measurable concentration. It is is a measure of the amount of study drug (MK-1064) in the blood plasma from pre-dose until the last measurable concentration of study drug could be determined.
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post dose (all Periods); 72 hours post-dose (Periods 3 and 4 only)
Population: All participants who received ≥1 dose of MK-1064.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Panel A: MK-1064 5 mg | Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064 | 0.94 µmol*hr/L | Standard Deviation 0.25 |
| Panel B: MK-1064 10 mg | Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064 | 1.67 µmol*hr/L | Standard Deviation 0.52 |
| Panel A: MK-1064 25 mg | Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064 | 5.32 µmol*hr/L | Standard Deviation 0.71 |
| Panel B: MK-1064 50 mg | Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064 | 9.89 µmol*hr/L | Standard Deviation 3.8 |
| Panel A: MK-1064 100 mg | Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064 | 23.12 µmol*hr/L | Standard Deviation 6.23 |
| Panel B: MK-1064 150 mg | Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064 | 25.92 µmol*hr/L | Standard Deviation 6.03 |
| Panel A: MK-1064 200 mg | Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064 | 53.37 µmol*hr/L | Standard Deviation 13.78 |
| Panel B: MK-1064 250 mg | Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064 | 57.10 µmol*hr/L | Standard Deviation 21.98 |
| Panel A: MK-1064 25 mg (Fed) | Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064 | 5.27 µmol*hr/L | Standard Deviation 1.13 |
| Panel B: MK-1064 50 mg (Night) | Area Under the Plasma Drug Concentration-time Curve From Time Zero to Last Measurable Concentration (AUC0-last) Following Single Doses of MK-1064 | 9.91 µmol*hr/L | Standard Deviation 4.32 |
Secondary
Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064
Cmax is the maximum (peak) concentration of study drug (MK-1064) observed in blood plasma.
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post dose (all Periods); 72 hours post dose (Periods 3 and 4 only)
Population: All participants who received ≥1 dose of MK-1064.
| Arm | Measure | Value (GEOMETRIC_MEAN) | Dispersion |
|---|---|---|---|
| Panel A: MK-1064 5 mg | Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 | 0.37 µmol/L | Standard Deviation 0.07 |
| Panel B: MK-1064 10 mg | Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 | 0.42 µmol/L | Standard Deviation 0.16 |
| Panel A: MK-1064 25 mg | Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 | 1.06 µmol/L | Standard Deviation 0.22 |
| Panel B: MK-1064 50 mg | Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 | 2.09 µmol/L | Standard Deviation 0.77 |
| Panel A: MK-1064 100 mg | Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 | 3.60 µmol/L | Standard Deviation 0.85 |
| Panel B: MK-1064 150 mg | Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 | 3.83 µmol/L | Standard Deviation 1.46 |
| Panel A: MK-1064 200 mg | Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 | 6.78 µmol/L | Standard Deviation 3.52 |
| Panel B: MK-1064 250 mg | Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 | 8.28 µmol/L | Standard Deviation 2.87 |
| Panel A: MK-1064 25 mg (Fed) | Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 | 0.80 µmol/L | Standard Deviation 0.13 |
| Panel B: MK-1064 50 mg (Night) | Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 | 1.99 µmol/L | Standard Deviation 0.64 |
Secondary
Time to Cmax (Tmax) Following Single Doses of MK-1064
Tmax is the amount of time to reach maximum (peak) plasma drug concentration following drug administration.
Time frame: Pre-dose and 0.5, 1, 2, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post dose (all Periods); 72 hours post dose (Periods 3 and 4 only)
Population: All participants who received ≥1 dose of MK-1064.
| Arm | Measure | Value (MEDIAN) | Dispersion |
|---|---|---|---|
| Panel A: MK-1064 5 mg | Time to Cmax (Tmax) Following Single Doses of MK-1064 | 1.0 hr | Full Range 0.07 |
| Panel B: MK-1064 10 mg | Time to Cmax (Tmax) Following Single Doses of MK-1064 | 1.5 hr | Full Range 0.16 |
| Panel A: MK-1064 25 mg | Time to Cmax (Tmax) Following Single Doses of MK-1064 | 1.5 hr | Full Range 0.22 |
| Panel B: MK-1064 50 mg | Time to Cmax (Tmax) Following Single Doses of MK-1064 | 2.0 hr | Full Range 0.77 |
| Panel A: MK-1064 100 mg | Time to Cmax (Tmax) Following Single Doses of MK-1064 | 2.0 hr | Full Range 0.85 |
| Panel B: MK-1064 150 mg | Time to Cmax (Tmax) Following Single Doses of MK-1064 | 1.0 hr | Full Range 1.46 |
| Panel A: MK-1064 200 mg | Time to Cmax (Tmax) Following Single Doses of MK-1064 | 2.0 hr | Full Range 3.52 |
| Panel B: MK-1064 250 mg | Time to Cmax (Tmax) Following Single Doses of MK-1064 | 2.0 hr | Full Range 2.87 |
| Panel A: MK-1064 25 mg (Fed) | Time to Cmax (Tmax) Following Single Doses of MK-1064 | 5.0 hr | Full Range 0.13 |
| Panel B: MK-1064 50 mg (Night) | Time to Cmax (Tmax) Following Single Doses of MK-1064 | 2.0 hr | Full Range 0.64 |