Phase 1
Completed N=16
A Single Dose Study of the Safety, Pharmacokinetics and Pharmacodynamics of MK-1064 (MK-1064-001)
Pharmacokinetics
Source: ClinicalTrials.gov NCT02549014 ↗
Enrolled (actual)
16
Serious AEs
1.3%
Results posted
Jan 2016
Primary outcomePrimary: Number of Participants Who Experienced One or More Adverse Events (AEs) — 4; 5; 5; 5 Participants
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.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Number of Participants Who Experienced One or More Adverse Events (AEs) |
4; 5; 5; 5; 5; 5 | — |
| PRIMARY Number of Participants Who Discontinued Study Due to an AE |
0; 0; 0; 0; 0; 0 | — |
| 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 |
0.77; 1.01; 2.99; 5.51; 9.75; 10.28 | — |
| SECONDARY 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; 1.67; 5.32; 9.89; 23.12; 25.92 | — |
| SECONDARY Maximum Observed Plasma Concentration (Cmax) Following Single Doses of MK-1064 |
0.37; 0.42; 1.06; 2.09; 3.60; 3.83 | — |
| SECONDARY Time to Cmax (Tmax) Following Single Doses of MK-1064 |
1.0; 1.5; 1.5; 2.0; 2.0; 1.0 | — |
| SECONDARY Apparent Terminal Half-life (t1/2) Following Single Doses of MK-1064 |
NA; NA; NA; NA; 11.1; 6.8 | — |
Eligibility Criteria
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
Data sourced from ClinicalTrials.gov (NCT02549014). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.