Drug-Drug Interaction Study to Evaluate the Effects of Ecopipam on the Pharmacokinetics of Multiple Substrates for Drug Metabolism and Transport

A Phase 1, Open-Label, Fixed Sequence, Drug-Drug Interaction Study to Evaluate the Effects of Repeat Titrated Doses of Ecopipam on the Pharmacokinetics of Multiple Substrates for Drug Metabolism and Transport in Healthy Subjects

This is a single center, open-label, fixed sequence Phase 1, drug-drug interaction (DDI) study in healthy subjects.

Study Overview

• Status: Completed
• Conditions: Drug Interaction
• Intervention / Treatment: Drug: Ecopipam; Combination product: Cohort 1 Probe Substrate Cocktail; Drug: Cohort 2 Probe Substrate; Combination product: Cohort 3 Probe Substrate Cocktail

Detailed Description

Following a Screening period, eligible subjects will be enrolled sequentially to one of three cohorts to receive a single dose of probe substrate(s), followed by repeated titrated doses of ecopipam twice daily (BID) (with subjects in Cohort 3 also receiving a single dose of ecopipam and probe substrates on Day 4 prior to titration). After steady-state ecopipam dosing is reached, ecopipam will be co-administered with a single dose of probe substrate(s) (with continuation of ecopipam BID (every 12 h) dosing during the blood sampling period for the respective probe substrates), followed by an ecopipam tapering period and clinic discharge assessments.

• Study Type: Interventional
• Enrollment (Actual): 56
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Texas
    • San Antonio, Texas, United States, 78209
      • ICON Early Phase Services

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Male subjects or female subjects of non-childbearing potential
• ≥18 and <55 years of age at the time of consent
• BMI >18.5 and <30 kg/m2 and a weight of ≥50 kg for males or ≥45 kg for females
• Subjects must be healthy, as determined by the Investigator, based on medical history, physical examination, ECG, and standard panel of blood and laboratory tests at Screening.
• Sexually active males must use a double barrier method of contraception during the study and for at least 90 days after the last dose of study drug
• Male subjects must be willing not to donate sperm until 90 days following the last study drug administration

Exclusion Criteria:

• Personal or family History of significant medical illness
• Clinically significant abnormalities on screening tests/exams
• History of or significant risk of committing suicide
• Donation of plasma within 7 days prior to dosing
• Donation or significant loss of blood within 30 days prior to the first dosing
• Major surgery within 3 months or minor surgery within 1 month prior to admission
• Use of prohibited prescription, over-the-counter medications or natural health products
• Alcohol-based products 24 hours prior to admission
• Female subjects who are currently pregnant or lactating
• Positive pregnancy test
• Use of tobacco or nicotine products within 3 months prior to Screening
• Significant alcohol consumption
• History of drug abuse within the previous 2 years, or a positive drug screen
• History of allergy to study medications
• Undergoing abrupt discontinuation of alcohol or sedatives
• Not suitable for study in the opinion of the Principal Investigator

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Non-Randomized
• Interventional Model: Parallel Assignment
• Masking: None (Open Label)

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Other: Cohort 1; ecopipam HCl oral tablets of 12.5, 50, 75, and 100 mg daily for up to 20 days Cohort 1 Probe Substrate Cocktail given on 2 separate days: midazolam: 1 µg infused IV; caffeine: 200 mg oral tablet; omeprazole: two 20 mg oral tablets; dextromethorphan: 1.6mL (containing ~10 mg) oral solution	Drug: Ecopipam; ecopipam HCl ~2mg/kg/day; Combination product: Cohort 1 Probe Substrate Cocktail; dextromethorphan, caffeine, omeprazole, and midazolam
Other: Cohort 2; ecopipam HCl oral tablets of 12.5, 50, 75, and 100 mg daily for up to 20 days Cohort 2 Probe Substrate given on 2 separate days: - bupropion: 100mg oral tablet	Drug: Ecopipam; ecopipam HCl ~2mg/kg/day; Drug: Cohort 2 Probe Substrate; bupropion
Other: Cohort 3; ecopipam HCl oral tablets of 12.5, 50, 75, and 100 mg daily for up to 20 days Cohort 3 Probe Substrate Cocktail given on 3 separate days: midazolam: 10 µg/mL given as 1mL oral solution.; dabigatran: 375 µg/mL and pitavastatin: 10 µg/mL given as 1mL oral solution; rosuvastatin: 25 µg/mL and atorvastatin: 50 µg/mL given as 2mL oral solution	Drug: Ecopipam; ecopipam HCl ~2mg/kg/day; Combination product: Cohort 3 Probe Substrate Cocktail; dabigatran, pitavastatin, rosuvastatin, atorvastatin, midazolam

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax of IV midazolam (and its 1'-hydroxymidazolam metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax of IV midazolam (and its 1'-hydroxymidazolam metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax of oral midazolam (and its 1'-hydroxymidazolam metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax oral midazolam (and its 1'-hydroxymidazolam metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax of dabigatran in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax of dabigatran in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax of pitavastatin (and its pitavastatin lactone metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax of pitavastatin (and its pitavastatin lactone metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax of rosuvastatin in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax of rosuvastatin in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax of atorvastatin (and its 4'-hydroxy atorvastatin metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax of atorvastatin (and its 4'-hydroxy atorvastatin metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of IV midazolam (and its 1'-hydroxymidazolam metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of IV midazolam (and its 1'-hydroxymidazolam metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of oral midazolam (and its 1'-hydroxymidazolam metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of oral midazolam (and its 1'-hydroxymidazolam metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of dabigatran in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of dabigatran in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of pitavastatin (and its pitavastatin lactone metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of pitavastatin (and its pitavastatin lactone metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of rosuvastatin in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of rosuvastatin in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of atorvastatin (and its 4'-hydroxy atorvastatin metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of atorvastatin (and its 4'-hydroxy atorvastatin metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of IV midazolam (and its 1'-hydroxymidazolam metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of IV midazolam (and its 1'-hydroxymidazolam metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of oral midazolam (and its 1'-hydroxymidazolam metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of oral midazolam (and its 1'-hydroxymidazolam metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of dabigatran in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of dabigatran in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of pitavastatin (and its pitavastatin lactone metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of pitavastatin (and its pitavastatin lactone metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of rosuvastatin in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of rosuvastatin in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of atorvastatin (and its 4'-hydroxy atorvastatin metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of atorvastatin (and its 4'-hydroxy atorvastatin metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUC0-24 of oral midazolam (and its 1'-hydroxymidazolam metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUC0-24 of oral midazolam (and its 1'-hydroxymidazolam metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUC0-24 of dabigatran in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUC0-24 of dabigatran in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUC0-24 of pitavastatin (and its pitavastatin lactone metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUC0-24 of pitavastatin (and its pitavastatin lactone metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUC0-24 of rosuvastatin in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUC0-24 of rosuvastatin in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUC0-24 of atorvastatin (and its 4'-hydroxy atorvastatin metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUC0-24 of atorvastatin (and its 4'-hydroxy atorvastatin metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax of bupropion (and its 4-hydroxybupropion metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax of bupropion (and its 4-hydroxybupropion metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax omeprazole (and its 5'-hydroxy omeprazole metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Cmax omeprazole (and its 5'-hydroxy omeprazole metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of bupropion (and its 4-hydroxybupropion metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of bupropion (and its 4-hydroxybupropion metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of omeprazole (and its 5'-hydroxy omeprazole metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUCinf of omeprazole (and its 5'-hydroxy omeprazole metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of bupropion (and its 4-hydroxybupropion metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of bupropion (and its 4-hydroxybupropion metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of omeprazole (and its 5'-hydroxy omeprazole metabolite) in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
AUClast of omeprazole (and its 5'-hydroxy omeprazole metabolite) in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for dextromethorphan in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for dextromethorphan in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL for IV midazolam in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL for IV midazolam in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for oral midazolam in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for oral midazolam in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for dabigatran in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for dabigatran in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for pitavastatin in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for pitavastatin in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for rosuvastatin in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for rosuvastatin in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for atorvastatin in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for atorvastatin in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for bupropion in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for bupropion in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for caffeine in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for caffeine in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for omeprazole in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
CL/F for omeprazole in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for dextromethorphan in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for dextromethorphan in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V for IV midazolam in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V for IV midazolam in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for oral midazolam in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for oral midazolam in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for dabigatran in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for dabigatran in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for pitavastatin in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for pitavastatin in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for rosuvastatin in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for rosuvastatin in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for bupropion in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for bupropion in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for atorvastatin in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for atorvastatin in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for caffeine in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for caffeine in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for omeprazole in the presence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
V/F for omeprazole in the absence of ecopipam	Up to 46 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 22
Total concentration of bilirubin in the presence of ecopipam	Bilirubin sampling will occur on Day 1 and Day 18	Up to Day 18
Total concentration of bilirubin in the absence of ecopipam	Bilirubin sampling will occur on Day 1 and Day 18	Up to Day 18
Unconjugated concentration of bilirubin in the presence of ecopipam	Bilirubin sampling will occur on Day 1 and Day 18	Up to Day 18
Unconjugated concentration of bilirubin in the absence of ecopipam	Bilirubin sampling will occur on Day 1 and Day 18	Up to Day 18
Conjugated concentration of bilirubin in the presence of ecopipam	Bilirubin sampling will occur on Day 1 and Day 18	Up to Day 18
Conjugated concentration of bilirubin in the absence of ecopipam	Bilirubin sampling will occur on Day 1 and Day 18	Up to Day 18
Average of the 6-hour plasma dextromethorphan: dextrorphan ratio in the presence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Average of the 8-hour plasma dextromethorphan: dextrorphan ratio in the presence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Average of the 12-hour plasma dextromethorphan: dextrorphan ratio in the presence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Average of the 6-hour plasma dextromethorphan: dextrorphan ratio in the absence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Average of the 8-hour plasma dextromethorphan: dextrorphan ratio in the absence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Average of the 12-hour plasma dextromethorphan: dextrorphan ratio in the absence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Average of the 6-hour plasma caffeine: paraxanthine metabolite ratio in the presence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Average of the 8-hour plasma caffeine: paraxanthine metabolite ratio in the presence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Average of the 12-hour plasma caffeine: paraxanthine metabolite ratio in the presence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Average of the 6-hour plasma caffeine: paraxanthine metabolite ratio in the absence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Average of the 8-hour plasma caffeine: paraxanthine metabolite ratio in the absence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Average of the 12-hour plasma caffeine: paraxanthine metabolite ratio in the absence of ecopipam	6 blood samples will be collected at the indicated time points for pharmacokinetic analysis	Up to Day 14
Safety and tolerability as demonstrated by the Modified Observer's Assessment of Alertness/Sedation (MOAA/S)	Score from 0-5 where 0 is no response and 5 is responds readily. MOAA/S measures will be recorded at the indicated timepoints	Up to Day 63
Safety and tolerability as demonstrated by the Columbia Suicide Severity Rating Scale (C-SSRS)	Safety and tolerability measures will be recorded at the indicated timepoints	Up to Day 63
Number of participants requiring concomitant medications	Participants will be continuously monitored for the use of concomitant medications	Up to Day 63
AEs with relatedness associated with dextromethorphan	Subjects will be continually monitored for adverse events	Up to Day 63
AEs with relatedness associated with IV midazolam	Subjects will be continually monitored for adverse events	Up to Day 63
AEs with relatedness associated with oral midazolam	Subjects will be continually monitored for adverse events	Up to Day 63
AEs with relatedness associated with dabigatran	Subjects will be continually monitored for adverse events	Up to Day 63
AEs with relatedness associated with pitavastatin	Subjects will be continually monitored for adverse events	Up to Day 63
AEs with relatedness associated with rosuvastatin	Subjects will be continually monitored for adverse events	Up to Day 63
AEs with relatedness associated with atorvastatin	Subjects will be continually monitored for adverse events	Up to Day 63
AEs with relatedness associated with bupropion	Subjects will be continually monitored for adverse events	Up to Day 63
AEs with relatedness associated with caffeine	Subjects will be continually monitored for adverse events	Up to Day 63
AEs with relatedness associated with omeprazole	Subjects will be continually monitored for adverse events	Up to Day 63
AEs with relatedness associated with ecopipam	Subjects will be continually monitored for adverse events	Up to Day 63
Absolute values of white blood cell (WBC), neutrophils, lymphocytes, monocytes, eosinophils, basophils and platelets (1000/mm3)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Absolute values of hematocrit (percent)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Absolute values of hemoglobin (g/dL)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Absolute values of Red blood cell (RBC) count (M/mm3)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Absolute values of sodium, potassium, chloride (mmol/L)	Blood samples will be collected for the assessment of clinical chemistry parameters	Up to Day 26
Absolute values of magnesium, urea, phosphorus, calcium, glucose, and total, conjugated and unconjugated bilirubin (mg/dL)	Blood samples will be collected for the assessment of clinical chemistry parameters	Up to Day 26
Absolute values of albumin and total protein (g/dL)	Blood samples will be collected for the assessment of clinical chemistry parameters	Up to Day 26
Absolute values of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), gamma glutamyl transferase (GGT), creatinine phosphokinase (CPK), and creatinine (U/L)	Blood samples will be collected for the assessment of clinical chemistry parameters	Up to Day 26
Absolute values of urine specific gravity	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Absolute values of urine pH	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Absolute values of urine glucose	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Absolute values of urine protein	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Absolute values of urine blood	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Absolute values of urine ketones	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Absolute values of urine bilirubin and nitrite	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Absolute values of urobilinogen (Eu/dL)	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Absolute values of urine leukocytes by dipstick	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Change from Day -1 to Day of Discharge white blood cell (WBC), neutrophils, lymphocytes, monocytes, eosinophils, basophils and platelets (1000/mm3)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Change from Day -1 to Day of Discharge in hematocrit (percent)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Change from Day -1 to Day of Discharge in hemoglobin (g/dL)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Change from Day -1 to Day of Discharge in Red blood cell (RBC) count (M/mm3)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Change from Day -1 to Day of Discharge in sodium, potassium, chloride (mmol/L)	Blood samples will be collected for the assessment of clinical chemistry parameters	Up to Day 26
Change from Day -1 to Day of Discharge in magnesium, urea, phosphorus, calcium, glucose, and total, conjugated and unconjugated bilirubin (mg/dL)	Blood samples will be collected for the assessment of clinical chemistry parameters	Up to Day 26
Change from Day -1 to Day of Discharge in albumin and total protein (g/dL)	Blood samples will be collected for the assessment of clinical chemistry parameters	Up to Day 26
Change from Day -1 to Day of Discharge in alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), gamma glutamyl transferase (GGT), and creatinine phosphokinase (CPK), and creatinine (U/L)	Blood samples will be collected for the assessment of clinical chemistry parameters	Up to Day 26
Change from Day -1 to Day of Discharge in urine specific gravity	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Change from Day -1 to Day of Discharge in urine pH	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Change from Day -1 to Day of Discharge in urine glucose	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Change from Day -1 to Day of Discharge in urine protein	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Change from Day -1 to Day of Discharge in urine blood	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Change from Day -1 to Day of Discharge in urine ketones	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Change from Day -1 to Day of Discharge in urine bilirubin and nitrite	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Change from Day -1 to Day of Discharge in urobilinogen (Eu/dL)	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Change from Day -1 to Day of Discharge in urine leukocytes by dipstick	Urine samples will be collected for the assessment of urine parameters	Up to Day 26
Absolute values of electrocardiogram (ECG) parameters: PR, QRS, QT, and QT interval corrected for heart rate using Fridericia's formula (QTcF) (Milliseconds)	Twelve-lead ECGs will be obtained with the participant in a supine position after a rest of at least 5 minutes using an automated ECG machine. PR, QRS, QT, and QTcF intervals will be measured	Up to Day 26
Change from pre-dose for the respective day in ECG parameters: PR, QRS, QT, and QTcF (Milliseconds)	Twelve-lead ECGs will be obtained with the participant in a supine position after a rest of at least 5 minutes using an automated ECG machine. PR, QRS, QT, and QTcF intervals will be measured	Up to Day 26
Absolute values of oral temperature (degrees Celsius)	Temperature will be assessed as part of vital signs	Up to Day 26
Change from pre-dose for the respective day in oral temperature (degrees Celsius)	Temperature will be assessed as part of vital signs	Up to Day 26
Absolute values of heart rate (beats/minute)	Heart rate will be assessed as part of vital signs	Up to Day 26
Change from pre-dose for the respective day in heart rate (beats/minute)	Heart rate will be assessed as part of vital signs	Up to Day 26
Absolute values of respiratory rate (breaths/minute)	Respiratory rate will be assessed as part of vital signs	Up to Day 26
Absolute values of systolic blood pressure (SBP) and diastolic blood pressure (DBP) (mmHG)	Blood pressure will be assessed as part of vital signs	Up to Day 26
Change from pre-dose for the respective day in SBP and DBP (mmHG)	Blood pressure will be assessed as part of vital signs	Up to Day 26
Absolute values of mean corpuscular hemoglobin (MCH) (pg)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Change from Day 1 to Day of Discharge of mean corpuscular hemoglobin (MCH) (pg)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Absolute values of mean corpuscular volume (MCV) (fL)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Change from Day 1 to Day of Discharge of mean corpuscular volume (MCV) (fL)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Absolute values of mean corpuscular hemoglobin concentration (MCHC) (g/dL)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26
Change from Day 1 to Day of Discharge of mean corpuscular hemoglobin concentration (MCHC) (g/dL)	Blood samples will be collected for the assessment of hematology parameters	Up to Day 26

Collaborators and Investigators

• Sponsor: Emalex Biosciences Inc.
• Collaborators: ICON Early Phase Services; Nuventra

Study record dates

Study Major Dates

• Study Start (Actual): April 26, 2022
• Primary Completion (Actual): August 1, 2022
• Study Completion (Actual): August 26, 2022

Study Registration Dates

• First Submitted: April 11, 2022
• First Submitted That Met QC Criteria: April 18, 2022
• First Posted (Actual): April 19, 2022

Study Record Updates

• Last Update Posted (Estimate): December 12, 2022
• Last Update Submitted That Met QC Criteria: December 9, 2022
• Last Verified: December 1, 2022

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Central Nervous System Depressants; Antipsychotic Agents; Tranquilizing Agents; Psychotropic Drugs; Dopamine Agents; Dopamine Antagonists; Ecopipam
• Other Study ID Numbers: EBS-101-HV-104

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: No

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: Yes
• Studies a U.S. FDA-regulated device product: No