MedPath

Drug Interaction Study

Phase 1
Completed
Conditions
Drug Interaction
Interventions
Registration Number
NCT06194864
Lead Sponsor
Emalex Biosciences Inc.
Brief Summary

This is a single center, 2-Part, Phase 1, open-label, fixed-sequence, drug-drug interaction study designed to compare the PK of ecopipam when administered alone and in combination with itraconazole (Part 1) or rifampicin (Part 2) in healthy subjects.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
45
Inclusion Criteria
  • Male subjects or femail subjects of non-childbearing potential
  • ≥18 and ≤55 years of age
  • BMI >18.5 and <30.0 kg/m2 and body weight ≥50.0 kg for males and ≥45.0 kg for females.
  • Subjects must be healthy, as determined by the Investigator, based on medical history, physical examination, ECG, vital signs, 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.
  • Willing to take off dentures or mouth piercing at the time of dosing.
Exclusion Criteria
  • 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 8 weeks 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
  • Female subjects who are currently pregnant or lactating
  • Positive pregnancy test
  • Positive urine drug screen, urine cotinine test, or alcohol breath test
  • Use of tobacco or nicotine products within 1 month prior to Screening
  • Significant alcohol consumption
  • History of drug abuse within the previous year, or a positive drug screen
  • History of allergy to study medications
  • Part 1 only: Presence of orthodontic braces or orthodontic retention wires
  • Recent participation in a clinical research study
  • Not suitable for study in the opinion of the Principal Investigator

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Part 1Itraconazoleecopipam 89.6 mg on Days 1 and 9 with repeat doses of itraconazole Days 6-16.
Part 1Ecopipamecopipam 89.6 mg on Days 1 and 9 with repeat doses of itraconazole Days 6-16.
Part 2rifampicinecopipam 179.2 mg on Days 1 and 13 with repeat doses of rifampicin days 6-20.
Part 2Ecopipamecopipam 179.2 mg on Days 1 and 13 with repeat doses of rifampicin days 6-20.
Primary Outcome Measures
NameTimeMethod
AUC0-inf of ecopipam when administered without rifampicinUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-t of ecopipam when administered with rifampicinUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-t of ecopipam when administered without rifampicinUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

Cmax of ecopipam when administered without itraconazoleUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

T½ el of ecopipam when administered with itraconazoleUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

T½ el of ecopipam when administered without itraconazoleUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-t of ecopipam when administered with itraconazoleUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-t of ecopipam when administered without itraconazoleUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-inf of ecopipam when administered with itraconazoleUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-inf of ecopipam when administered without itraconazoleUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-inf of ecopipam when administered with rifampicinUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

Cmax of ecopipam when administered with rifampicinUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

Cmax of ecopipam when administered with itraconazoleUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

Cmax of ecopipam when administered without rifampicinUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

T½ el of ecopipam when administered with rifampicinUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

T½ el of ecopipam when administered without rifampicinUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

Secondary Outcome Measures
NameTimeMethod
Safety and tolerability as demonstrated by AEs without itraconazoleUp to Day 30

Subjects will be continually monitored for adverse events

Safety and tolerability as demonstrated by AEs with rifampicinUp to Day 30

Subjects will be continually monitored for adverse events

Respiratory rate pressure with itraconazole (breaths/minute)Up to Day 21

Respiratory rate will be assessed as part of vital signs

Respiratory rate without itraconazole (breaths/minute)Up to Day 21

Respiratory rate will be assessed as part of vital signs

Respiratory rate with rifampicin (breaths/minute)Up to Day 21

Respiratory rate will be assessed as part of vital signs

T½ el of EBS-101-40853 glucuronideUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-4 for ecopipamUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-4 for EBS-101-40853Up to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-inf of EBS-101-40853Up to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-inf of ecopipam glucuronideUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

Heart rate without itraconazole (beats/minute)Up to Day 21

Heart rate will be assessed as part of vital signs

Heart rate with rifampicin (beats/minute)Up to Day 21

Heart rate will be assessed as part of vital signs

AUC0-inf of EBS-101-40853 glucuronideUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-t of EBS-101-40853Up to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

Cmax of EBS-101-40853Up to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

Cmax of ecopipam glucuronideUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

Cmax of EBS-101-40853 glucuronideUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

Safety and tolerability as demonstrated by Systolic blood pressure (SBP) and diastolic blood pressure (DBP) without rifampicin(mmHG)Up to Day 21

Blood pressure will be assessed as part of vital signs

Heart rate with itraconazole (beats/minute)Up to Day 21

Heart rate will be assessed as part of vital signs

Respiratory rate without rifampicin (breaths/minute)Up to Day 21

Respiratory rate will be assessed as part of vital signs

Oral temperature with itraconazole (degrees Celsius)Up to Day 21

Temperature will be assessed as part of vital signs

Electrocardiogram (ECG) parameters: PR, RR, QRS, QT, and QT interval corrected for heart rate using Fridericia's formula (QTcF) with itraconazole (Milliseconds)Up to Day 21

Twelve-lead ECGs will be obtained at the indicated timepoints

Electrocardiogram (ECG) parameters: PR, RR, QRS, QT, and QT interval corrected for heart rate using Fridericia's formula (QTcF) with rifampicin (Milliseconds)Up to Day 21

Twelve-lead ECGs will be obtained at the indicated timepoints

AUC0-t of ecopipam glucuronideUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-t of EBS-101-40853 glucuronideUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

T½ el of EBS-101-40853Up to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

T½ el of ecopipam glucuronideUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-4 for ecopipam glucuronideUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

AUC0-4 for EBS 101-40853 glucuronideUp to Day 21

Up to 38 samples will be collected at the indicated time points for pharmacokinetic analysis

Minimum Modified Observer's Assessment of Alertness/Sedation (MOAA/S) scoreUp to Day 21

Score from 0-5 where 0 is no response and 5 is responds readily. MOAA/S measures will be recorded at the indicated timepoints

AUEC for Visual Analogue Scale (VAS)Up to Day 21

Score from 0 - 100 where 0 is not sedated and 100 is very sedated. VAS measures will be recorded at the indicated timepoints.

Maximum sedation for Visual Analogue Scale (VAS)Up to Day 21

Score from 0 - 100 where 0 is not sedated and 100 is very sedated. VAS measures will be recorded at the indicated timepoints.

AUEC for Reaction Time Index (RTI) scoreUp to Day 21

Reaction time for subject to release the response button after presentation of target stimulus.

Maximum sedation for Reaction Time Index (RTI) scoreUp to Day 21

Reaction time for subject to release the response button after presentation of target stimulus.

Safety and tolerability as demonstrated by AEs with itraconazoleUp to Day 30

Subjects will be continually monitored for adverse events

Safety and tolerability as demonstrated by AEs without rifampicinUp to Day 30

Subjects will be continually monitored for adverse events

Safety and tolerability as demonstrated by Systolic blood pressure (SBP) and diastolic blood pressure (DBP) with itraconazole (mmHG)Up to Day 21

Blood pressure will be assessed as part of vital signs

Safety and tolerability as demonstrated by Systolic blood pressure (SBP) and diastolic blood pressure (DBP) without itraconazole(mmHG)Up to Day 21

Blood pressure will be assessed as part of vital signs

Safety and tolerability as demonstrated by Systolic blood pressure (SBP) and diastolic blood pressure (DBP) with rifampicin(mmHG)Up to Day 21

Blood pressure will be assessed as part of vital signs

Heart rate without rifampicin (beats/minute)Up to Day 21

Heart rate will be assessed as part of vital signs

Oral temperature without rifampicin (degrees Celsius)Up to Day 21

Temperature will be assessed as part of vital signs

Safety and tolerability as demonstrated by the Columbia Suicide Severity Rating Scale (C-SSRS)Up to Day 21

C-SSRS to be administered at the indicated timepoints

Values of white blood cell (WBC), neutrophils, lymphocytes, monocytes, eosinophils, basophils and platelets (1000/mm3)Up to Day 21

Blood samples will be collected for the assessment of hematology parameters

Oral temperature without itraconazole (degrees Celsius)Up to Day 21

Temperature will be assessed as part of vital signs

Oral temperature with rifampicin (degrees Celsius)Up to Day 21

Temperature will be assessed as part of vital signs

Electrocardiogram (ECG) parameters: PR, RR, QRS, QT, and QT interval corrected for heart rate using Fridericia's formula (QTcF) without itraconazole (Milliseconds)Up to Day 21

Twelve-lead ECGs will be obtained at the indicated timepoints

Values of albumin and total protein (g/dL)Up to Day 21

Blood samples will be collected for the assessment of clinical chemistry parameters

Values of urine proteinUp to Day 21

Urine samples will be collected for the assessment of urine parameters

Electrocardiogram (ECG) parameters: PR, RR, QRS, QT, and QT interval corrected for heart rate using Fridericia's formula (QTcF) without rifampicin (Milliseconds)Up to Day 21

Twelve-lead ECGs will be obtained at the indicated timepoints

Value of hematocrit (percent)Up to Day 21

Blood samples will be collected for the assessment of hematology parameters

Value of hemoglobin (g/dL)Up to Day 21

Blood samples will be collected for the assessment of hematology parameters

Values of urine ketonesUp to Day 21

Urine samples will be collected for the assessment of urine parameters

Red blood cell (RBC) count (M/mm3)Up to Day 21

Blood samples will be collected for the assessment of hematology parameters

Values of urine glucoseUp to Day 21

Urine samples will be collected for the assessment of urine parameters

Values of urine bilirubin and nitriteUp to Day 21

Urine samples will be collected for the assessment of urine parameters

Values of urobilinogenUp to Day 21

Urine samples will be collected for the assessment of urine parameters

Values of urine leukocyte esterase by dipstickUp to Day 21

Urine samples will be collected for the assessment of urine parameters

Values of sodium, potassium, chloride (mmol/L)Up to Day 21

Blood samples will be collected for the assessment of clinical chemistry parameters

Values of urea, phosphorus, calcium, glucose, and total, direct and indirect bilirubin (mg/dL)Up to Day 21

Blood samples will be collected for the assessment of clinical chemistry parameters

Values of alanine aminotransferase (ALT), aspartate aminotransferase (AST),alkaline phosphatase (ALP), gamma glutamyl transferase (GGT), creatininephosphokinase (CPK), and creatinine (U/L)Up to Day 21

Blood samples will be collected for the assessment of clinical chemistry parameters

Values of urine specific gravityUp to Day 21

Urine samples will be collected for the assessment of urine parameters

Values of urine pHUp to Day 21

Urine samples will be collected for the assessment of urine parameters

Values of urine bloodUp to Day 21

Urine samples will be collected for the assessment of urine parameters

Trial Locations

Locations (1)

Syneos Health Clinic Inc.

🇨🇦

Québec, Quebec, Canada

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