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

Emalex Biosciences

Status and phase: Completed; Phase 1

Conditions: Drug Interaction

Treatments: Drug: Ecopipam; Combination Product: Cohort 3 Probe Substrate Cocktail; Combination Product: Cohort 1 Probe Substrate Cocktail; Drug: Cohort 2 Probe Substrate

Study type: Interventional

Funder types: Industry; Other

Identifiers

NCT05334108

EBS-101-HV-104

Details and patient eligibility

About

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

Full 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.

Enrollment: 56 patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

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

Trial design

Primary purpose: Basic Science

Allocation: Non-Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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56 participants in 3 patient groups

Cohort 1

Other group

Description:

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

Treatment:

Combination Product: Cohort 1 Probe Substrate Cocktail

Drug: Ecopipam

Cohort 2

Other group

Description:

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

Treatment:

Drug: Cohort 2 Probe Substrate

Drug: Ecopipam

Cohort 3

Other group

Description:

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

Treatment:

Combination Product: Cohort 3 Probe Substrate Cocktail

Drug: Ecopipam