An Open-label Study to Assess the Potential for Pre-systemic Inhibition of Cytochrome P450 3A4 (CYP3A) by Idebenone in Healthy Male Subjects Using Midazolam as a Substrate

Santhera Pharmaceuticals1 site in 1 country32 target enrollmentSeptember 2016

ConditionsDrug-Drug Interaction

DrugsRaxone (idebenone 150 mg)Midazolam 2,5 mg

Overview

Phase: Phase 1
Intervention: Not specified
Conditions: Drug-Drug Interaction
Sponsor: Santhera Pharmaceuticals
Enrollment: 32
Locations: 1
Primary Endpoint: Area Under the Curve (AUC) from the time of dosing to the time of the last observed concentration (AUC0-t)
Status: Completed
Last Updated: 8 years ago

Overview Investigators Eligibility Criteria Outcomes Sites Similar Trials

Overview

Brief Summary

This phase I open label study is conducted to assess the potential pharmacokinetic interaction of Raxone® with midazolam in healthy male volunteers

Registry

clinicaltrials.gov

Start Date

September 2016

End Date

November 2016

Last Updated

8 years ago

Study Type

Interventional

Study Design

Single Group

Sex

Male

Investigators

Sponsor

Santhera Pharmaceuticals

Responsible Party

Sponsor

Eligibility Criteria

Inclusion Criteria

•Healthy male aged 18 to 55 years.
•A Body Mass Index (BMI) of 18-
•BMI = Body weight (kg) / Height (m)
•Male subject willing to use an acceptable effective contraceptive measure for the entire duration of study participation.
•No clinically significant abnormal serum biochemistry, haematology and urine examination values.
•A negative urinary test for drugs of abuse and alcohol breath screen. A positive alcohol test may be repeated at the discretion of the Investigator.
•Negative HIV and Hepatitis B and C results.
•No clinically significant abnormalities in 12 lead electrocardiogram (ECG).
•No clinically significant abnormalities in blood pressure, pulse or oral temperature.
•No allergy or sensitivity to midazolam, idebenone or any of their excipients.

Exclusion Criteria

•A clinically significant history of gastrointestinal disorder likely to influence drug absorption.
•Use of any medication (prescription or OTC, including health supplements and herbal remedies, except paracetamol, within 2 weeks or 5 half-lives (whichever is longer) prior to the first dose of trial medication.
•Use of any medication known to induce or inhibit any of the enzymes within the CYP3A system within 28 days of Day 1, or grapefruit within 7 days of Day 1
•Evidence of renal, hepatic dysfunction, cardiovascular or metabolic dysfunction.
•History of obstructive sleep apnoea syndrome.
•History of any significant drug allergy including benzodiazepine.
•A clinically significant history of drug or alcohol abuse.
•Inability to communicate well with the Investigator (i.e., language problem, poor mental development or impaired cerebral function).
•Participation in a clinical trial of a New Chemical Entity within the previous 3 months or of a Marketed Product within the previous 30 days (or 5 times the half-life, whichever is longer).
•Donation of 450 mL or more blood within the previous 3 months.

Outcomes

Primary Outcomes

Area Under the Curve (AUC) from the time of dosing to the time of the last observed concentration (AUC0-t)

Time Frame: 13 days

Area Under the Curve (AUC) extrapolated to infinity from dosing time, based on the last observed concentration (AUC0-∞)

Time Frame: 13 days

Maximum plasma concentration (Cmax)

Time Frame: 13 days

Time to Maximum plasma concentration (Cmax) during a dosing interval (tmax)

Time Frame: 13 days

Terminal elimination half-life (t1/2)

Time Frame: 13 days

Clearance, calculated as dose/AUC0-∞ (CL/F)

Time Frame: 13 days

Volume of distribution during terminal phase after non-intravenous administration (Vz/F)

Time Frame: 13 days

Secondary Outcomes

Area Under the Curve (AUC) from the time of dosing to the time of the last observed concentration (AUC0-t)(13 days)
Area Under the Curve (AUC) extrapolated to infinity from dosing time, based on the last observed concentration (AUC0-∞)(13 days)
Maximum plasma concentration (Cmax)(13 days)
Time to Maximum plasma concentration (Cmax) during a dosing interval (tmax)(13 days)
Terminal elimination half-life (t1/2)(13 days)
Clearance (CL)(13 days)
Clearance, calculated as dose/AUC0-∞ (CL/F)(13 days)
Volume of distribution (Vz)(13 days)
Volume of distribution during terminal phase after non-intravenous administration (Vz/F)(13 days)