Drug-drug Interaction and Food-effect Study With GLPG4716 and Midazolam in Healthy Subjects

An Open-label, Fixed Sequence, Drug-drug Interaction Study in Healthy Subjects to Evaluate the Effect of GLPG4716 on the Pharmacokinetics of Midazolam, a Sensitive Index Substrate of CYP3A4, and to Assess the Effect of Food on the Pharmacokinetics of GLPG4716

The purpose of this study is to determine the effect of the administration of multiple doses of GLPG4716 on the amount of midazolam (MDZ) that gets into the blood when the two drugs are administered together compared to when midazolam is administered alone. Other objectives of this study are to evaluate the safety and tolerability of GLPG4716 when administered with midazolam and assess the amount of GLPG4716 that gets into the blood when administered with midazolam. This study will also assess the effect of food on the amount of GLPG4716 that gets into the blood.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: GLPG4716; Drug: Midazolam

• Study Type: Interventional
• Enrollment (Actual): 19
• Phase: Phase 1

Contacts and Locations

Study Locations

• Canada
  • Montréal, Canada, QC H3P 3P1
    • Altasciences

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 55 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Male or female between 18 and 55 years of age (extremes included), on the date of signing the informed consent form. Female subjects should be of non-childbearing potential.
• A body mass index between 18.0 and 30.0 kg/m2, inclusive.

• Judged to be in good health by the investigator based upon:

  • The results of a medical history
  • Physical examination
  • Vital signs
  • Oxygen saturation
  • 12-lead electrocardiogram
  • Fasting clinical laboratory safety tests. Aspartate aminotransferase and alanine aminotransferase must be no greater than 1.5x upper limit of normal range and total bilirubin no greater than 1x upper limit of normal. Other clinical laboratory safety test results must be within the reference ranges or test results that are outside the reference ranges need to be considered not clinically significant in the opinion of the investigator.

This list only contains the key inclusion criteria.

Exclusion Criteria:

• Known hypersensitivity to ingredients of GLPG4716 and/or MDZ
• History of a significant allergic reaction to ingredients of GLPG4716 and/or MDZ as determined by the investigator.

• Treatment with any medication including:

  • Over-the-counter and/or prescription medication
  • Dietary supplements
  • Nutraceuticals, vitamins and/or herbal supplements, and hormonal replacement therapy
  • Except occasional paracetamol (maximum dose of 2 g/day and maximum of 10 g/2 weeks) in the last 2 weeks or 5 half-lives of the drug, whichever is longer, prior to the first dosing.

This list only contains the key exclusion criteria.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: N/A
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

1

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: GLPG4716 and Midazolam	Drug: GLPG4716; From Day 3 to Day 14, participants will receive GLPG4716 tablets once daily in fasted state. On Day 8 GLPG4716 will be administered in fed state.; Drug: Midazolam; On Days 1, 3 and 13, participants will receive a single oral dose of MDZ as an oral solution in fasted state.

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Maximum observed plasma concentration (Cmax) of MDZ	To determine the effect of GLPG4716 on the pharmacokinetics (PK) of MDZ	From Day 1 pre-dose until Day 15
Area under the plasma concentration-time curve from time zero to infinity (AUC0-inf) of MDZ	To determine the effect of GLPG4716 on the PK of MDZ	From Day 1 pre-dose until Day 15

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Cmax of GLPG4716	To assess the effect of food on the PK of GLPG4716.	From Day 1 pre-dose until Day 15
Area under the plasma concentration-time curve over the dosing interval (AUCt) of GLPG4716	To assess the effect of food on the PK of GLPG4716.	From Day 1 pre-dose until Day 15
Frequency and severity of treatment-emergent adverse events (TEAEs), treatment-emergent (SAEs), and TEAEs leading to treatment discontinuations	To evaluate the safety and tolerability of GLPG4716 when co-administered with MDZ	From Day 1 through study completion, an average of one month

Collaborators and Investigators

• Sponsor: Galapagos NV
• Investigators: Study Director: Natalia Rueda-Rincon, MD, Galapagos NV

Study record dates

Study Major Dates

• Study Start (Actual): September 8, 2021
• Primary Completion (Actual): November 13, 2021
• Study Completion (Actual): November 13, 2021

Study Registration Dates

• First Submitted: August 30, 2021
• First Submitted That Met QC Criteria: August 30, 2021
• First Posted (Actual): September 1, 2021

Study Record Updates

• Last Update Posted (Actual): November 24, 2021
• Last Update Submitted That Met QC Criteria: November 23, 2021
• Last Verified: November 1, 2021

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; Anesthetics, Intravenous; Anesthetics, General; Anesthetics; Tranquilizing Agents; Psychotropic Drugs; Hypnotics and Sedatives; Adjuvants, Anesthesia; Anti-Anxiety Agents; GABA Modulators; GABA Agents; Midazolam
• Other Study ID Numbers: GLPG4716-CL-102

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