A Study in Healthy Male Volunteers Investigating the Safety, Absorption and Elimination of Single Doses of GLPG4059

A First-in-human, Randomized, Double-blind, Placebo-controlled, Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single Ascending Oral Doses of GLPG4059 in Adult, Healthy, Male Subjects

The main purpose of this study is to evaluate the safety, tolerability and pharmacokinetics of GLPG4059 in healthy volunteers after single oral administrations of GLPG4059 (SAD), compared to placebo (part 1). The effect of food (FE) (high-fat, high calorie) on the pharmacokinetics and relative bioavailability (rBA) of GLPG4059 will be assessed (part 2).

Study Overview

• Status: Terminated
• Conditions: Healthy
• Intervention / Treatment: Drug: Placebo; Drug: GLPG4059 oral suspension; Drug: GLPG4059 tablet

• Study Type: Interventional
• Enrollment (Actual): 32
• Phase: Phase 1

Contacts and Locations

Study Locations

• Netherlands
  • Groningen, Netherlands, 9728
    • PRA Health Sciences

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 54 years (ADULT)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: Male

Description

Inclusion Criteria:

• Male between 18-54 years of age (extremes included), on the date of signing the informed consent form (ICF).
• A body mass index (BMI) between 18-30 kg/m2, inclusive.
• Judged to be in good health by the investigator based upon the results of a medical history, physical examination, vital signs, 12-lead ECG, and fasting clinical laboratory safety tests, available at screening and prior to randomization. ECG and vital signs parameters must be within the normal ranges. Bilirubin, aspartate aminotransferase (AST), and alanine aminotransferase (ALT) must be no greater than 1.5x upper limit of normal (ULN). Fasting plasma glucose must be <6.99 mmol/L, fasting defined as no caloric intake for at least 8 hours and hemoglobin A1c (HbA1c) <6.5% (48 mmol/mol). The test should be performed in a laboratory using a method that is national glycohemoglobin standardization program (NGSP) certified and standardized to the diabetes control and complications trial (DCCT) assay. 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 Investigational Medicinal Product (IMP) ingredients or history of a significant allergic reaction to IMP ingredients as determined by the investigator.
• Positive serology for hepatitis B virus surface antigen (HBsAg) or hepatitis C virus (HCV) or history of hepatitis from any cause with the exception of hepatitis A that was resolved at least 3 months prior to first dosing of the IMP.

This list only contains the key exclusion criteria.

Study Plan

How is the study designed?

Design Details

• Primary Purpose: BASIC_SCIENCE
• Allocation: RANDOMIZED
• Interventional Model: SEQUENTIAL
• Masking: QUADRUPLE

Number of Arms

5

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
EXPERIMENTAL: GLPG4059 SAD; Single doses of GLPG4059 at up to 6 dose levels in ascending order	Drug: GLPG4059 oral suspension; GLPG4059 for oral administration
PLACEBO_COMPARATOR: Placebo SAD; Single doses of placebo	Drug: Placebo; Placebo oral suspension
EXPERIMENTAL: GLPG4059 rBA/FE oral suspension fasted; Single dose of GLPG4059 in fasted state	Drug: GLPG4059 oral suspension; GLPG4059 for oral administration
EXPERIMENTAL: GLPG4059 rBA/FE tablet fed; Single dose of GLPG4059 in fed state	Drug: GLPG4059 tablet; GLPG4059 for oral administration
EXPERIMENTAL: GLPG4059 rBA/FE tablet fasted; Single dose of GLPG4059 in fasted state	Drug: GLPG4059 tablet; GLPG4059 for oral administration

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Frequency and severity of treatment-emergent adverse events (TEAEs), treatment-emergent serious adverse events, and TEAEs leading to treatment discontinuations	To evaluate the safety and tolerability of single ascending oral doses of GLPG4059, in adult, healthy, male subjects compared with placebo.	From screening through study completion, an average of 7 months

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Maximum observed plasma concentration (Cmax) of GLPG4059	To evaluate the pharmacokinetics (PK) of single ascending oral doses of GLPG4059, in adult, healthy, male subjects.	Between Day 1 pre-dose and Day 4
Area under curve (AUC) of GLPG4059	To evaluate the PK of single ascending oral doses of GLPG4059, in adult, healthy, male subjects	Between Day 1 pre-dose and Day 4
Terminal elimination half-life (t1/2) of GLPG4059	To evaluate the PK of single ascending oral doses of GLPG4059, in adult, healthy, male subjects	Between Day 1 pre-dose and Day 4

Collaborators and Investigators

• Sponsor: Galapagos NV

Study record dates

Study Major Dates

• Study Start (ACTUAL): September 16, 2020
• Primary Completion (ACTUAL): April 8, 2021
• Study Completion (ACTUAL): April 8, 2021

Study Registration Dates

• First Submitted: September 29, 2020
• First Submitted That Met QC Criteria: September 29, 2020
• First Posted (ACTUAL): October 5, 2020

Study Record Updates

• Last Update Posted (ACTUAL): May 11, 2021
• Last Update Submitted That Met QC Criteria: May 7, 2021
• Last Verified: May 1, 2021

More Information

Terms related to this study

• Other Study ID Numbers: GLPG4059-CL-101; 2020-000036-22 (EUDRACT_NUMBER)

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
• product manufactured in and exported from the U.S.: No