A Study to Evaluate How Well Single and Multiple Doses of GLPG3121-modified Release Formulation Are Tolerated in Healthy, Adult Subjects

A Phase I, Randomized, Double-blind, Placebo-controlled Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single and Multiple Ascending Oral Doses of GLPG3121-modified Release Formulation in Adult, Healthy, Male Subjects

The aim of the study is to examine the safety and tolerability of GLPG3121-modified release formulation when given to healthy male subjects once as a single dose or multiple times over a period of 14 days in fasting condition or after a standard breakfast.

The study will evaluate how the body absorbs and breaks down GLPG3121, and how GLPG3121 and the major breakdown product of GLPG3121 are eliminated from the body. In addition, the study will investigate the effect of food (high-fat) after a single oral dose of GLPG3121 as modified release tablet.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Placebo; Drug: GLPG3121

• Study Type: Interventional
• Enrollment (Actual): 50
• Phase: Phase 1

Contacts and Locations

Study Locations

• Germany
  • Berlin, Germany, 10117
    • Charite Research Organisation GmbH

Participation Criteria

Eligibility Criteria

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

Description

Inclusion Criteria:

• Male between 18 and 55 years of age (extremes included), on the date of signing the informed consent form (ICF).
• A body mass index (BMI) 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, 12-lead electrocardiogram (ECG), and fasting clinical laboratory safety tests, available at screening and prior to randomization. Hemoglobin, neutrophil, lymphocyte, and platelet counts must be above the lower limit of normal range. Total bilirubin, aspartate aminotransferase (AST), alanine aminotransferase (ALT), and serum creatinine must be no greater than the upper limit of normal (ULN). 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.
• Subject must be able and willing to comply with restrictions on prior and concomitant medication.
• Negative screen for drugs (amphetamines, barbiturates, benzodiazepines, cannabis, cocaine, opiates, methadone, tricyclic antidepressants) and alcohol.

This list only contains the key inclusion criteria.

Exclusion Criteria:

• Known hypersensitivity to investigational product (IP) ingredients or history of a significant allergic reaction to IP 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 IP.
• History of or a current immunosuppressive condition (e.g. human immunodeficiency virus [HIV] infection).
• Having any illness, judged by the investigator as clinically significant, in the 3 months prior to first dosing of the IP.
• Presence or sequelae of gastrointestinal, liver, kidney (estimated glomerular filtration rate [eGFR] <=90 mL/min/1.73 m2, using the Chronic Kidney Disease Epidemiology Collaboration [CKD-EPI] formula) or other conditions known to interfere with the absorption, distribution, metabolism, or excretion of drugs.

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: Parallel Assignment
• Masking: Quadruple

Number of Arms

6

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Placebo Comparator: Placebo SAD; Single doses of placebo	Drug: Placebo; Matching placebo
Placebo Comparator: Placebo MAD; Multiple doses of placebo	Drug: Placebo; Matching placebo
Experimental: GLPG3121 SAD; Single doses of GLPG3121 at up to 3 dose levels in ascending order	Drug: GLPG3121; GLPG3121 modified-release tablet
Experimental: GLPG3121 MAD; Multiple doses of GLPG3121 at up to 3 dose levels in ascending order	Drug: GLPG3121; GLPG3121 modified-release tablet
Experimental: GLPG3121 FE fed; Single dose of GLPG3121 in fed state	Drug: GLPG3121; GLPG3121 modified-release tablet
Experimental: GLPG3121 FE fasted; Single dose of GLPG3121 in fasted state	Drug: GLPG3121; GLPG3121 modified-release tablet

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 and multiple ascending oral doses of GLPG3121-modified-release formulation (GLPG3121-MR), in adult, healthy, male subjects compared with placebo	From screening through study completion, an average of 8 months

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Maximum observed plasma concentration (Cmax) of GLPG3121 in SAD	To evaluate the pharmacokinetics (PK) of single ascending oral doses of GLPG3121 in adult, healthy, male subjects	Between Day 1 pre-dose and Day 6
Cmax of GLPG3121's main metabolite in SAD	To evaluate the PK of single ascending oral doses of GLPG3121's metabolite in adult, healthy, male subjects	Between Day 1 pre-dose and Day 6
Cmax of GLPG3121 in MAD	To evaluate the PK of multiple ascending oral doses of GLPG3121 in adult, healthy, male subjects	Between Day 1 pre-dose and Day 19
Cmax of GLPG3121's main metabolite in MAD	To evaluate the PK of multiple ascending oral doses of GLPG3121's main metabolite in adult, healthy, male subjects	Between Day 1 pre-dose and Day 19
Area under the plasma concentration-time curve (AUC) of GLPG3121 in SAD	To evaluate the PK of single ascending oral doses of GLPG3121 in adult, healthy, male subjects	Between Day 1 pre-dose and Day 6
AUC of GLPG3121's main metabolite in SAD	To evaluate the PK of single ascending oral doses of GLPG3121's main metabolite in adult, healthy, male subjects	Between Day 1 pre-dose and Day 6
AUC of GLPG3121 in MAD	To evaluate the PK of multiple ascending oral doses of GLPG3121 metabolite in adult, healthy, male subjects	Between Day 1 pre-dose and Day 19
AUC of GLPG3121's main metabolite in MAD	To evaluate the PK of multiple ascending oral doses of GLPG3121's main metabolite in adult, healthy, male subjects	Between Day 1 pre-dose and Day 19
Terminal elimination half-life (t1/2) of GLPG3121 in SAD	To evaluate the PK of single ascending oral doses of GLPG3121 in adult, healthy, male subjects	Between Day 1 pre-dose and Day 6
t1/2 of GLPG3121's main metabolite in SAD	To evaluate the PK of single ascending oral doses of GLPG3121's main metabolite in adult, healthy, male subjects	Between Day 1 pre-dose and Day 6
t1/2 of GLPG3121 in MAD	To evaluate the PK of multiple ascending oral doses of GLPG3121 in adult, healthy, male subjects	Between Day 1 pre-dose and Day 19
t1/2 of GLPG3121's main metabolite in MAD	To evaluate the PK of multiple ascending oral doses of GLPG3121's main metabolite in adult, healthy, male subjects	Between Day 1 pre-dose and Day 19

Collaborators and Investigators

• Sponsor: Galapagos NV
• Investigators: Study Director: Magdalena Petkova, MD, Galapagos NV

Study record dates

Study Major Dates

• Study Start (Actual): April 27, 2021
• Primary Completion (Actual): November 8, 2021
• Study Completion (Actual): November 8, 2021

Study Registration Dates

• First Submitted: April 14, 2021
• First Submitted That Met QC Criteria: April 19, 2021
• First Posted (Actual): April 23, 2021

Study Record Updates

• Last Update Posted (Actual): September 19, 2024
• Last Update Submitted That Met QC Criteria: September 13, 2024
• Last Verified: December 1, 2021

More Information

Terms related to this study

• Other Study ID Numbers: GLPG3121-CL-103; 2020-004174-21 (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