A Study to Assess Safety, Tolerability and Pharmacokinetics of GLPG3067 in Healthy Subjects.

Phase 1

Completed

• Conditions: Healthy
• Interventions: Drug: GLPG3067 oral tablet; Drug: Placebo single dose; Drug: Placebo multiple dose; Drug: GLPG3067/GLPG2222 multiple dose; Drug: GLPG3067 single dose; Drug: GLPG3067 oral suspension; Drug: GLPG3067 multiple dose; Drug: GLPG3067/GLPG2222/GLPG2737 multiple dose; Drug: GLPG3067/GLPG2222/GLPG2737 Placebo multiple dose; Drug: GLPG3067/GLPG2222 Placebo multiple dose

• Registration Number: NCT03128606
• Lead Sponsor: Galapagos NV

Brief Summary

The study is a First-in-Human, Phase I, randomized, double-blind, placebo-controlled, single center study, evaluating single and multiple ascending oral doses of GLPG3067 and the combination of GLPG3067 and GLPG2222 and the combination of GLPG3067,GLPG2222 and GLPG2737 given for 14 days in healthy women of non-childbearing potential.

The purpose of the study is to evaluate the safety and tolerability of single ascending oral doses and multiple ascending oral doses of GLPG3067 given to healthy women of non-childbearing potential compared to placebo, as well as of multiple oral doses of the combination of GLPG3067/GLPG2222 compared to matching placebo for each compound and multiple oral doses of the combination of GLPG3067/GLPG2222/GLPG2737 compared to matching placebo for each compound.

Detailed Description

Not available

Study Timeline

• Study Start: 2017-03-28
• Study First Submitted: 2017-04-21
• Study First Submitted QC: 2017-04-21
• Study First Posted: 2017-04-25
• Primary Completion: 2018-02-20
• Study Completion: 2018-02-20
• Status Verified: 2018-04
• Last Update Submitted: 2018-04-09
• Last Update Posted: 2018-04-10

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Female
• Target Recruitment: 81

Inclusion Criteria

• Female subject between 18-70 years of age, inclusive, on the date of signing the informed consent form (ICF).
• Be of non-childbearing potential defined as surgically sterile (hysterectomy, bilateral salpingectomy and bilateral oophorectomy), or post-menopausal (at least 12 consecutive months without menstruation, without an alternative medical cause [including hormone replacement therapy]).
• Have a body mass index between 18-30 kg/m2, inclusive.
• Judged by the investigator to be in good health based upon the results of a medical history, physical examination, vital signs, 12-lead triplicate electrocardiogram (ECG), and clinical safety laboratory tests prior to the initial study drug administration.
• Discontinuation of all medications (including over-the-counter and/or prescription medication, dietary supplements, nutraceuticals, vitamins and/or herbal supplements, and hormonal replacement therapy for postmenopausal subjects) except occasional paracetamol (maximum dose of 2 g/day and maximum of 10 g/2 weeks) at least 2 weeks prior to the first study drug administration.

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Exclusion Criteria

• Known hypersensitivity to study drug ingredients or a significant allergic reaction to any drug as determined by the investigator, such as anaphylaxis requiring hospitalization.
• Clinically significant symptoms or illness in the 3 months before screening.
• Presence or having sequelae of gastrointestinal, liver, kidney, or other conditions known to interfere with the absorption, distribution, metabolism, or excretion of drugs.
• Any laboratory result considered by the investigator as clinically significant prior to study drug administration.
• Creatinine clearance ≤80 mL/min using the Cockcroft-Gault formula for subjects aged ≤50 years, or creatinine clearance ≤70 mL/min using the Cockcroft-Gault formula for subjects aged >50 years. A 24-hour urine collection to determine the actual value may be performed to confirm creatinine clearance if required.
• Clinically significant abnormalities of vital signs at screening.
• Clinically relevant abnormalities detected on ECG regarding either rhythm or conduction (e.g. QT interval corrected for heart rate using Fridericia's formula [QTcF] >470 ms) or a known long QT syndrome. A first degree heart block or sinus arrhythmia will not be considered as a significant abnormality.
• Participation in a drug, drug and device delivery system or combination, or biologic investigational research study within 8 weeks or 5 times the half-life of the investigational drug, if the half-life is known (whichever is longer) prior to initial study drug administration. Subjects who have been dosed previously with GLPG3067 in a clinical trial are allowed to participate Part 4 of this study as long as they completed their last follow-up visit or a washout period of 5 times the half-life of GLPG3067 (whichever is longer) after the last study drug administration is respected.

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Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SEQUENTIAL

Arm && Interventions

Group	Intervention	Description
GLPG3067 oral tablet fed 1	GLPG3067 oral tablet	Single dose 1 of GLPG3067 oral tablet after a standardized breakfast.
Placebo single dose	Placebo single dose	Single dose of Placebo oral suspension.
GLPG3067 oral tablet fed 2	GLPG3067 oral tablet	Single dose 2 of GLPG3067 oral tablet after a standardized breakfast.
Placebo multiple dose	Placebo multiple dose	Multiple doses of Placebo oral suspension.
GLPG3067/GLPG2222 multiple dose	GLPG3067/GLPG2222 multiple dose	Multiple doses of GLPG3067 oral suspension combined with GLPG2222 oral tablet up to 2 dose levels in ascending order.
GLPG3067 single dose	GLPG3067 single dose	Single dose of GLPG3067 oral suspension at up to 6 dose levels in ascending order.
GLPG3067 oral suspension fed 1	GLPG3067 oral suspension	Single dose 1 of GLPG3067 oral suspension after a standardized breakfast.
GLPG3067 oral tablet fasted 1	GLPG3067 oral tablet	Single dose 1 of GLPG3067 oral tablet after an overnight fast.
GLPG3067 oral tablet fed 2 high-fat high-calorie	GLPG3067 oral tablet	Single dose 2 of GLPG3067 oral tablet after a high-fat high-calorie breakfast
GLPG3067 multiple dose	GLPG3067 multiple dose	Multiple doses of GLPG3067 oral suspension at up to 5 dose levels in ascending order.
GLPG3067/GLPG2222/GLPG2737 multiple dose	GLPG3067/GLPG2222/GLPG2737 multiple dose	Multiple doses of GLPG3067 oral tablet combined with GLPG2222 oral tablet and GLPG2737 oral capsule at up to 2 dose levels in ascending order.
GLPG3067/GLPG2222/GLPG2737 Placebo multiple dose	GLPG3067/GLPG2222/GLPG2737 Placebo multiple dose	Multiple doses of GLPG3067 matching placebo oral tablet combined with GLPG2222 matching placebo oral tablet and GLPG2737 matching placebo oral capsule.
GLPG3067/GLPG2222 Placebo multiple dose	GLPG3067/GLPG2222 Placebo multiple dose	Multiple doses of GLPG3067 matching placebo oral suspension combined with GLPG2222 matching placebo oral tablet.

Primary Outcome Measures

Name	Time	Method
Change versus placebo in the proportion of subjects with adverse events	Between screening and 14 days after the last dose	To assess safety and tolerability of single ascending doses, multiple ascending doses of GLPG3067 alone, or in combination with GLPG2222, or in combination with GLPG2222 and GLPG2737 versus placebo in healthy subjects

Secondary Outcome Measures

Name	Time	Method
Ratio of 4-beta-hydroxycholesterol/cholesterol in plasma after multiple oral doses in healthy subjects	Day 1 predose and Day 14	To assess the potential for CYP3A4 interaction with GLPG3067, GLPG3067 and GLPG2222, or GLPG3067 and GLPG2222 and GLPG2737
Maximum observed plasma concentration of GLPG3067 (Cmax) given alone in fed state	Between Day 1 predose and 10 days after the last dose	To assess the relative bioavailability of GLPG3067 when given as a single dose of oral suspension or an oral tablet both administered in fed state
Maximum observed plasma concentration of GLPG3067 (Cmax) given alone in fasted state	Between Day 1 predose and 10 days after the last dose	To assess the effect of food on the pharmacokinetics of GLPG3067 when given under fasted versus fed conditions
Concentration in plasma observed at 24 hours post dose (C24h) of GLPG3067 given alone in fed state	Between Day 1 predose and 10 days after the last dose	To assess the relative bioavailability of GLPG3067 when given as a single dose of oral suspension or an oral tablet both administered in fed state
Concentration in plasma observed at 24 hours post dose (C24h) of GLPG3067 given alone in fasted state	Between Day 1 predose and 10 days after the last dose	To assess the effect of food on the pharmacokinetics of GLPG3067 when given under fasted versus fed conditions
Area under the plasma concentration-time curve of GLPG3067 (AUC0-t) given alone in fasted state	Between Day 1 predose and 10 days after the last dose	To assess the effect of food on the pharmacokinetics of GLPG3067 when given under fasted versus fed conditions
Maximum observed plasma concentration of GLPG3067 (Cmax) given alone or in combination with GLPG2222 or in combination with GLPG2222 and GLPG2737	Between Day 1 predose and 10 days after the last dose	To characterize pharmacokinetics of GLPG3067 after a single oral dose and of GLPG3067, GLPG2222, and GLPG2737 after multiple oral doses in healthy subjects
Area under the plasma concentration-time curve of GLPG3067 (AUC0-t) given alone or in combination with GLPG2222 or in combination with GLPG2222 and GLPG2737	Between Day 1 predose and 10 days after the last dose	To characterize pharmacokinetics of GLPG3067 after a single oral dose and of GLPG3067, GLPG2222, and GLPG2737 after multiple oral doses in healthy subjects
Area under the plasma concentration-time curve of GLPG3067 (AUC0-t) given alone in fed state	Between Day 1 predose and 10 days after the last dose	To assess the relative bioavailability of GLPG3067 when given as a single dose of oral suspension or an oral tablet both administered in fed state

Trial Locations

Locations (1)

SGS LSS Clinical Pharmacology Unit Antwerp; 🇧🇪 Antwerp, Belgium