Clinical trial NCT03143725: Study to Compare Bioavailability of GLPG1972 Given as 2 Different Tablet Formulations Versus an Oral Solution
Official title: Open-label Study to Compare the Bioavailability of an Oral Wet Granulation Tablet of GLPG1972 Relative to an Oral Solution and to an Oral Direct Compression Tablet After Single-dose Intake in Healthy Subjects, and to Evaluate the Effect of Food on the Bioavailability of an Oral Wet Granulation Tablet.
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Galapagos NV
Sponsor class: INDUSTRY
First posted: 2017-05-08
Enrollment: 12
Sex: MALE
Minimum age (years): 18
Maximum age (years): 50
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: TREATMENT

Brief summary: This study is a Phase I, randomized, open-label, cross-over study with 4 single-dose treatments of GLPG1972 to compare the bioavailability of the oral wet granulation (WG) tablet relative to an oral solution and to the oral direct compression (DC) tablet after single dose intake in healthy male subjects and to evaluate the effect of food on the bioavailability of the WG oral tablet.


Eligibility criteria: Inclusion Criteria:

1. Male between 18 and 50 years of age, inclusive,
2. A body mass index (BMI) between 18-30 kg/m², inclusive, weight of at least 50 kg.
3. Judged by the investigator to be in good health based upon the results of a medical history, physical examination, vital signs, 12-lead ECG, and laboratory findings.
4. Discontinuation of all medications except occasional paracetamol at least 2 weeks or 5 half-lives prior to the first study drug administration.
5. Non-smokers and not using any nicotine-containing products.
6. Negative urine drug screen and alcohol breath test.
7. Current sexually active male agrees to use adequate contraception
8. Willing to consume a non-vegetarian high-fat and high-calorie breakfast
9. Able and willing to sign the ICF

Exclusion Criteria:

1. Known hypersensitivity to study drug ingredients or a significant allergic reaction to any drug
2. Positive serology for hepatitis B virus surface antigen (HBsAg) or hepatitis C virus (HCV) or any history of hepatitis from any cause with the exception of hepatitis A.
3. History of or a current immunosuppressive condition
4. Symptoms of clinically significant illness in the 3 months before the initial study drug administration.
5. History of malignancy within the past 5 years
6. Clinically relevant abnormalities detected on ECG regarding either rhythm or conduction (e.g. QTcF \>450 msec, or a known long QT syndrome).
7. Presence of abnormal liver function
8. Renal function with an estimated creatinine clearance \<80 ml/min based on the Cockcroft-Gault formula.
9. Presence of any condition known to interfere with absorption, distribution, metabolism or excretion of drugs.
10. Clinically relevant abnormalities detected on "vital signs"
11. Dietary requirements precluding participation.
12. Significant blood loss including blood donation or had a transfusion of any blood product within 12 weeks
13. Hemoglobin level \<7.5 mmol/L (12 g/dL).
14. Active drug or alcohol abuse within 2 years prior to the initial study drug administration.
15. Current (2 weeks before screening) and planned uninterrupted consumption of large quantities (\> 6 cups) of coffee
16. Administration of an injectable drug within 30 days prior to the initial study drug administration.
17. Concurrent participation, or participation in a drug/device study within 8 weeks or 5 half-lives of the drug or within 6 months for biologicals
18. Investigator or any sub-investigator, research assistant, pharmacist, study coordinator, or other staff

Primary outcomes:
measure: Assessment of the maximum observed plasma concentration of GLPG1972 after single oral doses
timeFrame: on day 1 pre-dose and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post doses
measure: Assessment of plasma concentration of GLPG1972 24hrs post-dose after single oral doses
timeFrame: At 24 hours post dose
measure: Assessment of time to achieve the maximal plasma concentration of GLPG1972 after single oral doses
timeFrame: on day 1 pre-dose and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post doses
measure: Assessment of the last quantifiable plasma concentration of GLPG1972 after single oral doses
timeFrame: on day 1 pre-dose and at 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 16, 24 and 48 hours post doses
Secondary outcomes:
measure: the number of subjects with adverse events
timeFrame: at screening, pre-dose at date 1 and post-dose at 24 and 48 hours
measure: the number of subjects with abnormal vital signs
timeFrame: at screening, pre-dose at date 1 and post-dose at 24 and 48 hours
measure: the number of subjects with abnormal ECG
timeFrame: at screening, pre-dose at date 1 and post-dose at 24 and 48 hours
measure: the number of subjects with abnormal laboratory assessments
timeFrame: at screening, pre-dose at date 1 and post-dose at 24 and 48 hours
Other outcomes:
Locations:
city: Antwerp
country: Belgium
facility: SGS Belgium Life Sciences
Study officials:
affiliation: Galapagos NV
name: Ann Fieuw, MD MSc
role: STUDY_DIRECTOR
References: