A Phase I, drug-drug interaction study between oral doses of GLPG1205 and an OCT2 probe substrate (metformin) or a BCRP probe substrate (rosuvastatin) in healthy male subjects

Completed

Conditions: inflammation induced pain
nociceptive pain
sensitization induced pain
10034606

Registration Number: NL-OMON44647

Lead Sponsor: Galapagos NV

Brief Summary: Not available

Detailed Description: Not available

Recruitment & Eligibility

Status: Completed

Sex: Not specified

Target Recruitment: 40

Inclusion Criteria

1. Subject has signed the informed consent form prior to any study related activity.
2. Subject is a healthy male volunteer between 18 and 50 years of age (inclusive) at the time of informed consent signature.
3. Subject has a BMI equal to or higher than 18.0 kg/m2 and equal to or lower than 30.0 kglm2 at the screening
4. Subject is appropriate for the study in the judgment of the investigator, based on physical examination, 12-lead electrocardiogram (ECG), laboratory tests, and subject's interview.
5. Subject has a high probability for compliance with and completion of the study.
6. Discontinuation of all medications (including over-the-counter medications, vitamin and herbal supplements) with the exception of occasional paracetamol (maximum dose of 2 g/day and maximum 10 g/2 weeks) at least 3 weeks, or 5 half-lives of the drug, whichever is longer, prior to the first study drug administration.
7. A non-smoker and not using any nicotine-containing products for at least 1 year prior to the study screening.
8. Negative tests for drug screen (amphetamines, barbiturates, benzodiazepines, cannabis, cocaine, and opiates), alcohol screen, and cotinine screen.
9. Subject agrees that he will use a condom and that in addition to that he (and his female partner of child-bearing potential) will use a highly effective method of contraception and will not donate sperm from the first study drug administration to 12 weeks after the last study drug administration.

Exclusion Criteria

1. Subject shows clinically significant abnormalities in Screening, Day -1 or Day 1 physical examination, ECG or vital signs, according to the investigator*s judgment.
2. Subject has a history of clinically significant endocrine, gastrointestinal, cardiovascular, hematological, hepatic, immunological, renal, respiratory, genitourinary or major neurological (including stroke and chronic seizures) abnormalities or diseases.
3. History of malignancy in the last 5 years, except basal cell carcinoma of the skin that has been treated and with no evidence of recurrence.
4. Subject has been exposed to GLPG1205 before.
5. Known hypersensitivity to GLPG1205 or excipients of the formulation, metformin, biguanides or rosuvastatin. A history of significant allergic reaction to any drug, such as anaphylaxis requiring hospitalization.
6. Having a contraindication as indicated in the respective Summary of Product Characteristics (or Package Leaflets) for metformin or rosuvastatin.
7. Subject is of Asian origin.
8. Subject had major surgery, donated or lost 1 unit of blood or plasma (approximately 500 mL) within 6 weeks prior to the first intake of the study drug.
9. Subject has participated in another investigational trial within 90 days prior to the first intake of the study drug in this study.
10. Subject has used any type of medication (including herbal medicine and vitamin supplements) within 3 weeks prior to the first intake of the study drug.
11. Clinically significant illness in the 12 weeks prior to study dosing, including severe vomiting or diarrhoea.
12. Presence or having sequelae of GI, liver or kidney (creatinine clearance * 90 mL/min using the Cockcroft formula) or other conditions known to interfere with the absorption, distribution, metabolism, or excretion of drugs.
13. Investigator or any sub-investigator, research assistant, pharmacist, study coordinator, or other staff or relative thereof who is directly involved in the conduct of the study.
14. Any history of vitamin B12 deficiency.
15. Clinically significant abnormalities detected on laboratory safety testing during Screening or Day -1, including (but not limited to):
a. Hemoglobin < 10 g/dL
b. WBC count < 3.0 x 10^9 cells/L
c. Neutrophil count < 1.5 x 10^9 cells/L
d. Platelet count < 100 x 10^9 cells/L
e. Serum ALT or aspartate aminotransferase (AST) > 2 x upper limit of normal (ULN)
f. Total bilirubin level > 1.5 x ULN, except in the case of documented Gilbert*s syndrome
16. Subject has a positive urinary drug screen during Screening or Day -1 (incl. amphetamine, barbiturates, benzodiazepines, cocaine, marijuana, methadone, methamphetamine, morphine, phencyclidine, and tricyclic antidepressants).
17. History of abuse of alcohol or drugs in the last 2 years (alcohol >23 units/week).
18. Subject has a positive test for HIV antibody, HBsAg, or HCV antibody.
19. Subject has a positive alcohol test during Screening or Day -1.
20. Subject consumes more than 5 cups of caffeine containing beverages per day.
21. Clinically significant abnormalities, during Screening or Day -1 on ECG of rhythm or conduction (e.g., QTcF > 450 ms, known long-QT syndrome), excluding first degree heart block.
22. Subject plans to father a child during the course of the study.