chronic inflammatory diseases chronic inflammatory diseases rheumatoid arthritis
Conditions
Interventions
Group 1:
Day/ Treatment/ Timing
1) 7.5 mg methotrexate as 3 oral tablets of 2.5 mg
5) 350 mg GLPG3970 as oral solution 7.5 mg methotrexate as 3 oral tablets of
2.5 mg
A maximum of 1 minute between
Sponsors
Galapagos NV
Eligibility
Age
18 Years to 99 Years
Inclusion criteria
Inclusion criteria: 1. Male or female Caucasian between 18-55 years of age (extremes included), on the date of signing the informed consent form (ICF). 2. Females should be of non-childbearing potential defined as permanently surgically sterile (bilateral oophorectomy, i.e. surgical removal of ovaries, bilateral salpingectomy or hysterectomy, i.e. surgical removal of uterus), or with no menses for 12 or more months without an alternative medical cause AND a follicle-stimulating hormone (FSH) level >35 IU/L. These subjects must also have a negative pregnancy test. For surgical sterilization, documented confirmation will be requested. 3. A body mass index (BMI) between 18-30 kg/m2, inclusive. 4. A BCRP c421C/C genotype. 5. 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 the first non investigational medicinal product (NIMP) administration. Bilirubin, aspartate aminotransferase (AST), and alanine aminotransferase (ALT) must be no greater than 1.5x upper limit of normal range (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.
Exclusion criteria
Exclusion criteria: 1. Known hypersensitivity to the IMP (GLPG3970), or NIMPs (MTX and sulfasalazine), or sulfa drugs, or to their ingredients, or history of a significant allergic reaction to IMP or NIMPs ingredients as determined by the investigator. 2. 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 NIMP. 3. History of or a current immunosuppressive condition (e.g. human immunodeficiency virus [HIV] infection). 4. Having any illness, judged by the investigator as clinically significant, in the 3 months prior to first dosing of the NIMP. 5. Presence or sequelae of gastrointestinal, liver, kidney (creatinine clearance
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| MTX and 7-OH MTX PK parameters: maximum observed concentration (Cmax) and area under the plasma concentration-time curve from time zero to infinity (AUC0-*) Sulfasalazine and sulfapyridine PK parameters: Cmax and AUC0-* Sulfapyridine to sulfasalazine AUC ratio | — |
Secondary
| Measure | Time frame |
|---|---|
| Safety and tolerability, assessed by the incidence and severity of treatment emergent adverse events (TEAEs) Safety and tolerability, assessed by the incidence and severity of TEAEs GLPG3970 PK parameters such as trough concentrations (Ctrough), Cmax, time of occurrence of Cmax (tmax), and AUC0-t | — |
Countries
Netherlands
Outcome results
None listed