Pharmacokinetics
Conditions
Brief summary
The cholesterol-lowering drug rosuvastatin is a substrate of the breast cancer resistance protein (BCRP). BCRP is an efflux transporter expressed e.g. in the small intestine. It limits the oral bioavailability of rosuvastatin by transporting rosuvastatin from enterocytes back to the gut lumen. Inhibition of BCRP can increase rosuvastatin bioavailability and systemic concentrations. Ticagrelor is a platelet aggregation inhibitor used in treatment and prevention of atherothrombotic events. Ticagrelor may inhibit BCRP in humans. This study is aimed to investigate the possible interaction of rosuvastatin with ticagrelor. Ten healthy male or female non-smoking volunteers aged 18-40 years are taken into the study. Primary endpoint is area under the plasma concentration-time curve of rosuvastatin.
Interventions
DRUGPlacebo
one tablet of placebo twice daily for two days
DRUGTicagrelor
Intervention Description: 90 mg tablet twice daily for two days
DRUGRosuvastatin
10 mg tablet, single dose
Sponsors
University of Helsinki
Helsinki University Central Hospital
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
BASIC_SCIENCE
Masking
DOUBLE (Subject, Investigator)
Eligibility
Sex/Gender
ALL
Age
18 Years to 40 Years
Healthy volunteers
Yes
Inclusion criteria
* Written informed consent * Age 18-40 * Healthy * Systolic blood pressure ≥100 mmHg * Accepted results from laboratory tests (blood haemoglobin, basic blood count and blood platelets, alanine aminotransferase, alkaline phosphatase, glutamyl transferase, creatinine, plasma potassium and sodium). Negative pregnancy test result (serum human chorionic gonadotropin) for women. * Fully vaccinated against COVID-19.
Exclusion criteria
* Significant disease * Abnormal result from the Helsinki University Hospital bleeding questionnaire * Smoking * Using oral contraception pills or other regular medication * Pregnancy (current or planned) or nursing * Participation in any other studies involving investigational or marketed drug products within three months prior to the entry into this study * Donation of blood within three months prior to the entry into this study * Significant overweight / small or hard-to-find veins * Weight \< 45 kg * BMI \< 18.5 kg/m2 * Insufficient Finnish language skills
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Area under the plasma concentration - time curve of rosuvastatin | Prior to and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 10, 23, and 47 hours after administration of rosuvastatin |
Secondary
| Measure | Time frame |
|---|---|
| Peak plasma concentration, half-life, time to peak plasma concentration, amount excreted, and renal clearance of rosuvastatin | Prior to and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 10, 23, and 47 hours after administration of rosuvastatin |
Countries
Finland
Contacts
Primary ContactMikko Niemi, MD, PhD
Backup ContactMinna Lehtisalo, MD
Outcome results
None listed