KF2019#1-trial: Effects of a Thrombocyte Inhibitor on a Cholesterol-lowering Drug

Phase 1

• Conditions: Pharmacokinetics
• Interventions: Drug: Placebo; Drug: Ticagrelor; Drug: Rosuvastatin

• Registration Number: NCT05373277
• Lead Sponsor: Helsinki University Central Hospital

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.

Detailed Description

Not available

Study Timeline

• Status Verified: 2022-05
• Study First Submitted: 2022-05-10
• Study First Submitted QC: 2022-05-10
• Last Update Submitted: 2022-05-10
• Study Start: 2022-05-11
• Study First Posted: 2022-05-13
• Last Update Posted: 2022-05-13
• Primary Completion: 2022-12-31
• Study Completion: 2022-12-31

Recruitment & Eligibility

• Status: UNKNOWN
• Sex: All
• Target Recruitment: 10

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

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: CROSSOVER

Arm && Interventions

Group	Intervention	Description
Placebo	Placebo	The subjects will be given orally placebo twice a day for 2 days, and a single 10 mg dose of rosuvastatin.
Ticagrelor	Rosuvastatin	The subjects will be given orally 90 mg ticagrelor twice a day for 2 days, and a single 10 mg dose of rosuvastatin.
Placebo	Rosuvastatin	The subjects will be given orally placebo twice a day for 2 days, and a single 10 mg dose of rosuvastatin.
Ticagrelor	Ticagrelor	The subjects will be given orally 90 mg ticagrelor twice a day for 2 days, and a single 10 mg dose of rosuvastatin.

Primary Outcome Measures

Name	Time	Method
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 Outcome Measures

Name	Time	Method
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

Trial Locations

Locations (1)

Department of Clinical Pharmacology; 🇫🇮 Helsinki, Finland