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

KF2019#1-tutkimus: Verihiutaleiden estäjän Vaikutus kolesterolilääkkeeseen

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.

Study Overview

• Status: Recruiting
• Conditions: Pharmacokinetics
• Intervention / Treatment: Drug: Placebo; Drug: Rosuvastatin; Drug: Ticagrelor

• Study Type: Interventional
• Enrollment (Anticipated): 10
• Phase: Phase 1

Contacts and Locations

• Study Contact: Name: Mikko Niemi, MD, PhD; Phone Number: +35894711; Email: mikko.niemi@hus.fi
• Study Contact Backup: Name: Minna Lehtisalo, MD; Phone Number: +35894711; Email: minna.lehtisalo@hus.fi

Study Locations

• Finland
  • Helsinki, Finland, 00290
    • Recruiting
    • Department of Clinical Pharmacology
    • Contact: Minna Lehtisalo, MD; Phone Number: +35894711; Email: minna.lehtisalo@hus.fi
    • Contact: Mikko Niemi, MD,PhD; Phone Number: +35894711; Email: mikko.niemi@hus.fi

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 18 years to 40 years (Adult)
• Accepts Healthy Volunteers: Yes
• Genders Eligible for Study: All

Description

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 Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: Double

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Placebo Comparator: Placebo; The subjects will be given orally placebo twice a day for 2 days, and a single 10 mg dose of rosuvastatin.	Drug: Placebo; one tablet of placebo twice daily for two days; Drug: Rosuvastatin; 10 mg tablet, single dose
Active Comparator: Ticagrelor; The subjects will be given orally 90 mg ticagrelor twice a day for 2 days, and a single 10 mg dose of rosuvastatin.	Drug: Rosuvastatin; 10 mg tablet, single dose; Drug: Ticagrelor; Intervention Description: 90 mg tablet twice daily for two days

What is the study measuring?

Primary Outcome Measures

Outcome 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 Outcome Measures

Outcome 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

Collaborators and Investigators

• Sponsor: Helsinki University Central Hospital
• Collaborators: University of Helsinki

Study record dates

Study Major Dates

• Study Start (Anticipated): May 11, 2022
• Primary Completion (Anticipated): December 31, 2022
• Study Completion (Anticipated): December 31, 2022

Study Registration Dates

• First Submitted: May 10, 2022
• First Submitted That Met QC Criteria: May 10, 2022
• First Posted (Actual): May 13, 2022

Study Record Updates

• Last Update Posted (Actual): May 13, 2022
• Last Update Submitted That Met QC Criteria: May 10, 2022
• Last Verified: May 1, 2022

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Enzyme Inhibitors; Platelet Aggregation Inhibitors; Purinergic P2Y Receptor Antagonists; Purinergic P2 Receptor Antagonists; Purinergic Antagonists; Purinergic Agents; Antimetabolites; Anticholesteremic Agents; Hypolipidemic Agents; Lipid Regulating Agents; Hydroxymethylglutaryl-CoA Reductase Inhibitors; Ticagrelor; Rosuvastatin Calcium
• Other Study ID Numbers: KF2019#1

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No