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

Helsinki University Central Hospital10 enrolled

Overview

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 Type

INTERVENTIONAL

Allocation

RANDOMIZED

Purpose

BASIC_SCIENCE

Masking

DOUBLE

Enrollment

Conditions

Pharmacokinetics

Interventions

Eligibility

Sex: ALLMin age: 18 YearsMax age: 40 YearsHealthy volunteers:

Medical Language ↔ Plain English

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

Outcomes

Primary Outcomes

Area under the plasma concentration - time curve of rosuvastatin

Time frame: 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 Outcomes

Peak plasma concentration, half-life, time to peak plasma concentration, amount excreted, and renal clearance of rosuvastatin

Time frame: Prior to and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 7, 8, 10, 23, and 47 hours after administration of rosuvastatin

Central Contacts

Mikko Niemi, MD, PhD

CONTACT

+35894711 mikko.niemi@hus.fi

Minna Lehtisalo, MD