Drug Interaction Study of Clopidogrel and Rosuvastatin

The Effects of Administering Clopidogrel on the Pharmacokinetics of Rosuvastatin in Healthy Volunteers

The purpose of this study is to determine if clopidogrel inhibits hepatic uptake transport of rosuvastatin clinically.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Rosuvastatin; Drug: Clopidogrel

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

Contacts and Locations

Study Locations

• United States
  • California
    • San Francisco, California, United States, 94143
      • Clinical Research Center, UCSF

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 16 years to 63 years (Adult, Older Adult)
• Accepts Healthy Volunteers: No
• Genders Eligible for Study: All

Description

Inclusion Criteria:

• Healthy individuals, male or female, age 18-65 years old, with no current medical conditions or active diagnoses as determined by the study doctor based on history, physical exam and laboratory evaluations
• Subjects that take no other medications 2 weeks prior to the study and during the time course of the study including prescription medications, over-the-counter medications (except acetaminophen), dietary supplements, or drugs of abuse
• Subjects with a SLCO1B1*1A genotype
• Subjects able to maintain adequate birth control during the study independent of hormonal contraceptive use
• Subjects able to abstain from grapefruit, grapefruit juice, orange juice, caffeinated beverages and/or alcoholic beverages from 3 pm the day before the study to completion of that study day.
• Participants determined to have normal liver and kidney function as measured at baseline
• BMI between 18.5 - 30 kg/m2
• Subjects capable of fasting from food and beverages at least 8 hours prior to medication dosing
• Be able to read, speak, and understand English

Exclusion Criteria:

• Subjects with active medical problems
• Subjects on chronic prescription or OTC medications that cannot be stopped 2 weeks prior to and during the study.
• Subjects incapable of multiple blood draws (HCT <30 mg/dL)
• Subjects with a history of rhabdomyolysis
• Subjects with a history of drug-related myalgias
• Subjects with a history or diagnosis of hemorrhagic tendencies or blood dyscrasias
• Subjects with a history of GI bleed or peptic ulcer disease
• Subjects with a recent history of trauma
• Subjects with a recent history of or upcoming plan of surgery
• Subjects that smoke tobacco or have ongoing alcohol or illegal drug use
• Subjects who are pregnant, lactating, or trying to conceive during the study period
• Subjects allergic to rosuvastatin or clopidogrel or any known component of the medications

Study Plan

How is the study designed?

Design Details

• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Active Comparator: Rosuvastatin	Drug: Rosuvastatin; Rosuvastatin 20 mg PO x 1
Experimental: Rosuvastatin + clopidogrel	Drug: Rosuvastatin; Rosuvastatin 20 mg PO x 1; Drug: Clopidogrel; Clopidogrel 300 mg PO x 1 (30 minutes prior to rosuvastatin dose); Clopidogrel 75 mg PO x 1 (24 hours post-rosuvastatin dose)

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Area-under-the-concentration curve (AUC) of rosuvastatin	Blood samples collected over a 48 hour period

Secondary Outcome Measures

Outcome Measure	Time Frame
Maximum plasma concentration (Cmax) of rosuvastatin	predose, 0, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36, and 48 hours post-dose
Time to concentration maximum (Tmax) of rosuvastatin	predose, 0, 0.5, 1, 1.5, 2, 3, 4, 6, 9, 12, 24, 36, and 48 hours post-dose

Collaborators and Investigators

• Sponsor: University of California, San Francisco

Study record dates

Study Major Dates

• Study Start: March 1, 2012
• Primary Completion (Actual): May 1, 2013
• Study Completion (Actual): May 1, 2013

Study Registration Dates

• First Submitted: October 28, 2011
• First Submitted That Met QC Criteria: November 7, 2011
• First Posted (Estimate): November 10, 2011

Study Record Updates

• Last Update Posted (Estimate): July 18, 2014
• Last Update Submitted That Met QC Criteria: July 16, 2014
• Last Verified: July 1, 2014

More Information

Terms related to this study

• Keywords: healthy volunteer; pharmacokinetics; clopidogrel; drug interaction; rosuvastatin; drug transporter
• 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; Clopidogrel; Rosuvastatin Calcium
• Other Study ID Numbers: 11-07522