Study of the Tolerability, Pharmacokinetics, and Pharmacodynamics of INS50589 Intravenous Infusion in Healthy Volunteers

This study has been completed.
Information provided by (Responsible Party):
Merck Sharp & Dohme Corp. Identifier:
First received: December 14, 2004
Last updated: January 19, 2015
Last verified: January 2015
The objectives of this study are to look at the safety and tolerability of the experimental drug, how people process the drug, how the drug affects people, and to identify a dose or doses to study in subsequent future studies.

Condition Intervention Phase
Cardiovascular Disease
Drug: INS50589 Intravenous Infusion
Phase 1

Study Type: Interventional
Study Design: Allocation: Randomized
Endpoint Classification: Pharmacokinetics/Dynamics Study
Intervention Model: Single Group Assignment
Masking: Double-Blind
Primary Purpose: Treatment
Official Title: Single-Center, Open-Labeled Dose Escalation Followed by Randomized, Double-Blind, Placebo-Controlled Cohort Study of the Tolerability, Pharmacokinetics, and Pharmacodynamics of INS50589 Intravenous Infusion in Healthy Volunteers

Further study details as provided by Merck Sharp & Dohme Corp.:

Primary Outcome Measures:
  • Platelet function

Secondary Outcome Measures:
  • Pilot study - not specified

Estimated Enrollment: 48
Study Start Date: December 2004
Study Completion Date: March 2005
Primary Completion Date: March 2005 (Final data collection date for primary outcome measure)
Detailed Description:

The purposes of this trial are to determine if administration of INS50589 Intravenous Infusion is well tolerated, to determine the pharmacological effects of INS50589 at different doses, and to identify an appropriate dose for later efficacy studies. More specifically, the objectives are to:

  • Evaluate safety and tolerability
  • Evaluate pharmacokinetics of INS50589 and its major metabolite(s)
  • Evaluate effects of INS50589 on platelet function at various dose levels
  • Evaluate potential relationship between plasma concentrations of INS50589 and various pharmacodynamic endpoints
  • Identify one or more dose levels of INS50589 for future studies

Ages Eligible for Study:   18 Years to 60 Years
Genders Eligible for Study:   Both
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • Have body mass index (BMI) between 18.5 kg/m2 and 35 kg/m2 and body weight no greater than 120 kg.
  • If female, must not be pregnant or lactating, and if of childbearing potential or sexually active, must use acceptable method of birth control.

Exclusion Criteria:

  • Have clinically significant acute or chronic disease (e.g., coronary artery disease, diabetes, chronic renal insufficiency, asthma).
  • Have major surgery within eight weeks of dosing.
  • Have overt viral illness within four weeks of dosing.
  • Have tendency or history in family of tendency for bleeding.
  • Have clinically significant abnormalities on clinical laboratory tests (chemistry, hematology, urinalysis).
  • Have taken aspirin or any other non-steroidal anti-inflammatory drug (NSAID) within 10 days prior to admission to study facility.
  • Have ever taken or received any of the following for medical conditions: (antiplatelet compounds including clopidogrel, ticlopidine, dipyridamole, tirofiban, eptifibatide, abciximab, adenosine, and prostacyclin) or (anticoagulants including vitamin K antagonists, thrombin inhibitors, heparins, hirudin or related compounds, argatroban and factor Xa inhibitors)
  • Have a clinically significant ECG abnormality.
  Contacts and Locations
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Please refer to this study by its identifier: NCT00099450

United States, Kansas
Quintiles Phase I Services
Lenexa, Kansas, United States, 66219
Sponsors and Collaborators
Merck Sharp & Dohme Corp.
Study Director: Amy Schaberg, BSN
  More Information

Responsible Party: Merck Sharp & Dohme Corp. Identifier: NCT00099450     History of Changes
Other Study ID Numbers: 025-101 
Study First Received: December 14, 2004
Last Updated: January 19, 2015
Health Authority: United States: Food and Drug Administration

Keywords provided by Merck Sharp & Dohme Corp.:
blood transfusion

Additional relevant MeSH terms:
Cardiovascular Diseases
INS 50589
Molecular Mechanisms of Pharmacological Action
Neurotransmitter Agents
Physiological Effects of Drugs
Purinergic Agents
Purinergic Antagonists
Purinergic P2 Receptor Antagonists processed this record on May 26, 2016