Clinical trial NCT00099450: Study of the Tolerability, Pharmacokinetics, and Pharmacodynamics of INS50589 Intravenous Infusion in Healthy Volunteers
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
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Cardiovascular Disease
Keywords: bleeding
blood transfusion
surgeries
Lead sponsor: Merck Sharp & Dohme LLC
Sponsor class: INDUSTRY
First posted: 2004-12-15
Enrollment: 48
Sex: ALL
Minimum age (years): 18
Maximum age (years): 60
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: SINGLE_GROUP
Primary purpose: TREATMENT

Brief summary: 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.

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

Eligibility criteria: 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.

Primary outcomes:
measure: Platelet function
Secondary outcomes:
measure: Pilot study - not specified
Other outcomes:
Locations:
city: Lenexa
country: United States
facility: Quintiles Phase I Services
state: Kansas
Study officials:
name: Amy Schaberg, BSN
role: STUDY_DIRECTOR
References:
citation: Johnson FL, Boyer JL, Leese PT, Crean C, Krishnamoorthy R, Durham T, Fox AW, Kellerman DJ. Rapid and reversible modulation of platelet function in man by a novel P2Y(12) ADP-receptor antagonist, INS50589. Platelets. 2007 Aug;18(5):346-56. doi: 10.1080/09537100701268741.