OraL Crushed and dIspersed Ticagrelor 180mg Compared to Whole Tablets of eQUal Dose in STEMI Patients unDergoing Primary PCI: a Pharmacokinetic/Pharmacodynamic Study (the LIQUID Study) (LIQUID)
Primary Purpose
ST Elevation Myocardial Infarction
Status
Completed
Phase
Phase 4
Locations
Greece
Study Type
Interventional
Intervention
Ticagrelor 180mg whole tablets
Ticagrelor 180mg crushed and dispersed
Sponsored by
About this trial
This is an interventional treatment trial for ST Elevation Myocardial Infarction focused on measuring ticagrelor, ST elevation myocardial infarction, liquid formulation
Eligibility Criteria
Inclusion Criteria:
- Age ≥18 years old
- Patients with STEMI (onset of pain<12 hours) with indication for primary PCI
- Informed consent obtained in writing
Exclusion Criteria:
Pregnancy/Breastfeeding
- Severe nausea or vomiting
- Treatment with a P2Y12 inhibitor within the previous 1 month
- Inability to give informed consent
- Hemodynamic instability
- Arrhythmias requiring cardioversion, temporary pacemaker insertion or intravenous antiarrhythmic agents
- Killip class ≥3
- Known hypersensitivity to ticagrelor
- History of gastrointestinal bleeding, genitourinary bleeding or other site abnormal bleeding within the previous 3 months.
- Other bleeding diathesis, or considered by investigator to be at high risk for bleeding
- Thombocytopenia (<100.000 / μL) at randomization
- Anaemia (Hct <30%) at randomization
- Polycytaemia (Hct > 52%) at randomization
- Periprocedural IIb/IIIa inhibitor administration
- Thrombolysis administration
- Recent (< 6 weeks) major surgery or trauma, including GABG.
- Concomitant oral or IV therapy with strong CY P3A inhibitors (ketoconazole, itraconazole, voriconazole, telithromycin, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, atazana vir, grapefruit juice N1 L/d), CYP3A substrates with narrow therapeutic indices (cyclosporine, quinidine), or strong CYP3A inducers (rifampin /rifampicin, phenytoin, carbamazepine).
- Patients considered by the investigator to be at increased risk of bradycardiac events.
- Dialysis required.
- Severe uncontrolled chronic obstructive pulmonary disease
- Known severe hepatic impairement
Sites / Locations
- Patras University Hospital Department of Cardiology
Arms of the Study
Arm 1
Arm 2
Arm Type
Active Comparator
Experimental
Arm Label
Ticagrelor 180mg whole tablets
Ticagrelor 180mg crushed and dispersed
Arm Description
Ticagrelor 180mg loading dose, in the form of 2 whole tablets administered per os in the supine position (standard administration)
Ticagrelor 180mg in the form of 2 tablets crushed and dispersed in purified water administered per os with 1-minute-stay in a 60-70 degrees semi-upright sitting position
Outcomes
Primary Outcome Measures
Ticagrelor's Cmax over 1 hour post ticagrelor administration
Area under the ticagrelor plasma concentration versus time curve (AUC0-1) over 1 hour post ticagrelor administration
Secondary Outcome Measures
Platelet reactivity at 1 hour post randomization
Platelet reactivity assessment with the VerifyNow assay
HPR rate at 1 hour post randomization
HPR rate at 1 hour post randomization between the two treatment arms
Platelet reactivity at 2 hours post randomization
Platelet reactivity assessment with the VerifyNow assay
HPR rate at 2 hours post randomization
HPR rate at 2 hours post randomization between the 2 treatment arms.
AR-C124910XX Cmax over 1 hour post ticagrelor administration
AR-C124910XX Cmax over 6 hours post ticagrelor administration
Ticagrelor Cmax over 6 hours post ticagrelor administration
Area under the AR-C124910XX plasma concentration versus time curve (AUC0-1) over 1 hour post ticagrelor administration
Area under the AR-C124910XX plasma concentration versus time curve (AUC0-6) over 6 hours post ticagrelor administration
Area under the Ticagrelor plasma concentration versus time curve (AUC0-6) over 6 hours post ticagrelor administration
Time for the maximum plasma concentration (Tmax) of Ticagrelor over 6 hours post Ticagrelor administration
Time for the maximum plasma concentration (Tmax) of AR-C124910XX over 6 hours post Ticagrelor administration
Full Information
NCT ID
NCT02046486
First Posted
January 23, 2014
Last Updated
January 26, 2015
Sponsor
University of Patras
1. Study Identification
Unique Protocol Identification Number
NCT02046486
Brief Title
OraL Crushed and dIspersed Ticagrelor 180mg Compared to Whole Tablets of eQUal Dose in STEMI Patients unDergoing Primary PCI: a Pharmacokinetic/Pharmacodynamic Study (the LIQUID Study)
Acronym
LIQUID
Official Title
OraL Crushed and dIspersed Ticagrelor 180mg Compared to Whole Tablets of eQUal Dose in STEMI Patients unDergoing Primary PCI: a Pharmacokinetic/Pharmacodynamic Study
Study Type
Interventional
2. Study Status
Record Verification Date
January 2015
Overall Recruitment Status
Completed
Study Start Date
January 2014 (undefined)
Primary Completion Date
January 2015 (Actual)
Study Completion Date
January 2015 (Actual)
3. Sponsor/Collaborators
Responsible Party, by Official Title
Principal Investigator
Name of the Sponsor
University of Patras
4. Oversight
Data Monitoring Committee
No
5. Study Description
Brief Summary
This is a single-center, prospective, randomized, single-blind, investigator initiated, pharmacokinetic/pharmacodynamic study of parallel design.Patients with ST elevation myocardial infarction (symptom onset<12 hours), undergoing primary percutaneous coronary intervention, who are P2Y12 inhibitor naïve, will be randomized after informed consent, immediately after diagnostic coronary angiography, in a 1:1 ratio to either:
Ticagrelor 180mg loading dose, in the form of 2 whole tablets administered per os in the supine position (standard administration)
Ticagrelor 180mg loading dose, in the form of 2 tablets crushed and dispersed in purified water and administered per os with 1-minute-stay in a 60-70 degrees semi-upright sitting position Platelet reactivity assessment will be performed at randomization (Hour 0) and at 0.5, 1, 2, 4 and 6 hours after randomization, using the VerifyNow assay, in platelet reactivity units (PRU). The cutoff >208 PRU will be used for definition of high platelet reactivity (HPR). All platelet reactivity assessments will be performed by a physician blind to the actual treatment given. Additional blood samples will be collected at the same time points for pharmacokinetic analysis. These samples will be collected in vacuum tubes with lithium heparin and will be kept in ice until centrifugation (3000 rpm at 4°C for 10 min, within 30 min of sampling). The resultant plasma will be transferred into a plain polypropylene tube (screw cap) and stored at or below -20°C until analysed.
Detailed Description
Preparation of Ticagrelor liquid formulation:
Crushed and dispersed Ticagrelor 180mg for oral administration will be prepared as follows: two ticagrelor 90mg tablets are placed in a mortar and crushed for 60 s using a pestle. 20 mL of purified water will be added in the mortar and stirred for 60s. The liquid is transferred to a dosing cup and another 15 mL of purified water is added to the mortar and stirred, ensuring that all powder has been dispersed and none remained on the mortar and pestle. Again the liquid is transferred to the dosing cup. The same procedure is repeated with 15 ml of purified water.The total contents are stirred for another 30 s to ensure that all remaining tablet particles are dispersed.
6. Conditions and Keywords
Primary Disease or Condition Being Studied in the Trial, or the Focus of the Study
ST Elevation Myocardial Infarction
Keywords
ticagrelor, ST elevation myocardial infarction, liquid formulation
7. Study Design
Primary Purpose
Treatment
Study Phase
Phase 4
Interventional Study Model
Parallel Assignment
Masking
Outcomes Assessor
Allocation
Randomized
Enrollment
20 (Anticipated)
8. Arms, Groups, and Interventions
Arm Title
Ticagrelor 180mg whole tablets
Arm Type
Active Comparator
Arm Description
Ticagrelor 180mg loading dose, in the form of 2 whole tablets administered per os in the supine position (standard administration)
Arm Title
Ticagrelor 180mg crushed and dispersed
Arm Type
Experimental
Arm Description
Ticagrelor 180mg in the form of 2 tablets crushed and dispersed in purified water administered per os with 1-minute-stay in a 60-70 degrees semi-upright sitting position
Intervention Type
Drug
Intervention Name(s)
Ticagrelor 180mg whole tablets
Intervention Type
Drug
Intervention Name(s)
Ticagrelor 180mg crushed and dispersed
Primary Outcome Measure Information:
Title
Ticagrelor's Cmax over 1 hour post ticagrelor administration
Time Frame
1 hour
Title
Area under the ticagrelor plasma concentration versus time curve (AUC0-1) over 1 hour post ticagrelor administration
Time Frame
1 hour
Secondary Outcome Measure Information:
Title
Platelet reactivity at 1 hour post randomization
Description
Platelet reactivity assessment with the VerifyNow assay
Time Frame
1 hour
Title
HPR rate at 1 hour post randomization
Description
HPR rate at 1 hour post randomization between the two treatment arms
Time Frame
1 hour
Title
Platelet reactivity at 2 hours post randomization
Description
Platelet reactivity assessment with the VerifyNow assay
Time Frame
2 hours
Title
HPR rate at 2 hours post randomization
Description
HPR rate at 2 hours post randomization between the 2 treatment arms.
Time Frame
2 hours
Title
AR-C124910XX Cmax over 1 hour post ticagrelor administration
Time Frame
1 hour
Title
AR-C124910XX Cmax over 6 hours post ticagrelor administration
Time Frame
6 hours
Title
Ticagrelor Cmax over 6 hours post ticagrelor administration
Time Frame
6 hours
Title
Area under the AR-C124910XX plasma concentration versus time curve (AUC0-1) over 1 hour post ticagrelor administration
Time Frame
1 hour
Title
Area under the AR-C124910XX plasma concentration versus time curve (AUC0-6) over 6 hours post ticagrelor administration
Time Frame
6 hours
Title
Area under the Ticagrelor plasma concentration versus time curve (AUC0-6) over 6 hours post ticagrelor administration
Time Frame
6 hours
Title
Time for the maximum plasma concentration (Tmax) of Ticagrelor over 6 hours post Ticagrelor administration
Time Frame
6 hours
Title
Time for the maximum plasma concentration (Tmax) of AR-C124910XX over 6 hours post Ticagrelor administration
Time Frame
6 hours
10. Eligibility
Sex
All
Minimum Age & Unit of Time
18 Years
Accepts Healthy Volunteers
No
Eligibility Criteria
Inclusion Criteria:
Age ≥18 years old
Patients with STEMI (onset of pain<12 hours) with indication for primary PCI
Informed consent obtained in writing
Exclusion Criteria:
Pregnancy/Breastfeeding
Severe nausea or vomiting
Treatment with a P2Y12 inhibitor within the previous 1 month
Inability to give informed consent
Hemodynamic instability
Arrhythmias requiring cardioversion, temporary pacemaker insertion or intravenous antiarrhythmic agents
Killip class ≥3
Known hypersensitivity to ticagrelor
History of gastrointestinal bleeding, genitourinary bleeding or other site abnormal bleeding within the previous 3 months.
Other bleeding diathesis, or considered by investigator to be at high risk for bleeding
Thombocytopenia (<100.000 / μL) at randomization
Anaemia (Hct <30%) at randomization
Polycytaemia (Hct > 52%) at randomization
Periprocedural IIb/IIIa inhibitor administration
Thrombolysis administration
Recent (< 6 weeks) major surgery or trauma, including GABG.
Concomitant oral or IV therapy with strong CY P3A inhibitors (ketoconazole, itraconazole, voriconazole, telithromycin, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, atazana vir, grapefruit juice N1 L/d), CYP3A substrates with narrow therapeutic indices (cyclosporine, quinidine), or strong CYP3A inducers (rifampin /rifampicin, phenytoin, carbamazepine).
Patients considered by the investigator to be at increased risk of bradycardiac events.
Dialysis required.
Severe uncontrolled chronic obstructive pulmonary disease
Known severe hepatic impairement
Facility Information:
Facility Name
Patras University Hospital Department of Cardiology
City
Patras
State/Province
Achaia
ZIP/Postal Code
26500
Country
Greece
12. IPD Sharing Statement
Citations:
PubMed Identifier
26315810
Citation
Alexopoulos D, Barampoutis N, Gkizas V, Vogiatzi C, Tsigkas G, Koutsogiannis N, Davlouros P, Hahalis G, Nylander S, Parodi G, Xanthopoulou I. Crushed Versus Integral Tablets of Ticagrelor in ST-Segment Elevation Myocardial Infarction Patients: A Randomized Pharmacokinetic/Pharmacodynamic Study. Clin Pharmacokinet. 2016 Mar;55(3):359-67. doi: 10.1007/s40262-015-0320-0.
Results Reference
derived
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OraL Crushed and dIspersed Ticagrelor 180mg Compared to Whole Tablets of eQUal Dose in STEMI Patients unDergoing Primary PCI: a Pharmacokinetic/Pharmacodynamic Study (the LIQUID Study)
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