Vorapaxar is indicated for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease (PAD). MedDRA version: 17.1 Level: LLT Classification code 10014501 Term: Embolism - blood clot System Organ Class: 100000004866
Conditions
Interventions
Product Name: Vorapaxar
Product Code: MK-5348
Pharmaceutical Form: Oral suspension
INN or Proposed INN: VORAPAXAR
Other descriptive name: VORAPAXAR SULPHATE
Concentration unit: mg/ml milligram(s)/mill
Sponsors
Merck Sharp & Dohme Corp., a subsidiary of Merck & Co.,Inc
Eligibility
Sex/Gender
All
Inclusion criteria
Inclusion criteria: 1) Healthy, non-smoking, male and female subjects, from 18 to 55 years of age. 2) BMI = 19.0 and =30.0 kg/m2 and weight =60 kg. 3) No clinically significant findings in vital-signs measurements. 4) No clinically significant abnormal laboratory values. 5) No clinically significant findings in a 12-lead electrocardiogram (ECG). 6) Have no significant diseases. 7) Willing to use an acceptable, effective method of contraception. 8) Be informed of the nature of the study and give written consent prior to any study procedure. 9) Have no clinically significant findings from a physical examination. Are the trial subjects under 18? no Number of subjects for this age range: F.1.2 Adults (18-64 years) yes F.1.2.1 Number of subjects for this age range 24 F.1.3 Elderly (>=65 years) no F.1.3.1 Number of subjects for this age range
Exclusion criteria
Exclusion criteria: 1) Known history or presence of any clinically significant medical condition. 2) Known or suspected carcinoma. 3) History of stroke, myocardial infarction (MI), transient ischemic attack (TIA), peripheral arterial disease (PAD) or intracranial hemorrhage (ICH). 4) Known history or presence of active clinically significant/pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage, clotting disorders). 5) Known history or presence of galactose or fructose intolerance, sucrase-isomaltase insufficiency, Lapp lactase insufficiency, galactosemia, or glucose-galactose malabsorption syndrome. 6) Subjects with mouth piercings, dentures, braces, dental appliances, or any other alteration to the mouth that may compromise drug delivery. 9) Presence of clinically significant gastrointestinal disease or history of malabsorption within the last year. 10) Presence of a medical condition requiring regular medication (prescription and/or over-the-counter) with systemic absorption. 11) History of drug or alcohol addiction requiring treatment. 12) Positive test result for HIV, Hepatitis B surface antigen or Hepatitis C antibody. 13) Positive test result for urine drugs of abuse (cannabinoids, opiates, amphetamines, cocaine, phencyclidine, tricyclic antidepressants, barbiturates, methadone and benzodiazepines) or urine cotinine. 14) Difficulty fasting or consuming standard meals. 15) Does not tolerate venipuncture. 16) Use of tobacco or nicotine-containing products within 6 months prior to drug administration. 17) On a special diet within 30 days prior to drug administration (e.g., liquid, protein, raw food diet). 18) Participated in a clinical trial, which involved administration of an investigational medicinal product within 30 days prior to drug administration, or recently participated in a clinical investigation that, in the opinion of the Investigator, would jeopardize subject safety or the integrity of the study results. 19) Donation or loss of whole blood (including clinical trials): • = 50 mL and = 499 mL within 30 days prior to drug administration; • = 500 mL within 56 days prior to drug administration. 20) Females who: • Have used oral or transdermal hormonal contraceptives within 21 days prior to drug administration; • Have used implanted, injected, intravaginal or intrauterine hormonal contraceptives within 6 months prior to drug administration; • Are pregnant (serum hCG consistent with pregnancy); or • Are lactating. 21) Have had a tattoo or body piercing within 30 days prior to drug administration. 22) Estimated creatinine clearance of =80 mL/min based on the Cockcroft-Gault equation. 23) Known history or presence of hypersensitivity or idiosyncratic reaction to vorapaxar (MK-5348) or any other drug substances with similar activity. 24) Subject is mentally or legally incapacitated, has significant emotional problems at the time of screening or expected during the conduct of the study or has a history of a clinically significant psychiatric disorder over the last 5 years. Subjects who have had situational depression may be enrolled in the study at the discretion of the investigator. 25) Have planned a surgery or dental procedure within 30 days after drug administration. 26) Within 30 days prior to the drug administration, use of: • antidepressants (e.g., SSRI [citalopram, fluoxetine], SNRI [dexvenlafaxine, duloxetine]); • antiplatelet, anticoagulants or fibrinolytics (e.g.
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Main Objective: To evaluate the comparative bioavailability between: • MK-5348 (vorapaxar) 0.2085 mg/mL oral suspension from Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., USA; and • MK-5348 (Zontivity™) 2.08 mg tablet (equivalent to 2.5 mg vorapaxar sulfate) from Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., USA; after a single-dose in healthy subjects under fasting conditions.;Secondary Objective: Not applicable;Primary end point(s): AUC0-last: The area under the analyte concentration versus time curve, from time zero (0) to the time of the last measurable analyte concentration, as calculated by the lin-up/log-down variant of the trapezoidal method. Cmax: Maximum measured analyte concentration over the sampling period. Tmax: Time of the maximum measured analyte concentration over the sampling period.;Timepoint(s) of evaluation of this end point: (0-hour) and 0.5, 1, 1.5, 2, 3, 4, 6, 12, 24, 48 and 72 hours post-dose | — |
Secondary
| Measure | Time frame |
|---|---|
| Timepoint(s) of evaluation of this end point: not applicable;Secondary end point(s): not applicable | — |
Countries
Canada
Contacts
Public ContactClinical Monitor
Merck Sharp & Dohme Corp.
Outcome results
None listed