Clinical trial NCT01876797: PKPD Study of Ticagrelor and Prasugrel in Healthy Korean Males
Official title: A Single Dose, Open-label, One Sequence, 2-period, Crossover Study to Characterize the Pharmacokinetics and Pharmacodynamics of Ticagrelor and Prasugrel in Healthy Male Adult Subjects
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Healthy
Lead sponsor: Asan Medical Center
Sponsor class: OTHER
First posted: 2013-06-13
Enrollment: 12
Sex: MALE
Minimum age (years): 19
Maximum age (years): 45
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NON_RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: TREATMENT

Brief summary: This study is to characterize the pharmacokinetic and pharmacodynamics of ticagrelor and prasugrel in healthy Korean male subjects.

The study is open label, one sequence, crossover design. In period 1, a single oral dose of 180 mg ticagrelor will be administrated. After at least 7 days washout period, in period 2, a single oral dose of 60 mg prasugrel will be administrated.

After dosing each period, blood sampling for PK and PD assessment will be conducted.

1. Blood Sampling Times

   1. PK :predose,10 min,15 min,25 min, 0.5,1,1.5,2,2.5,4,6,8,12 and 24h post-dose
   2. PD :predose,15 min,0.5,1,2,4,6,8,12 and 24h post-dose
2. Bioanalysis

   1. plasma Ticagrelor
   2. plasma AR-C124910XX (active metabolite of ticagrelor)
   3. plasma R-95913 (inactive metabolite of prasugrel)
   4. plasma R-13727 (active metabolite of prasugrel)
3. Platelet Aggregation Test using turbidometric Method Maximal Platelet Aggregation(MPA)
4. PK-PD Modeling analysis


Eligibility criteria: Inclusion Criteria:

1. male aged 19 - 45 years at screening visit
2. body weight at least 60 kg at screening visit
3. body mass index 18 - 30 kg/m2
4. SBP 90 - 149 mmHg and DBP 60 - 99 mmHg and pulse rate(beat per minute) 45 - 100 at screening visit

Exclusion Criteria:

1. any history of or having any clinically significant abnormalities
2. any gastrointestinal disorder having impact on absorption of study drug
3. any history of hypersensitivity of ticagrelor or prasugrel or compounds related study drugs
4. any history of taking original medicines within 30 days before dosing or history of taking prescribed drug within 14 days before dosing or history of taking OTC drug within 7 days before dosing
5. any history of taking other study drug within 60 days before dosing
6. any history of whole blood transfusion within 60 days before dosing or history of blood elements transfusion or history of heaving been transfused within 30 days before 30 days
7. any history of taking metabolic inducer or inhibitor
8. overuse (caffeine: \> 5 units/day , alcohol: \> 21 units /week, smoking: \> 10 cigarettes/day)
9. positive serology testy(Hbs antigen, HIV, Hepatitis C virus, Syphilis)
10. any abnormality in clinical laboratory tests result or any ECG finding considered to be inadequate by investigator

Primary outcomes:
measure: plasma ticagrelor parent,AR-C124910XX,R-95913 and R-13727
timeFrame: 0,10 min,15 min,25 min,0.5h,1h,1.5h,2h,2.5h,4h,6h,8h,12h and 24h
Secondary outcomes:
measure: Maximal Platelet Aggregation(MPA)
timeFrame: 0,15 min,0.5 min, 1h,2h,4h,8h and 24h
Other outcomes:
measure: adverse event monitoring
timeFrame: up to 1 week
Locations:
city: Seoul
country: Korea, Republic of
facility: Asan Medical Center
Study officials:
affiliation: Asan Medical Center
name: Hyeong-Seok Lim, Professor
role: PRINCIPAL_INVESTIGATOR
References:
citation: Jeon HS, Kim MJ, Choi HY, Kim YH, Kim EH, Kim AR, Park HJ, Bae KS, Lim HS. Pharmacokinetics and pharmacodynamics of ticagrelor and prasugrel in healthy male Korean volunteers. Clin Ther. 2015 Mar 1;37(3):563-73. doi: 10.1016/j.clinthera.2015.01.010. Epub 2015 Feb 16.