Abstract
Ticagrelor has a greater antiplatelet efficacy than clopidogrel but may be accompanied by an increased risk of bleeding. This study evaluated the antiplatelet effect and pharmacokinetic profile of low-dose ticagrelor in healthy Chinese volunteers. Thirty healthy subjects were randomized to receive standard-dose ticagrelor (180-mg loading dose, 90-mg twice daily [bid] [n = 10]), low-dose ticagrelor (90-mg loading dose, 45-mg bid [n = 10]), or clopidogrel (600-mg loading dose, 75-mg once daily [n = 10]). Platelet reactivity was assessed by using the VerifyNow P2Y12 assay at baseline and 0.5, 1, 2, 4, 8, 24, 48, and 72 hours post-dosing. The ticagrelor and AR-C124910XX concentrations were measured for pharmacokinetic analysis. The percentage inhibition of P2Y12 reaction units was higher in the low-dose and standard-dose ticagrelor group than in the clopidogrel group at 0.5, 1, 2, 4, 8, and 48 hours post-dosing (P < 0.05 for all), but did not differ significantly between the two ticagrelor doses at any time-point (P > 0.05). The plasma ticagrelor and ARC124910XX concentrations were approximately 2-fold higher with standard-dose versus low-dose ticagrelor. No serious adverse events were reported. In conclusion, low-dose ticagrelor achieved faster and higher inhibition of platelet functions in healthy Chinese subjects than did clopidogrel, with an antiplatelet efficacy similar to that of standard-dose ticagrelor.
Highlights
Study has found that the mean P2Y12 reaction units (PRU) value in Chinese patients after ticagrelor treatment (90-mg bid) is far below the previous thresholds associated with a bleeding risk[16]
The subjects were eligible to participate if they had a body mass index (BMI) between 18.5 and 24 kg/m2 and a body weight >5 0 kg, and were in good health according to their medical history, physical examination, vital signs, laboratory tests, and 12-lead electrocardiography (ECG)
The mean percentage inhibition of PRU measured by the VerifyNow assay was significantly higher in the low-dose and standard-dose ticagrelor groups than in the clopidogrel group at 0.5, 1, 2, 4, 8, and 48 h after loading, whereas there was no significant difference in the mean percentage inhibition between the two ticagrelor doses at any time point (P > 0.05)
Summary
Study has found that the mean P2Y12 reaction units (PRU) value in Chinese patients after ticagrelor treatment (90-mg bid) is far below the previous thresholds associated with a bleeding risk[16]. Previous studies have suggested that exposure to ticagrelor and AR-C124910XX is higher in Asian than in Caucasian subjects[15,17]. These findings raise a clinical question as to whether the current recommended dose of ticagrelor is suitable for the Chinese population. We conducted this study to assess the antiplatelet effect and pharmacokinetic profile of low-dose ticagrelor (90-mg loading dose followed by a 45-mg bid maintenance dose [MD]) in healthy Chinese volunteers
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