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. 2016 Aug 24:6:31838.
doi: 10.1038/srep31838.

Low-dose ticagrelor yields an antiplatelet efficacy similar to that of standard-dose ticagrelor in healthy subjects: an open-label randomized controlled trial

Pan Li  1 , Ying Gu  1 , Yawei Yang  1 , Lizhi Chen  2 , Junmei Liu  1 , Lihong Gao  2 , Yongwen Qin  1 , Quancai Cai  3 , Xianxian Zhao  1 , Zhuo Wang  2 , Liping Ma  1
Affiliations

Low-dose ticagrelor yields an antiplatelet efficacy similar to that of standard-dose ticagrelor in healthy subjects: an open-label randomized controlled trial

Pan Li et al. Sci Rep. .

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.

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Conflict of interest statement

The authors declare no competing financial interests.

Figures

Figure 1
Figure 1. Flow chart. LD, loading dose; BID, twice daily; QD, once daily.
Figure 2
Figure 2. Platelet reactivity as assessed by the VerifyNow P2Y12 assay across time points.
(A) Mean % inhibition of PRU after LD and MD of standard-dose ticagrelor, low-dose ticagrelor or clopidogrel. †P < 0.001, *P < 0.05, low-dose ticagrelor vs clopidogrel. (B) The individual PRU values at all time points. LD, loading dose; BID, twice daily; PRU, P2Y12 reaction units.
Figure 3
Figure 3
Mean plasma concentrations of ticagrelor (A) and AR-C124910XX (B) across time points.
Figure 4
Figure 4. Ticagrelor plasma concentration versus % inhibition of PRU.
PRU, P2Y12 reaction units.
See this image and copyright information in PMC

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