Safety,pharmacokinetic and pharmacodynamic studies of batifiban injection following single- and multiple-dose administration to healthy Chinese subjects |
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Authors: | Hui Chen Jian Qiao Qian Li Jungang Deng Zhirong Tan Tao Guo Weiyong Li |
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Affiliation: | 1. Department oflnfectious DiseaseUnion Hospital, Tongji Medical College,Huazhong University of Science and Technology, Wuhan 430022, China 2. Institute of Clinic PharmacyUnion Hospital, Tongji Medical College,Huazhong University of Science and Technology, Wuhan 430022, China 3. Department of Hematology,Union Hospital, Tongji Medical College,Huazhong University of Science and Technology, Wuhan 430022, China 4. Institute of Clinical Pharmacology, Central South University, Changsha 410083, China |
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Abstract: | Summary Batifiban, a synthetic cyclic peptide, is a potent platelet glycoprotein GPIIb/IIIa antagonist which may be useful in the
treatment and prevention of acute coronary syndromes. The pharmacokinetics and pharmacodymanic (inhibition of platelet aggregation)
effects, and tolerability of batifiban were investigated in healthy subjects following single bolus injection with doses of
55, 110, or 220 μg/kg, or multiple doses of an bolus followed intravenous infusion for 24 h (180 μg/kg plus 2.0 μg/min·kg,
and 220 μg/kg plus 2.5 μg/min·kg) in this phase I clinical trial. Plasma levels of batifiban and areas under the curve were
found to be proportional to doses. Batifiban was rapidly eliminated with a half-life of approximately 2.5 h. Significant differences
were noted for plasma levels of batifiban and areas under the curve between males and females. No significant differences
in the terminal half-life were found between males and females. Batifiban reversibly inhibited ex vivo platelet aggregation in a dose- and concentration-dependent manner, consistent with its mechanism as a GPIIb/IIIa antagonist.
Single and multiple intravenous doses of batifiban were found to be safe and well tolerated in healthy subjects. These results
support a bolus injection plus intravenous infusion regimen of batifiban for the treatment and prevention of acute coronary
syndromes. |
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Keywords: | Batifiban platelet aggregation pharmacokinetics and pharmacodynamics |
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