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Исследования нового антиагреганта
The Effect of Elinogrel on High Platelet Reactivity During Dual Antiplatelet Therapy and the Relation to CYP 2C19*2 Genotype: First Experience in Patients
Paul A. Gurbel, M.D., Kevin P. Bliden, B.S., Mark J. Antonino B.S., Gillian Stephens, Ph.D.*, Daniel D. Gretler, M.D.*, Marzena M. Jurek, M.S.*, Ruth E. Pakyz, BS.**, Alan R. Shuldiner MD.**, Pamela B. Conley, Ph.D.*, Udaya S. Tantry, Ph.D.
Summary: To study the effect of a new direct acting reversible P2Y12 inhibitor, elinogrel (PRT060128) and the relation to cytochrome P450 (CYP) polymorphisms in patients with High platelet reactivity ( HPR) on standard dual antiplatelet therapy.
Methods and Results: We studied the pharmacodynamic and pharmacokinetc effects of a single 60 mg oral dose of elinogrel in 20 of 45 previously stented stable patients with HPR. We also genotyped for CYP2C19*2,3,5,17 and CYP3A5* 3. Platelet reactivity fell within 4 hours of dosing, the earliest time point evaluated as measured by the following assays: maximum 5 μM and 10 μM ADP LTA (p<0.001 for both vs. pre-dosing); maximum 20 μM ADP LTA (p <0.05); VerifyNow (p<0.001); thrombelastography (p<0.05); VASP phosphorylation (p<0.01); and perfusion chamber assay (p<0.05); and was reversible within 24 hours in these same assays (p=NS vs. pre-dosing for all assays). CYP2C19*2 was present in 44% of all patients but was more frequent in HPR patients (77% vs. 16%, p=0.0004).
Conclusions: HPR is reversibly overcome by a single 60 mg oral dose of elinogrel, a drug now being investigated in a phase 2 trial. CYP2C19*2 was associated with HPR during conventional dual antiplatelet therapy.
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