Individual variability in the disposition of and response to clopidogrel: Pharmacogenomics and beyond

Bioequivalence Study of Clopidogrel 75 Mg Tablets in Healthy Male Volunteers

“…As is now widely accepted that there is marked inter individual variability in the metabolism of clopidogrel. The difference may be related to CYP2C19*2 genotype, which affects the metabolism of clopidogrel [17], Significant variability in the frequencies of CYP2C19 allelic variants has been found among ethnic groups [7,9,11], which may explain ethnicity-specific responses to drugs.…”

“…Although the PK characteristics of clopidogrel have been studied previously [12][13][14][15], all these studies were performed in whites, blacks or Korean volunteers. These PK characteristics may not be fully generalized or extrapolated to the Chinese people due to significantly greater frequencies of the CYP2C19*2 variant alleles in Chinese subjects than white or black subjects [7,9,11]. However, the search of PubMed and Embase in November 30, 2011, using the terms such as clopidogrel, bioavailability, pharmacokinetic and Chinese, did not identify any published reports concerning the PK and bioavailability of clopidogrel in the Chinese population.…”

“…Several studies have shown that ethnicity is one of the important factors that could affect clopidogrel metabolism and its anti-platelet effect [9,10], in part because the allele frequency of CYP2C19*2 variant in the Chinese population (30%) is twice than that in whites (14.7%) and blacks (17.3%) [7,9,11]. Although the PK characteristics of clopidogrel have been studied previously [12][13][14][15], all these studies were performed in whites, blacks or Korean volunteers.…”

Bedside stratification of patients according to CYP2C19*2 genotype

“…Among the non-genetic factors, ethnicity, sex, age, body weight, comorbidities, drug-drug interactions, and other factors might also significantly affect the response to clopidogrel -antiplatelet therapy (Xie et al, 2011).…”

Synthesis of 3-Unsubstituted 4-Aryl-4,7-Dihydrothieno[2,3-b]Pyridine-2,5-Dicarboxylates / 3-Neaizvietotu 4-Aril-4,7-Dihidrotiēno[2,3-B]Piridīn-2,5-Dikarbonskābes Esteru Sintēze

“…Clopidogrel (trade name Plavix) -(+)-(S)-methyl-2-(2-chlorophenyl)-2-(6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl) acetate is an oral antiplatelet agent [4][5][6][7][8]. Methyl 4,7-dihydro-3-isobutyl-6-methyl-4-(3-nitrophenyl)-thieno [2,3-b]pyridine-5-carboxylate (S-312) is widely investigated as a calcium channel blocking agent, potential cardiovascular [9][10][11][12][13][14][15] and anticonvulsant drug [16,17].…”