Quantitative determination of clopidogrel and its metabolites in biological samples: A mini-review

Clopidogrel has been applied in antiplatelet therapy since 1998 and is the thienopyridine with the largest clinical experience. By 2011, clopidogrel (Plavix®) was the second top-selling drug in the world. Following complete patent expiry in 2012/2013 its use is expected to grow even further from generics entering the market. Prefaced by a brief description of clopidogrel metabolism, this review analyzes analytical methods addressing the quantification of clopidogrel and its metabolites in biological samples. Techniques that have been applied to analyze human plasma or serum are predominantly LC–MS and LC–MS/MS. The lowest level of clopidogrel quantification that has been achieved is 5 pg/mL, the shortest runtime is 1.5 min and almost 100% recovery has been reported using solid-phase extraction for sample preparation.

Figure optionsDownload as PowerPoint slideHighlights
► Overview of analytical techniques for the quantification of clopidogrel and clopidogrel carboxylic acid in biological samples.
► New developments addressing the determination of the active clopidogrel metabolite.
► Thorough comparison of validation data obtained by the reviewed literature reports.