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The introduction of irinotecan has revolutionized the applicability of camptothecins as predominant topoisomerase I inhibitor for anti‐cancer therapy. The potent anti‐tumor activity of irinotecan is due to rapid formation of an in vivo active metabolite, SN‐38. Therefore, irinotecan is considered as a pro‐drug to generate SN‐38. Over the past decade, side‐by‐side with the clinical advancement of the use of irinotecan in the oncology field, a plethora of bioanalytical methods have been published to quantify irinotecan, SN‐38 and other metabolites. Because of the availability of HPLC, LC‐MS and LC‐MS/MS methods, the pharmacokinetic profiling of irinotecan and its metabolites has been accomplished in multiple species, including cancer patients. The developed assays continue to find use in the optimization of newly designed delivery systems with regard to pharmacokinetics to promote safe and effective use of …