A Pharmacokinetic Analysis and Pharmacogenomic Study of 6-mercaptopurine

<p><strong>Background:</strong> The efficacy and safety of 6-mercaptopurine (6-MP) therapy rely on the concentration of its metabolites. The aim of the current study is the pharmacokinetic analysis of 6-MP and the detection of its metabolites as well as the role of Thiopurine S-met...

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Main Authors: Vicha A (Author), Katsila T (Author), Giannopoulou E (Author), Leontari H (Author), El Mubarak M (Author), Gravia A (Author), Chondrou V (Author), Symeonidis A (Author), Patrinos GP (Author), Kalofonos HP (Author), Sivolapenko G (Author)
Format: Book
Published: International Journal of Pharmaceutical Sciences and Developmental Research - Peertechz Publications, 2015-05-23.
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Summary:<p><strong>Background:</strong> The efficacy and safety of 6-mercaptopurine (6-MP) therapy rely on the concentration of its metabolites. The aim of the current study is the pharmacokinetic analysis of 6-MP and the detection of its metabolites as well as the role of Thiopurine S-methyl transferase (TPMT), the enzyme associated with 6-MP metabolism, as a pharmacogenomics biomarker.</p><p><strong>Materials and Methods:</strong> Data were collected from 19 patients with different types of leukemia and lymphoma who received 6-MP chemotherapy. Pharmacokinetic analysis was performed using an HPLC. The VNTR promoter polymorphisms of TPMT were detected.</p><p><strong>Results and Conclusion:</strong> The pharmacokinetic analysis confirmed the heterogeneity of the 6-MP metabolism. The TPMT genotyping revealed a correlation between the TPMT*3C variant and increased levels of 6-thioguanine nucleotides (TGs). No methylation pattern was obtained.</p>
DOI:10.17352/ijpsdr.000002