A Pharmacokinetic Analysis and Pharmacogenomic Study of 6-mercaptopurine

Vicha A, Katsila T, Giannopoulou E, Leontari H, El Mubarak M, Gravia A, Chondrou V, Symeonidis A, Patrinos GP, Kalofonos HP and Sivolapenko G*

Background: 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.

Materials and Methods: 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.

Results and Conclusion: 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.

Keywords: 6-Mercaptopurine; Pharmacokinetic analysis; Thiopurine S-methyl transferase

Published on: May 23, 2015 Pages: 2-7

Full Text PDF Full Text HTML DOI: 10.17352/ijpsdr.000002
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