Individual dose of tofacitinib based on pharmacokinetic and pharmacogenomic analysis

2016 Fiscal Year Final Research Report

• Project/Area Number: 26860100
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Medical pharmacy
• Research Institution: Shiga University of Medical Science
• Principal Investigator: Hira Daiki 滋賀医科大学, 医学部, 特任助教 (50636959)
• Research Collaborator: TERADA TOMOHIRO 滋賀医科大学, 医学部, 教授 (10324641)
• Project Period (FY): 2014-04-01 – 2017-03-31
• Keywords: 個別医療 / トファシチニブ / 薬物動態 / 関節リウマチ

Outline of Final Research Achievements

The aim of the present study is to develop the individual dose of tofacitinib, which is a novel synthetic disease modifying anti-rheumatic drug (DMARD) that selectively inhibits Janus kinase (JAKs), particularly JAK1 and JAK3.
In the present study, a novel and simple HPLC-UV assay method for the estimation of tofacinib concentration has been developed and validated. Transport characteristics of ABCB1 (P-glycoprotein, P-gp) and ABCG2 (breast cancer resistance protein, BCRP) were assessed by HEK293 cells stably expressing ABCB1 and ABCG2. The cellular accumulation of tofacitinib in HEK293-ABCB1 and HEK293-ABCG2 were markedly decreased than that in HEK293 cell as a control. These findings suggest that pharmacogenomic analysis help to optimize the individual dose of tofacitinib.

Free Research Field

医療薬学