Application of a Sensitive Liquid Chromatography-Tandem Mass Spectrometric Method to Pharmacokinetic Study of Telbivudine in Humans

Introduction

Telbivudine is a synthetic L-nucleoside analogue, which is phosphorylated to its active metabolite, 5’-triphosphate, by cellular kinases. The telbivudine 5’-triphosphate inhibits HBV DNA polymerase (a reverse transcriptase) by competing with the natural substrate, dTTP. Incorporation of 5’-triphosphorylated-telbivudine into viral DNA obligates DNA chain termination, resulting in inhibition of HBV replication. The objectives of the current studies were to develop a selective and sensitive LC-MS/MS method to determine of telbivudine in human plasma.

June 12, 2014 GMT