Bioanalysis Zone

Identification of a novel human circulating metabolite of tenofovir disoproxil fumarate with LC–MS/MS

0

Background: Tenofovir disoproxil fumarate (TDF) is an antiretroviral drug used for the treatment of Human Immunodeficiency Virus and Hepatitis B infections. Results: A metabolite that has previously not been observed in the circulation of humans was detected by LC–MS/MS in early time point plasma samples following administration of TDF to healthy volunteers. The metabolite was identified using a range of LC–MS/MS-based techniques as a monoester of TDF, derived from the partially hydrolyzed bis-ester prodrug. TDF, when spiked into plasma, was observed to degrade first to the putative monoester and subsequently to tenofovir. Conclusion: The presence of this unstable metabolite in some samples has implications for sample collection, handling and storage in studies of tenofovir where serum concentrations are determined.

To view restricted content, please:

Share:

Leave A Comment

Please wait...

Bioanalysis Zone New Investigator Award

Why not start this year by doing something good by nominating an early career scientist for the Bioanalysis Zone New Investigator Award. Complete the details below to register your interest!