ABSTRACT

Tenofovir (TFV) is an acyclic nucleoside phosphonate analog of adenosine 5′-monophosphate and belongs to the nucleotide reverse transcriptase inhibitor (NRTI) class of antiretrovirals. It is converted in vivo by intracellular phosphorylation to its active form, tenofovir diphosphate (TFV-DP), as shown in Figure 232.1. TFV-DP is a competitive inhibitor of human immunodeficiency virus (HIV) reverse transcriptase and is incorporated into the growing DNA chain, causing termination (Squires, 2001). Structure of TFV and its prodrugs TDF and TAF. TFV is phosphorylated to the active TFV-DP. https://s3-euw1-ap-pe-df-pch-content-public-p.s3.eu-west-1.amazonaws.com/9781315152110/08d8042d-9481-4a8d-8c27-9bd589f6de6b/content/fig232_1.tif" xmlns:xlink="https://www.w3.org/1999/xlink"/> (Reprinted with permission from Margot et al. (2015))