07/06/2018 - Role of transporters in drug ADME

Tenofovir Alafenamide and Tenofovir Disoproxil Fumarate are not transported by Concentrative Nucleoside Transporter 2

Cusato J, Calcagno A, De Nicolò A, Mogyorosi K, D’Avolio A, Di Perri G, Bonora S.

Diagn Microbiol Infect Dis. 2019 Jun;94(2):202-204. doi:10.1016/j.diagmicrobio.2018.07.001. Epub 2018 Jul 6.

PMID: 30922593


Tenofovir-associated renal toxicity is influenced by several factors, including plasma exposure and genetic variants in transporter-encoding genes. Tenofovir plasma exposure has been associated with a polymorphism in SLC28A2 gene (encoding the concentrative nucleoside transporter 2, CNT2): particularly, SLC28A2 124 CT/TT genotype patients show higher plasma tenofovir concentrations, compared to CC group. In literature, substrate studies are lacking; for this reason, our aim was to understand if tenofovir and tenofovir-alafenamide are CNT2 substrates. We performed an in vitro study using CNT2 expressing MDCKII cells. We observed that tenofovir and tenofovir-alafenamide are not substrates of CNT2. Tenofovir alafenamide influx pathway remains to be clarified.

Keywords: CNT2; HAART; HIV; Renal toxicity; SLC28A2; TAF; TDF.

Copyright © 2018 Elsevier Inc. All rights reserved.

open_in_new Read the Source

Next: Correlation Analysis of Potential Breast Cancer Resistance Protein Probes in Different Monolayer Systems

Previous: Human OATP1B1 (SLCO1B1) transports sulfated bile acids and bile salts with particular efficiency