Tenofovir diphosphate intracellular concentration following tenofovir alafenamide administration in bictegravir‐containing vs . dolutegravir‐containing antiretroviral regimens

This study investigates intracellular (IC) exposure of tenofovir alafenamide (TAF) and its clinical determinants in experienced people living with HIV. We conducted a monocentric retrospective analysis of 86 adults treated with either bictegravir (BIC)‐ or dolutegravir (DTG)‐containing regimen. Plasma and IC trough concentrations (C trough ) of tenofovir diphosphate (TFV‐DP) were examined in relation to demographic and renal parameters. A significant correlation emerged between plasma and IC TFV‐DP C trough . Higher plasma TFV levels were associated with older age and reduced estimated glomerular filtration rate. Adherence calculated as proportion of days covered (PDC) did not differ between regimens. These findings provide novel real‐world insights into IC TFV‐DP pharmacokinetics and suggest that BIC‐containing regimens may enhance IC drug accumulation, although the impact of this observation on virological outcomes requires further studies.

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Publication Details

Journal
British Journal of Clinical Pharmacology
Published
2026-10-30
DOI
https://doi.org/10.1002/bcp.70881
Primary Topic
HIV/AIDS drug development and treatment
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article
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article

Tenofovir diphosphate intracellular concentration following tenofovir alafenamide administration in bictegravir‐containing vs . dolutegravir‐containing antiretroviral regimens

Amedeo De Nicolò, Silvia Fantino, Alice Palermiti, Erica Clemente et al.
British Journal of Clinical Pharmacology
HIV/AIDS drug development and treatment
article

Tenofovir diphosphate intracellular concentration following tenofovir alafenamide administration in bictegravir‐containing vs . dolutegravir‐containing antiretroviral regimens

Amedeo De Nicolò, Silvia Fantino, Alice Palermiti, Erica Clemente, Antonio D’Avolio, Sara Soloperto, Viviana Maccario, Stefano Bonora, Giovanni Di Perri, Sergio Maria Ferrara, Federica Barrera
article en

Abstract

This study investigates intracellular (IC) exposure of tenofovir alafenamide (TAF) and its clinical determinants in experienced people living with HIV. We conducted a monocentric retrospective analysis of 86 adults treated with either bictegravir (BIC)‐ or dolutegravir (DTG)‐containing regimen. Plasma and IC trough concentrations (C trough ) of tenofovir diphosphate (TFV‐DP) were examined in relation to demographic and renal parameters. A significant correlation emerged between plasma and IC TFV‐DP C trough . Higher plasma TFV levels were associated with older age and reduced estimated glomerular filtration rate. Adherence calculated as proportion of days covered (PDC) did not differ between regimens. These findings provide novel real‐world insights into IC TFV‐DP pharmacokinetics and suggest that BIC‐containing regimens may enhance IC drug accumulation, although the impact of this observation on virological outcomes requires further studies.

British Journal of Clinical Pharmacology
University of Turin (IT)
Openalex Percentile: Top 12%
HIV/AIDS drug development and treatment
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