Abstract

Tenofovir disoproxil fumarate is a prodrug, i.e. inative substance converted in vivo, after absorption to the active form deesterified tenofovir, which acts as an inhibitor of viral reverse transcriptase. To better understand the toxic effects of these drugs in the environment, three organisms were tested, the effective concentration (EC50) and inhibitory concentration (IC50) of tenofovir disoproxil that resulted in 50% growth inhibition of Microcystis novacekii, 50% immobilization of Artemia salina, and 50% loss of bioluminescence of Aliivibrio fischeri were evaluated. The EC50 value after 96 h of treatment for the cyanobacterium was 161.01 (156.81 - 165.21) mg·L-1; the IC50 value for A. salina after 24 h of treatment was 111.82 (103.18 - 120.45) mg·L-1; and the IC50 at 15 min for A. fischeri was 14.83 (13.87 - 15.79) mg·L-1. The test organism most sensitive to the drug was A. fischeri, indicating the importance of using representative models at different trophic levels to assess the potential risk of drugs for environmental toxicity. These results highlight the possible effect of tenofovir disoproxil on decomposer organisms, which may contribute to the environmental persistence of this drug.

Highlights

  • Drug residues have been reported in several environmental systems and are considered emerging contaminants [1] [2]

  • Tenofovir disoproxil fumarate is a prodrug, i.e. inative substance converted in vivo, after absorption to the active form de-esterified tenofovir, which acts as an inhibitor of viral reverse transcriptase

  • To better understand the toxic effects of these drugs in the environment, three organisms were tested, the effective concentration (EC50) and inhibitory concentration (IC50) of tenofovir disoproxil that resulted in 50% growth inhibition of Microcystis novacekii, 50% immobilization of Artemia salina, and 50% loss of bioluminescence of Aliivibrio fischeri were evaluated

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Summary

Introduction

Drug residues have been reported in several environmental systems and are considered emerging contaminants [1] [2]. Tenofovir disoproxil fumarate (TDF) is an antiretroviral belonging to the class of nucleotide analogs used in the treatment of HIV/AIDS and viral hepatitis. TDF is a prodrug, i.e. inative substance hydrolyzed in vivo to release the active portion of the molecule, tenofovir (TFV) (Figure 1). The prodrug is used to enhance tenofovir liposolubility and permeation across the intestinal cells

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