A prodrug of the antiviral tenofovir
Tenofovir disoproxil fumarate is a nucleotide reverse transcriptase inhibitor that inhibits the replication of human immunodeficiency virus (HIV) in MT-2 cells and PBMC with the half maximal effective concentration EC50 values of 0.007 μmol/L and 0.005 μmol/L [1].
Shortly upon administration, tenofovir disoproxil fumarate rapidly goes through esterase hydrolysis removing the two ester groups and yielding tenofovir, which is a nucleotide analogue with anti-viral activity against retroviruses including HIV-1, HIV-2 and hepadnaviruses. Tenofovir is phosphorylated by cellular nucleotide kinase and adenylate kinase and eventually converted into its active anabolite tenofovir diphosphate, which inhibits HIV-1 reverse transcriptase and terminates the growing DNA chain [2].
参考文献:
[1] Fung HB, Stone EA, Piacenti FJ. Tenofovir disoproxil fumarate: a nucleotide reverse transcriptase inhibitor for the treatment of HIV infection. Clin Ther. 2002 Oct;24(10):1515-48.
[2] Brian P. Kearney, John F. Flaherty, Jaymin Shah. Tenofovir Disoproxil Fumarate. Clinical Pharmacokinetics. August 2004, Volume 43, Issue 9, pp 595-612
| Cell experiment [1]: | |
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Cell lines |
MT-2 cells and PBMCs |
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Preparation method |
The solubility of this compound in DMSO is > 31.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.007 μM or 0.005 μM |
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Applications |
In MT-2 cells and PBMCs, Tenofovir Disoproxil Fumarate inhibited HIV replication with the EC50 values of 0.007 μM and 0.005 μM, respectively. The anti-HIV activity of Tenofovir Disoproxil Fumarate was shown to be 36- to 90-fold greater than that of Tenofovir. |
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参考文献: [1]. Fung HB, Stone EA, Piacenti FJ. Tenofovir disoproxil fumarate: a nucleotide reverse transcriptase inhibitor for the treatment of HIV infection. Clin Ther. 2002 Oct;24(10):1515-48. | |
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