Tenofovir disoproxil fumarate: A nucleotide reverse transcriptase inhibitor for the treatment of HIV infection

Fung, Horatio B.; Stone, Elizabeth; Piacenti, Frank J.

doi:10.1016/s0149-2918(02)80058-3

Cited by 129 publications

(83 citation statements)

References 39 publications

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“…Tenofovir disoproxil fumarate (tenofovir DF, TDF) is the first nucleotide analogue reverse transcriptase inhibitor approved for the treatment of HIV infection [1]. The potency of TDF has been demonstrated in treatmentexperienced [2,3] and in treatment-naive patients [4].…”

Section: Introductionmentioning

confidence: 99%

Minor changes in calculated creatinine clearance and anion‐gap are associated with tenofovir disoproxil fumarate‐containing highly active antiretroviral therapy

et al. 2006

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BackgroundTenofovir disoproxil fumarate (Tenofovir DF, TDF), the first nucleotide reverse transcriptase inhibitor approved for the treatment of HIV disease, has been associated with renal dysfunction in isolated cases. The aim of this study was to assess changes in renal parameters in individuals receiving TDFand non-TDF-containing highly active antiretroviral therapy (HAART). MethodsAll individuals on HAART attending our clinic were included in the analysis. Time-weighted changes in serum creatinine, calculated creatinine clearance (CCrCl) and anion-gap were assessed for individuals on TDF-and non-TDF HAART. ResultsOf 948 individuals on HAART, 290 (31%) and 618 (65%) were on TDF-and non-TDF HAART, with 40 (4%) having ceased TDF HAART. Baseline values for serum creatinine, CCrCl and anion-gap were similar for those on TDF-and non-TDF HAART. In a multivariate analysis, statistically significant differences were observed in time-weighted change from baseline in anion-gap and CCrCl between individuals on TDF-and non-TDF HAART [mean difference in change between groups: anion-gap 0.78 mmol/L (standard error, 0.19) and CCrCl À 6.80 (standard error 2.2); P 5 0.005 and P 5 0.032, respectively] after adjusting for baseline anion-gap and CCrCl, respectively. Two cases of TDF-associated renal failure were observed. ConclusionOvert renal failure with TDF HAART is rare. However, subtle but statistically significant changes in anion-gap and CCrCl were observed which were associated with TDF HAART. These parameters may be of use in monitoring individuals on HAART. Cidofovir and adefovir, compounds structurally related to TDF, have been associated with an increased risk of acute renal insufficiency. In particular, a dose-and timedependent development of a Fanconi-like syndrome has been reported [5,6]. In pivotal studies assessing the safety and efficacy of TDF, renal safety profiles were found to be similar in individuals receiving and in those not receiving TDF-containing highly active antiretroviral therapy (HAART) [2][3][4]. In addition, a recent large cohort has described no significant evidence of renal dysfunction with the use of TDF in clinical practice [7]. However, there are mounting numbers of anecdotal reports describing Fanconi's syndrome and renal insufficiency induced by TDF therapy [8][9][10][11][12][13][14][15][16][17][18]. Predisposing factors for the development of acute renal failure with the use of TDF remain obscure.Several groups reporting no significant evidence of renal dysfunction with the use of TDF have relied on serum creatinine as a marker of renal function [7]. A recent report utilizing glomerular filtration rate (GFR) calculated on the basis of a 24-h urine collection has observed a lower GFR associated with TDF treatment [19].The aim of this study was to investigate changes in anion-gap and calculated creatinine clearance (CCrCl) in a large cohort of HIV-1-infected individuals receiving TDFand non-TDF-containing HAART. Methods Study designAll individuals currently on HAART attending the Departmen...

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Section: Introductionmentioning

confidence: 99%

Minor changes in calculated creatinine clearance and anion‐gap are associated with tenofovir disoproxil fumarate‐containing highly active antiretroviral therapy

et al. 2006

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“…TE is active against a variety of drug resistant HIV-I strains. Recently, the combination of EM and TE has demonstrated significantly greater HIV RNA suppression compared to the combination of zidovudine and lamivudine [1][2][3] Several analytical methods that have been reported for the individual determination of TE in biological fluids and pharmaceutical formulations which include liquid chromatography coupled with spectrofluorimetric, UV, and mass spectroscopy detection [4][5][6][7][8][9][10] . For EM several analytical methods have been reported for its individual analysis which includes chiral liquid chromatography, liquid chromatography with UV detection [11][12][13] .…”

Section: Tenofovir (Te; 9-[(r)-2-[[bis[[(isopropoxycarbonyl) Oxy] Metmentioning

confidence: 99%

Simultaneous Determination of Emtricitabine and Tenofovir by Area Under Curve and Dual Wavelength Spectrophotometric Method

Ghorpade¹,

Sali²,

Kategaonkar³

et al. 2010

J. Chil. Chem. Soc.

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Two methods for the simultaneous determination of Emtricitabine and Tenofovir by spectroscopy have been developed. These two simple, accurate and precise methods include Area Under the Curve (AUC) method and Dual Wavelength Method. From a solvent effect studies and the spectral behaviours of Emtricitabine and Tenofovir, methanol was selected as solvent. Emtricitabine shows maximum absorbance at 281 nm and Tenofovir shows maximum absorbance at 259 nm. For the AUC method, the wavelength ranges between 242-248 nm and 269-275 nm were selected with reference to the absorbance curves plotted between the wavelengths of 200-400 nm. In the second method i.e. Dual method in which two wavelengths were selected for each drug in a way so that the difference in absorbance is zero for another drug. Emtricitabine shows equal absorbance at 230.696 nm and 250 nm, where the differences in absorbance were measured for the determination of Tenofovir. Similarly, differences in absorbances at 250 nm and 268.670 nm were measured for determination of Emtricitabine. These methods allows rapid analysis of two drug combination. The results of analysis were validated statistically and by recovery studies. This tablet containing both drugs was assayed using the methods developed, showing a good accuracy and precision.

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“…[9][10][11][12][13] . Literature reveals that the above three molecules HIV integrase inhibitors, nucleoside reverse transcriptase inhibitors and nucleotide reverse transcriptase inhibitors from three originated medicines being used to treat HIV/AIDS 14,15 .…”

Section: Introductionmentioning

confidence: 99%

A Stability-Indicating HPLC Method for the Determination of Potential Impurities in a New Fixed Dose Combination of Dolutegravir, Lamivudine and Tenofovir Disoproxil Fumarate Tablets Used in the First Line Treatment of Hiv-1 Infection

Jagadabi¹,

Kumar²,

Pamidi³

et al. 2018

Int. Res. J. Pharm.

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Developing a single method for the quantification of related compounds for a combination product containing three active ingredients is difficult task. Separation and compromising run time to elute all known and unknown degradation products are crucial for a combination product. The aim of current work is to develop a new stability indicative method and validate for a fixed dose combination product containing dolutegravir, lamivudine, tenofovir disoproxil fumarate and their potential impurities in a single run by HPLC. The critical separation between dolutegravir, lamivudine, tenofovir disoproxil fumarate and its impurities was successfully attained by a new core-shell bi-phenyl, 250x4.6mm, 5µm column with a run time of 150 min. The run time was 150min. Forced degradation studies were verified to prove the stability-indicating nature of the method. Stability-indicating nature was confirmed by peak purity of all the three active components and impurities. The developed method was validated to prove the potentiality of the method as per ICH guidelines with respect to specificity, linearity, accuracy, precision ad robustness. The sensitivity of the method was proved by establishing limit of detection (LOD) and limit of quantification (LOQ) of for dolutegravir, lamivudine, tenofovir disoproxil fumarate and potential impurities.

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Tenofovir disoproxil fumarate: A nucleotide reverse transcriptase inhibitor for the treatment of HIV infection

Cited by 129 publications

References 39 publications

Minor changes in calculated creatinine clearance and anion‐gap are associated with tenofovir disoproxil fumarate‐containing highly active antiretroviral therapy

Minor changes in calculated creatinine clearance and anion‐gap are associated with tenofovir disoproxil fumarate‐containing highly active antiretroviral therapy

Simultaneous Determination of Emtricitabine and Tenofovir by Area Under Curve and Dual Wavelength Spectrophotometric Method

A Stability-Indicating HPLC Method for the Determination of Potential Impurities in a New Fixed Dose Combination of Dolutegravir, Lamivudine and Tenofovir Disoproxil Fumarate Tablets Used in the First Line Treatment of Hiv-1 Infection

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