scholarly journals Nelfinavir Mesylate

2020 ◽  
Author(s):  
Keyword(s):  
Nelfinavir Mesylate

scholarly journals Spectrophometric Determination of Nelfinavir Mesylate

2006 ◽  
Vol 3 (2) ◽  
pp. 78-82 ◽  
Author(s):  
K. Vanitha Prakash ◽  
Jangala Venkateswara Rao
Keyword(s):  
Ferric Chloride ◽  
Dosage Form ◽  
Potassium Ferricyanide ◽  
Reagent Blank ◽  
Spectrophotometric Methods ◽  
Bluish Green ◽  
Nelfinavir Mesylate ◽  
Bulk Drug ◽  
Tablet Dosage

Two new simple, sensitive, rapid and economical Spectrophotometric Methods (A and B) have been developed for the determination of Nelfinavir Mesylate in pharmaceutical bulk and tablet dosage form. The method A is based on the reaction of Nelfinavir with ferric chloride, potassium ferricyanide and hydrochloric acid to form a bluish green colored chromogen. The Method B is based on the formation of blood red colored chromogen with Ferric chloride and 1,10-phenanthroline. The absorbances of the chromogen were measured at their respective wavelength of maximum absorbance against the corresponding reagent blank. The proposed methods have been successfully applied to the analysis of the bulk drug and its tablet dosage form. The methods have been statistically evaluated and were found to be precise and accurate.

scholarly journals Activities of the human immunodeficiency virus type 1 (HIV-1) protease inhibitor nelfinavir mesylate in combination with reverse transcriptase and protease inhibitors against acute HIV-1 infection in vitro.

1997 ◽  
Vol 41 (10) ◽  
pp. 2159-2164 ◽  
Author(s):  
A K Patick ◽  
T J Boritzki ◽  
L A Bloom
Keyword(s):  
Human Immunodeficiency Virus ◽  
Protease Inhibitors ◽  
Drug Combination ◽  
Cellular Cytotoxicity ◽  
Immunodeficiency Virus ◽  
Nelfinavir Mesylate ◽  
Acute Hiv ◽  
Hiv 1

Nelfinavir mesylate (formerly AG1343) is a potent and selective, nonpeptidic inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that was discovered by protein structure-based design methodologies. We evaluated the antiviral and cytotoxic effects of two-drug combinations of nelfinavir with the clinically approved antiretroviral therapeutics zidovudine (ZDV), lamivudine (3TC), dideoxycytidine (ddC; zalcitabine), stavudine (d4T), didanosine (ddI), indinavir, saquinavir, and ritonavir and a three-drug combination of nelfinavir with ZDV and 3TC against an acute HIV-1 strain RF infection of CEM-SS cells in vitro. Quantitative assessment of drug interaction was evaluated by a universal response surface approach (W. R. Greco, G. Bravo, and J. C. Parsons, Pharm. Rev. 47:331-385, 1995) and by the method of M. N. Prichard and C. Shipman (Antiviral Res. 14:181-206, 1990). Both analytical methods yielded similar results and showed that the two-drug combinations of nelfinavir with the reverse transcriptase inhibitors ZDV, 3TC, ddI, d4T, and ddC and the three-drug combination with ZDV and 3TC resulted in additive to statistically significant synergistic interactions. In a similar manner, the combination of nelfinavir with the three protease inhibitors resulted in additive (ritonavir and saquinavir) to slightly antagonistic (indinavir) interactions. In all combinations, minimal cellular cytotoxicity was observed with any drug alone and in combination. These results suggest that administration of combinations of the appropriate doses of nelfinavir with other currently approved antiretroviral therapeutic agents in vivo may result in enhanced antiviral activity with no associated increase in cellular cytotoxicity.

The Antiretroviral Agent Nelfinavir Mesylate

2017 ◽  
Vol 70 (1) ◽  
pp. 115-126 ◽  
Author(s):  
Cecilia G. Sanchez ◽  
Steven V. Molinski ◽  
Rafael Gongora ◽  
Meredith Sosulski ◽  
Taylor Fuselier ◽  
...  
Keyword(s):  
Nelfinavir Mesylate

scholarly journals Lack of Pharmacokinetic Drug Interaction between Tenofovir Disoproxil Fumarate and Nelfinavir Mesylate

2005 ◽  
Vol 49 (10) ◽  
pp. 4386-4389 ◽  
Author(s):  
Marta Boffito ◽  
Anton Pozniak ◽  
Brian P. Kearney ◽  
Christopher Higgs ◽  
Anita Mathias ◽  
...  
Keyword(s):  
Drug Interaction ◽  
Healthy Volunteers ◽  
Tenofovir Disoproxil Fumarate ◽  
Time Curve ◽  
Once Daily ◽  
Dosing Interval ◽  
Pharmacokinetic Drug Interaction ◽  
Nelfinavir Mesylate ◽  
Pharmacokinetic Drug

ABSTRACT A study explored the pharmacokinetics of tenofovir (300 mg administered once daily) and nelfinavir (1,250 mg twice daily) when coadministered in 29 healthy volunteers. Tenofovir, nelfinavir, and M8 pharmacokinetics was unaltered when tenofovir and nelfinavir were coadministered, and tenofovir administration did not affect the M8/nelfinavir area under the concentration-versus-time curve over the dosing interval (AUCtau) ratio. No interaction between tenofovir and nelfinavir was observed.

Spectrophotometric Methods for the Determination of Nelfinavir Mesylate

2004 ◽  
Vol 59 (6) ◽  
pp. 552-556 ◽  
Author(s):  
Seshagiri V. M. Mohan Rao ◽  
Tadi R. S. Reddy ◽  
Isukapatla N. Rao ◽  
Chilukuri S. P. Sastry
Keyword(s):  
Spectrophotometric Methods ◽  
Nelfinavir Mesylate

scholarly journals The anti-HIV Drug Nelfinavir Mesylate (Viracept) is a Potent Inhibitor of Cell Fusion Caused by the SARS-CoV-2 Spike (S) Glycoprotein Warranting further Evaluation as an Antiviral against COVID-19 infections

2020 ◽  
Author(s):  
Farhana Musarrat ◽  
Vladimir Chouljenko ◽  
Rafiq Nabi ◽  
Achyut Dahal ◽  
Seetharama D. Jois ◽  
...  
Keyword(s):  
Cell Fusion ◽  
Neutralizing Antibodies ◽  
Antiviral Drug ◽  
Proteolytic Processing ◽  
Viral Envelope ◽  
Hiv Protease ◽  
Virus Infectivity ◽  
Dependent Manner ◽  
African Green Monkey Kidney ◽  
Nelfinavir Mesylate

AbstractCoronaviruses belong to a group of enveloped, positive-single stranded RNA viruses that are known to cause severe respiratory distress in animals and humans. The current SARS coronavirus-2 (SARS CoV-2) pandemic has caused more than 2,000,000 infections globally and nearly 200,000 deaths. Coronaviruses enter susceptible cells via fusion of the viral envelope with the plasma membrane and/or via fusion of the viral envelope with endosomal membranes after endocytosis of the virus into endosomes. Previous results with SARS and MERS CoV have shown that the Spike (S) glycoprotein is a major determinant of virus infectivity and immunogenicity. Herein, we show that expression of SARS CoV-2 S (S-n) glycoprotein after transient transfection of African green monkey kidney (Vero) cells caused extensive cell fusion in comparison to limited cell fusion caused by the SARS S (S-o) glycoprotein. S-n expression was detected intracellularly and on transfected Vero cell surfaces and caused the formation of very large multinucleated cells (syncytia) by 48 hours post transfection. These results are in agreement with published pathology observations of extensive syncytial formation in lung tissues of COVID-19 patients. This differential S-n versus S-o-mediated cell fusion suggests that SARS-CoV-2 is able to spread from cell-to-cell much more efficiently than SARS effectively avoiding extracellular spaces and neutralizing antibodies. A systematic screening of several drugs for ability to inhibit S-n and S-o cell fusion revealed that the FDA approved HIV-protease inhibitor, nelfinavir mesylate (Viracept) drastically inhibited S-n and S-o-mediated cell fusion in a dose-dependent manner. Complete inhibition of cell fusion was observed at a 10 micromolar concentration. Computational modeling and in silico docking experiments suggested the possibility that nelfinavir may bind inside the S trimer structure, proximal to the S2 amino terminus directly inhibiting S-n and S-o-mediated membrane fusion. Also, it is possible that nelfinavir mesylate acts on cellular processes to inhibit S proteolytic processing. These results warrant further investigations of the potential of nelfinavir mesylate as an antiviral drug, especially at early times after SARS-CoV-2 symptoms appear.

scholarly journals Nelfinavir Is Active Against SARS-CoV-2 in Vero E6 Cells

2020 ◽  
Author(s):  
Zhijian Xu ◽  
Hangping Yao ◽  
Jingshan Shen ◽  
Nanping Wu ◽  
Yechun Xu ◽  
...  
Keyword(s):  
Cellular Level ◽  
Effective Concentration ◽  
High Potency ◽  
Response Curves ◽  
Main Protease ◽  
Similar Dose ◽  
Nelfinavir Mesylate ◽  
Half Maximal Effective Concentration ◽  
Computational Drug Discovery ◽  
Target Agent

Utilizing an integrative computational drug discovery approach, we predicted that nelfinavir is a potential inhibitor of SARS-CoV-2 main protease. Further docking nelfinavir to 30 potential target proteins of COVID-19, we found that nelfinavir is most probably a multi-target agent. The half-maximal effective concentration (EC<sub>50</sub>) of nelfinavir mesylate against SARS-CoV-2 was 2.89±0.65 μM while that of remdesivir was 1.00±0.34 μM, both drugs showed similar dose-response curves. Based on its high potency against SARS-CoV-2 at cellular level, its higher exposure in lung than in plasma, its good safe profile and its potential to reduce inflammation, nelfinavir deserves further exploration for the treatment of COVID-19.

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