Tamiflu mechanism of action

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Tamiflu Mechanism of Action: Neuraminidase Inhibition

Tamiflu (oseltamivir) works by targeting the influenza virus's neuraminidase enzyme. This enzyme is essential for the virus because it helps newly formed virus particles escape from infected respiratory cells and spread to other cells in the body. By inhibiting neuraminidase, Tamiflu blocks the release of these new virus particles, effectively stopping the virus from spreading further within the respiratory tract 134.

Molecular Details of Tamiflu Binding to Neuraminidase

Structural studies have shown that oseltamivir binds directly to the active site of the neuraminidase enzyme. This binding prevents the enzyme from functioning, which is crucial for the antiviral effect. Detailed molecular modeling and X-ray diffraction studies confirm that oseltamivir fits into the neuraminidase active site, interacting with key amino acids and blocking its activity 23. The drug’s structure and binding preferences have been mapped, providing insight into how it effectively inhibits the enzyme .

Resistance and Drug Binding Pathways

While resistance to Tamiflu is rare, it can occur due to mutations in the neuraminidase enzyme. Molecular dynamics simulations have revealed that an electrostatic funnel in the neuraminidase helps guide oseltamivir into its binding site. Mutations can disrupt this pathway, making it harder for the drug to bind and thus reducing its effectiveness. Understanding these pathways helps researchers design new drugs that can overcome resistance .

Conclusion

In summary, Tamiflu’s primary mechanism of action is the inhibition of the influenza virus neuraminidase enzyme, which blocks the release and spread of new virus particles in the respiratory tract. This action is well-supported by structural and molecular studies, and while resistance can develop, ongoing research is focused on understanding and overcoming these challenges 1234.

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Most relevant research papers on this topic

Clinical Use of Tamiflu (Oseltamivir)

Oseltamivir (Tamiflu) is a neuraminidase inhibitor used for treating and preventing influenza and avian influenza, with rare resistance development and a recommended adult dose of 75mg b.i.d. for 5 days.

2008·

1citation

·M. Chang et al.

The elusive crystal structure of the neuraminidase inhibitor Tamiflu (oseltamivir phosphate): molecular details of action.

The crystal structure of Tamiflu, the anti-influenza agent, provides insights into its binding preferences and molecular details of its action.

2013·

15citations

·P. Naumov et al.

Synthesis of tamiflu and its phosphonate congeners possessing potent anti-influenza activity.

Oseltamivir and its phosphonate congeners show strong anti-influenza activity, offering potential for new anti-influenza drugs.

Highly Cited

2007·

180citations

·Jiun-Jie Shie et al.

Molecular Dynamics Simulations Suggest that Electrostatic Funnel Directs Binding of Tamiflu to Influenza N1 Neuraminidases

Tamiflu's resistance to influenza N1 neuraminidases is linked to an electrostatic binding funnel, suggesting new drugs could circumvent resistance mechanisms.

2010·

67citations

·Ly Le et al.

Neuroexcitatory actions of Tamiflu and its carboxylate metabolite

Oseltamivir has effects on the central nervous system, especially when combined with other agents, and may cause neuronal firing and hypothermia.

Non-RCTAnimal StudyHighly Cited

2007·

91citations

·Y. Izumi et al.

A broadly protective therapeutic antibody against influenza B virus with two mechanisms of action

46B8 is a superior therapeutic antibody against influenza B virus, providing protection against lethal challenge in mice when administered 72 hours post infection, with an additive antiviral effect when combined with Tamiflu.

In Vitro Study

2017·

60citations

·N. Chai et al.

Synthesis and evaluation of anti-Giardia activity of oseltamivir analogs.

Oseltamivir analogs 3b, 2c, 11i, and 11d show superior anti-Giardia activity compared to the parent oseltamivir.

In Vitro Study

2024·

0citations

·Harrison W VanKoten et al.

Sugar-based synthesis of Tamiflu and its inhibitory effects on cell secretion.

This study presents a practical synthesis of Tamiflu using D-glucal, a readily available starting material, and reveals that its active metabolite, oseltamivir carboxylate, inhibits neuroendocrine PC12 cell secretion, potentially causing side-effects on neuro

2010·

45citations

·Jimei Ma et al.

Oseltamivir (Tamiflu) and its potential for use in the event of an influenza pandemic.

Oseltamivir (Tamiflu) is effective in treating and preventing influenza in adults, adolescents, and children, and is also active against avian influenza virus strains.

Highly Cited

2005·

440citations

·P. Ward et al.

Photocatalytic degradation of the antiviral drug Tamiflu by UV-A/TiO2: Kinetics and mechanisms.

Photocatalytic degradation of Tamiflu by TiO2-P25 under UV-A irradiation effectively removes over 95% of the drug, but its removal efficiency of total organic carbon is only 45.6% and 67.0% after 360 minutes.

2015·

37citations

·Wen-Long Wang et al.

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