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Oseltamivir

Generic Name
Oseltamivir
Brand Names
Ebilfumin, Tamiflu
Drug Type
Small Molecule
Chemical Formula
C16H28N2O4
CAS Number
196618-13-0
Unique Ingredient Identifier
20O93L6F9H
Background

Oseltamivir (marketed as the product TamifluⓇ), is an antiviral neuraminidase inhibitor used for the treatment and prophylaxis of infection with influenza viruses A (including pandemic H1N1) and B. Oseltamivir exerts its antiviral activity by inhibiting the activity of the viral neuraminidase enzyme found on the surface of the virus, which prevents budding from the host cell, viral replication, and infectivity.

The clinical benefit of use of oseltamivir is greatest when administered within 48 hours of the onset of influenza symptoms since effectiveness decreases significantly after that point in time; there is generally no benefit in use beyond 48 hours for healthy, low-risk individuals as influenza is a self-limiting illness. However, antiviral treatment might be beneficial when initiated after 48 hours for patients with severe, complicated or progressive illness or for hospitalized patients. According to the CDC, data from clinical trials and observational studies have demonstrated that early antiviral treatment can shorten the duration of fever and illness symptoms, and may reduce the risk of some complications (including pneumonia and respiratory failure). They recommend the use of oseltamivir in people with a higher risk of developing complications including children younger than 2 years, people over 65 years, people with some chronic conditions or immunosuppression, pregnant women, residents of long term care facilities, and indigenous communities for example.

The benefits of oseltamivir use are controversial; a 2014 Cochrane Review of the evidence found that oseltamivir treatment had limited benefit. The authors concluded that oseltamivir use in healthy adults had small, non-specific effects on symptoms (where the time to first alleviation of symptoms was only reduced from 7 to 6.3 days), it had no effect on hospitalizations, and that there was no evidence for any reductions in complications of influenza such as pneumonia. Due to the risk of adverse effects such as nausea, vomiting, psychiatric effects and renal adverse events in adults and vomiting in children, the harms are generally considered to outweigh the small clinical benefit of use of oseltamivir.

Notably, in 2017, the World Health Organization downgraded oseltamivir from its essential medicines list from a "core" drug to a "complementary" drug, due to limited cost-effectiveness. Yearly vaccination with the influenza vaccine is still considered the best preventative measure.

Indication

According to FDA prescribing information, oseltamivir is indicated for the treatment of acute, uncomplicated illness due to influenza A and B infection in patients 2 weeks of age and older who have been symptomatic for no more than 48 hours . In particular, this agent is indicated in adults and children including full-term neonates who present with symptoms typical of influenza when influenza virus is circulating in the community. Efficacy has been demonstrated when treatment is initiated within two days of the first onset of symptoms.

Oseltamivir is also indicated for the prophylaxis of influenza in patients one year and older . Specifically, post-exposure prevention in individuals one year of age or older following contact with a clinically diagnosed influenza case when influenza virus is circulating in the community qualifies for such prophylactic therapy. Oseltamivir would only be indicated for post-exposure prevention of influenza in infants less than 1 year of age during a pandemic influenza outbreak.

Associated Conditions
Flu caused by Influenza, Influenza A Virus Infection, Influenza A, Influenza B, Influenza Type B

Pharmacologic Study of Oseltamivir in Healthy Volunteers

Phase 1
Completed
Conditions
Avian Influenza A Virus
First Posted Date
2007-02-23
Last Posted Date
2009-07-28
Lead Sponsor
Mahidol University
Target Recruit Count
21
Registration Number
NCT00439530
Locations
🇹🇭

Bangkok Hospital for Tropical Diseases Research Unit, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand

A Study of Tamiflu (Oseltamivir) Treatment in Laboratory-Confirmed Influenza.

Phase 4
Terminated
Conditions
Influenza
First Posted Date
2007-02-16
Last Posted Date
2017-02-17
Lead Sponsor
Hoffmann-La Roche
Registration Number
NCT00436124

Safety and Pharmacokinetic Effects of Oseltamivir Alone or in Combination With Amantadine

Phase 1
Completed
Conditions
Healthy
First Posted Date
2006-12-28
Last Posted Date
2007-11-30
Lead Sponsor
Novartis
Target Recruit Count
18
Registration Number
NCT00416962
Locations
🇺🇸

Novartis Investigative Site, East Hanover, New Jersey, United States

A Study of Oseltamivir (Tamiflu) for the Seasonal Prophylaxis of Influenza in Immunocompromised Participants

Phase 4
Completed
Conditions
Influenza
Interventions
Drug: Placebo
First Posted Date
2006-12-18
Last Posted Date
2016-06-10
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
477
Registration Number
NCT00412737

A Study of Tamiflu (Oseltamivir) for Seasonal Prophylaxis of Influenza in Children.

Phase 4
Completed
Conditions
Influenza
Interventions
First Posted Date
2006-12-18
Last Posted Date
2020-08-18
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
52
Registration Number
NCT00412555

Oseltamivir Treatment for Children Less Than 24 Months of Age With Influenza

Phase 1
Completed
Conditions
Influenza
Interventions
First Posted Date
2006-10-24
Last Posted Date
2013-05-01
Lead Sponsor
National Institute of Allergy and Infectious Diseases (NIAID)
Target Recruit Count
87
Registration Number
NCT00391768
Locations
🇺🇸

Emory Children's Center - Pediatric Infectious Diseases, Atlanta, Georgia, United States

🇺🇸

The University of Texas Southwestern Medical Center, Dallas, Texas, United States

🇺🇸

MetroHealth Medical Center - Pediatric Infectious Disease, Cleveland, Ohio, United States

and more 29 locations

Alternative Oseltamivir Dosing Strategies

Phase 2
Completed
Conditions
Influenza
First Posted Date
2006-06-08
Last Posted Date
2017-07-02
Lead Sponsor
National Institute of Allergy and Infectious Diseases (NIAID)
Target Recruit Count
48
Registration Number
NCT00334529
Locations
🇺🇸

Brooke Army Medical Center, Houston, Texas, United States

🇺🇸

VA Greater Los Angeles Healthcare System, Los Angeles, California, United States

🇺🇸

National Institutes of Health Clinical Center, 9000 Rockville Pike, Bethesda, Maryland, United States

and more 1 locations

Evaluation of Alternative Oseltamivir (Tamiflu) Dosing Strategies.

Phase 4
Completed
Conditions
Influenza
Interventions
First Posted Date
2006-03-17
Last Posted Date
2009-09-23
Lead Sponsor
US Department of Veterans Affairs
Target Recruit Count
48
Registration Number
NCT00304434
Locations
🇺🇸

VA Palo Alto Health Care System, Palo Alto, California, United States

High-Dose Versus Standard-Dose Oseltamivir to Treat Severe Influenza and Avian Influenza

Phase 2
Completed
Conditions
Influenza
Avian Influenza
Severe Influenza
Interventions
First Posted Date
2006-03-01
Last Posted Date
2014-06-06
Lead Sponsor
National Institute of Allergy and Infectious Diseases (NIAID)
Target Recruit Count
326
Registration Number
NCT00298233
Locations
🇸🇬

Changi General Hospital, Singapore, Singapore

🇹🇭

Queen Sirikit National Institute of Child Health, Bangkok, Thailand

🇹🇭

Siriraj Hospital Mahidol University, Bangkok, Thailand

and more 9 locations
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