MedPath

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

A Pharmacokinetic/Pharmacodynamic (PK/PD) and Safety Evaluation of Oseltamivir [Tamiflu] in the Treatment of Infants 0 to <12 Months of Age With Confirmed Flu Infection

Phase 1
Completed
Conditions
Influenza
Interventions
First Posted Date
2009-10-02
Last Posted Date
2017-03-20
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
65
Registration Number
NCT00988325
Locations
🇩🇪

Onkologische Schwerpunktpraxis Dr. Med. O. Burkhard & B. Reimann, Worms, Germany

🇮🇹

Fondazione Ospedale Maggiore Policlinico, Milan, Lombardia, Italy

🇵🇱

Vitamed, Bydgoszcz, Poland

and more 9 locations

Long Term Influenza Prophylaxis With Inhaled Zanamivir or Oral Oseltamivir

Phase 4
Completed
Conditions
Influenza
Interventions
Drug: placebo capsule
Drug: placebo for inhalation
First Posted Date
2009-09-18
Last Posted Date
2010-09-22
Lead Sponsor
University of Oxford
Target Recruit Count
390
Registration Number
NCT00980109
Locations
🇹🇭

Hospital for Tropical Diseases, Bangkok, Thailand

🇹🇭

Faculty of Medicine Siriraj Hospital, Bangkok, Bangkoknoi, Thailand

A Clinical Trial Comparing Oseltamivir With Placebo And Zanamivir With Control As First Line Treatment For Human Swine Influenza Infection

Phase 3
Terminated
Conditions
Upper Respiratory Tract Infection
Influenza
Interventions
First Posted Date
2009-09-18
Last Posted Date
2011-04-11
Lead Sponsor
Chinese University of Hong Kong
Target Recruit Count
4
Registration Number
NCT00979667
Locations
🇭🇰

Sai Ying Pun Jockey Club General Outpatient Clinic, Hong Kong, Hong Kong

🇨🇳

Shau Kei Wan Jockey Club Clinic, Hong Kong, Hong Kong, China

🇭🇰

Fanling Family Medicine Centre, Hong Kong, Hong Kong

Oral Triple Combination Antiviral Drug Therapy for Treatment of Influenza A in Immunocompromised Subjects

Phase 2
Completed
Conditions
Influenza
Interventions
First Posted Date
2009-09-17
Last Posted Date
2014-04-14
Lead Sponsor
Adamas Pharmaceuticals, Inc.
Target Recruit Count
2
Registration Number
NCT00979251
Locations
🇸🇬

Adamas Investigational Site, Singapore, Singapore

🇦🇺

Adamas Investigative Site, Parkville, Victoria, Australia

A Study on Emergence of Resistance With Oseltamivir (Tamiflu) in Participants With Seasonal Influenza

Phase 3
Completed
Conditions
Influenza
Interventions
First Posted Date
2009-07-30
Last Posted Date
2016-08-08
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
37
Registration Number
NCT00949533

Chinese Medicinal Herbs Treatment on Novel Influenza A (H1N1)Pneumonia: Multi-centre, Prospective, Randomized Controlled Study

First Posted Date
2009-07-09
Last Posted Date
2009-11-01
Lead Sponsor
Capital Medical University
Target Recruit Count
400
Registration Number
NCT00936013
Locations
🇨🇳

Capital Medical University affiliated Bejing Chaoyang Hospital, Beijing Respiratory Medicine Institute, Beijing, China

Chinese Medicinal Herbs Treatment on Novel Influenza A (H1N1) : Multi-centre, Prospective, Randomized Controlled Study

Phase 4
Completed
Conditions
Influenza
Interventions
First Posted Date
2009-07-08
Last Posted Date
2009-12-01
Lead Sponsor
Capital Medical University
Target Recruit Count
102
Registration Number
NCT00935194
Locations
🇨🇳

Capital Medical University affiliated Beijing Chaoyang Hospital, Beijing Respiratory Medicine Insititute, Beijing, China

Pharmacokinetic Study of Oseltamivir and Intravenous Zanamivir in Healthy Adults

Phase 1
Completed
Conditions
Influenza
Virus Diseases
Interventions
First Posted Date
2009-06-16
Last Posted Date
2010-03-19
Lead Sponsor
National Institute of Allergy and Infectious Diseases (NIAID)
Target Recruit Count
17
Registration Number
NCT00921726
Locations
🇹🇭

Mathidol University, Salaya, Thailand

Influenza Resistance Information Study

Completed
Conditions
Influenza
Interventions
First Posted Date
2009-04-20
Last Posted Date
2016-10-19
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
4561
Registration Number
NCT00884117

A Study of the Pharmacology of Oseltamivir (Tamiflu) in Pregnancy

Phase 1
Withdrawn
Conditions
Influenza
Pregnancy
Interventions
Procedure: Blood Draws
First Posted Date
2009-04-02
Last Posted Date
2015-09-29
Lead Sponsor
University of Pittsburgh
Registration Number
NCT00873886
Locations
🇺🇸

Magee-Womens Hospital of University of Pittsburgh Medical Center, Pittsburgh, Pennsylvania, United States

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