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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
Associated Therapies
-

Study to Assess the Safety, Pharmacokinetics, and Efficacy of Baloxavir Marboxil in Healthy Pediatric Participants With Influenza-Like Symptoms

Phase 3
Completed
Conditions
Influenza
Interventions
First Posted Date
2018-08-14
Last Posted Date
2020-04-29
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
173
Registration Number
NCT03629184
Locations
🇺🇸

The Probe Medical Research, Los Angeles, California, United States

🇺🇸

Kentucky Pediatric Research Center, Bardstown, Kentucky, United States

🇺🇸

Orange County Research Institute, Ontario, California, United States

and more 34 locations

Proof-of-Concept: A Pilot, Randomized, Double-Blind Study of Oseltamivir Versus Placebo for Immune Thrombocytopenia

Phase 3
Conditions
Immune Thrombocytopenia
Interventions
Drug: Placebo
Drug: Oseltamivir
First Posted Date
2018-05-09
Last Posted Date
2020-10-22
Lead Sponsor
Unity Health Toronto
Target Recruit Count
30
Registration Number
NCT03520049
Locations
🇨🇦

St. Michael's Hospital, Toronto, Ontario, Canada

Efficiency of Antagonist Drugs of the Cellular Transcriptomic Signature of Influenza A Virus Infection.

Phase 2
Terminated
Conditions
Flu
Interventions
First Posted Date
2017-07-11
Last Posted Date
2023-02-06
Lead Sponsor
University Hospital, Lille
Target Recruit Count
85
Registration Number
NCT03212716
Locations
🇫🇷

Chu Amiens Picardie, Amiens, France

🇫🇷

CH ARRAS, Arras, France

🇫🇷

Ch Pierre Oudot Bourgoin Jallieu, Bourgoin-Jallieu, France

and more 16 locations

Dose Ranging Study to Evaluate the Efficacy and Safety of MEDI8852 in Adults Who Are Hospitalized With Type A Influenza.

Phase 2
Withdrawn
Conditions
Influenza - Type A Strains
Interventions
Drug: Oseltamivir
Drug: MEDI8852
Drug: Placebo
First Posted Date
2017-01-23
Last Posted Date
2019-03-14
Lead Sponsor
MedImmune LLC
Registration Number
NCT03028909

A Study to Assess the Relative Oral Bioavailability of a Single Dose of JNJ-63623872/Oseltamivir Fixed-dose Combination Tablet and Single Agent Concept Formulations of JNJ-63623872 Compared to Their Respective Reference Formulation in Healthy Adult Participants

Phase 1
Completed
Conditions
Healthy
Interventions
First Posted Date
2017-01-18
Last Posted Date
2017-05-25
Lead Sponsor
Janssen-Cilag International NV
Target Recruit Count
45
Registration Number
NCT03023852
Locations
🇧🇪

SGS Life Science Services, Antwerp, Belgium

A Study of S-033188 (Baloxavir Marboxil) Compared With Placebo or Oseltamivir in Otherwise Healthy Patients With Influenza

First Posted Date
2016-11-03
Last Posted Date
2019-05-08
Lead Sponsor
Shionogi
Target Recruit Count
1436
Registration Number
NCT02954354

A Drug-Drug Interaction Study to Evaluate the Effect of AL-794 on the Pharmacokinetics of Oseltamivir and JNJ-63623872

Phase 1
Completed
Conditions
Influenza in Humans
Interventions
First Posted Date
2016-09-05
Last Posted Date
2018-06-25
Lead Sponsor
Alios Biopharma Inc.
Target Recruit Count
68
Registration Number
NCT02888327
Locations
🇬🇧

Hammersmith Medicines Research, London, United Kingdom

A Pharmacokinetics, Pharmacodynamics and Safety Study of Warfarin in Combination With Tamiflu (Oseltamivir)

Phase 4
Completed
Conditions
Drug Therapy, Combination
Interventions
First Posted Date
2016-05-23
Last Posted Date
2016-10-26
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
20
Registration Number
NCT02780622

A Study to Investigate the Safety, Tolerability, and Pharmacokinetics (PK) of Oseltamivir and Its Carboxylate Metabolite, RO0640802 in Healthy Participants

Phase 1
Completed
Conditions
Healthy Volunteer
Interventions
Drug: Placebo
Drug: Oseltamivir
First Posted Date
2016-03-24
Last Posted Date
2016-06-27
Lead Sponsor
Hoffmann-La Roche
Target Recruit Count
99
Registration Number
NCT02717754
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