An Effective Anti-influenza Drug: Oseltamivir (Tamiflu)
Date of publication：2020/6/12 17:13:42
Influenza, commonly known as "flu", is an infectious disease caused by influenza virus. Symptoms can be mild to severe. The most common symptoms include: fever, runny nose, sore throat, muscle and joint pain, headache, cough and feeling tired.
Influenza remains an important cause of morbidity and mortality, and it will increase substantial economic costs due to hospitalization, especially for the elderly aged 65 or over and those with high-risk medical conditions. Although the influenza vaccination is considered to be the most effective control measure for healthy people and patients with chronic diseases, it is less effective for the elderly and immunocompromised patients.
Therefore, there is still a need for effective anti-influenza drugs, and neuraminidase inhibitors are the mainstay of anti-influenza therapy today. Oseltamivir is the most famous neuraminidase inhibitor, has become a drug of public health importance since it was included in the influenza pandemic management plan.
Oseltamivir (also known by the trade name Tamiflu), is the orally-active ethyl ester prodrug of oseltamivir carboxylate [(3R, 4R, 5S)-4-acetylamino-5-amino-3(1-ethylpropoxyl)-1-cyclohexene-1-carboxylic acid], that used to treat and prevent influenza A and influenza B. The conversion of oseltamivir to oseltamivir carboxylate occurs through a carboxylesterase which is located mainly in the liver.
The drug binds to the active site of the influenza virus neuraminidase to prevent the cleavage of N-acetylneuraminic acid (sialic acid) from the hemagglutinin receptor on epithelial cells.By leaving the receptor intact, viruses can accumulate, preventing them from entering the epithelial cells. Intact hemagglutinin receptors can also cause the aggregation of new virus particles on the cell surface.
Oral oseltamivir is rapidly absorbed and cleaved to active carboxylate by carboxyesterase in the liver and gastrointestinal tract. The bioavailability of carboxylate is estimated to be approximately 80%, and it takes 2.5 to 5 hours for the carboxylate to reach its maximum plasma concentration.
Oseltamivir shows dose linear kinetics with an elimination half-life of approximately 7.7 hours in healthy individuals. Oseltamivir carboxylate is cleared by the kidney primarily through glomerular filtration and tubular secretion, with an average half-life of 6-10 hours. Both clearance and tissue distribution are reduced by probenecid.
Many medical organizations recommend Oseltamivir for people who have symptoms of infection or who have a high risk of complications within 48 hours of the first symptoms of infection. It can be taken orally, either as a pill or liquid.
Huateng Pharma, a leading pharmaceutical intermediates manufacturers in China, is exclusively focusing on manufacturing anti-viral intermediates, such as Remdesivir intermediates, Favipiravir intermediates, Baloxavir Marboxil intermediates, Oseltamivir intermediates and so on. We are able to provide the production of these key intermediates with capacities varying from gram to kilograms with high purity to our customers all over the world.
Oseltamivir intermediates: CAS No. 204254-96-6, CAS. No 651324-08-2, CAS. No 651324-09-3