Aoà o Sā taā wei wéi (oseltamivir) is a specific inhibitor of neuraminidase, which can inhibit the mature influenza virus from leaving the host cell, thus inhibiting the spread of influenza virus in human body to treat influenza.
Oseltamivir is a successful case of rational drug design based on structure. Computer-aided drug design has been widely used in the research and development of this drug. According to the three-dimensional structure of the target enzyme, a neuraminidase inhibitor with high efficiency, low toxicity and strong specificity was designed.
The earliest appearance of oseltamivir was zanamivir developed by GlaxoSmithKline. Because the physical and chemical properties of zanamivir are not conducive to biological absorption, the bioavailability of zanamivir is low, the route of administration is single, and the patient's compliance is poor.
On the basis of zanamivir, oseltamivir is obtained through reasonable drug design according to the molecular structure of natural substrate of neuraminidase and the spatial structure of catalytic center of neuraminidase. It is another drug successfully obtained through reasonable drug design after HIV integrase inhibitor.
The oseltamivir was first synthesized in 1996 and patented in the United States on February 26th, 1998. It was first launched in Sweden in June, 1999, then entered the Canadian, European Union and American markets, and was approved to be listed in China in 2002.
From June 5438 to February 2005, the research results of Oxford University showed that avian influenza virus began to develop resistance to Tamiflu. 65438+On February 22nd, Roche Pharmaceuticals strongly requested to increase the dosage of Tamiflu to fight against avian influenza.
Roche Pharmaceutical Co., Ltd. is the patent holder of oseltamivir, and its oseltamivir phosphate capsules (Tamiflu in Chinese mainland, Tamiflu in Hongkong and Influenza in Taiwan Province Province) are the only oseltamivir preparations on the market at present.
From June 5438 to October 2005 10, due to the global spread of avian influenza, there was a global rush to buy Tamiflu, and Roche was widely condemned for refusing to open the patent right of oseltamivir and restricting the sale of Tamiflu.