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The current production method is based on the first scalable synthesis developed by Gilead Sciences [4] starting from naturally occurring quinic acid or shikimic acid.Due to lower yields and the extra steps required (because of the additional dehydration), the quinic acid route was dropped in favour of the one based on shikimic acid, which received further improvements by Hoffmann-La Roche.
It was originally synthesised from shikimic acid extracted from the star anise plant. Oseltamivir is a prodrug that requires metabolism in the liver to the active form, oseltamivir carboxylate. This binds at the active site of the neuraminidase enzyme, preventing it from cleaving sialic acid to release the virus particle from the host cell ...
Oseltamivir, sold under the brand name Tamiflu among others, is an antiviral medication used to treat and prevent influenza A and influenza B, viruses that cause the flu. [5] Many medical organizations recommend it in people who have complications or are at high risk of complications within 48 hours of first symptoms of infection. [ 6 ]
Shikimic acid can also be extracted from the seeds of the sweetgum (Liquidambar styraciflua) fruit, [2] which is abundant in North America, in yields of around 1.5%. For example, 4 kg (8.8 lb) of sweetgum seeds is needed for fourteen packages of Tamiflu. By comparison, star anise has been reported to yield 3% to 7% shikimic acid.
Viferon is a suppository of (non-pegylated [12]) interferon alpha-2b, ascorbic acid (vitamin C), and tocopherol (vitamin E) which was reported in two small studies to be as effective as arbidol. [ 13 ] [ 14 ] Another interferon alfa-2b medicine, "Grippferon", nasal drops, is used for treatment and emergency prevention of Influenza and cold. [ 15 ]
Aminoshikimic acid is an unnatural carbohydrate, although aminoshikimic acid is the namesake of the aminoshikimate pathway, which generates the 3-amino-5-hydroxybenzoic acid (AHBA) starter unit required for the biosynthesis of the ansamycins and mitomycins. [1]
For many biologics (e.g., monoclonal antibodies), injection site reactions are the most common adverse effect of the drug, and have been reported to have an incidence rate of 0.5–40%. [ 2 ] In trials of subcutaneous administration of oligonucleotides , between 22 and 100% of subjects developed reactions depending on the oligonucleotide.
EPSP synthase is a monomeric enzyme with a molecular mass of approximately 46,000. [2] [3] [4] It consists of two domains connected by protein strands that function as a hinge, allowing the two domains to move closer together.