Lamivudine
The lamivudine (2 ', 3 ' - didéoxy-3'-thia Cytidine, 3TC ) is a powerful inhibiter of the Transcriptase reverses marketed under the name of Epivir . It can inhibit the two types (1 and 2) of transcriptase opposite of HIV like that of the virus of the Hépatite B. So that it becomes active, it is necessary that it is phosphorylée in its form triphosphate. The triphosphate of 3TC inhibits thus cellular DNA polymerase.
The lamivudine is managed by oral way, and it is quickly absorbed with an bio-availability higher than 80%. Zidovudine, with which it is highly synergistic. Lamivudine treatment has been shown to restore zidovudine sensitivity off previously resistant HIV. Several mutagenicity tests show that lamivudine should not show Mutagen ic activity in therapeutical amounts. -->
History
Bernard Belleau and Nghe Nguyen-Ga At the Quebec-based BioChem Pharma in 1989. The drug was later licensed to the British pharmaceutical company Glaxo for has 14 bore royalty. --> The lamivudine was discovered by screening in 1989 by Bernard BELLEAU and Nghe NGUYEN-GA.The team works of the doctor-researcher Lorne Tyrrell of the University of Alberta, Canada, showed that Lamivudine was an effective cure against the Hépatite B.
The synthesis of novo is carried out in completely anhydrous medium, because of the sensitivity of sulfur acetal formed to the aqueous acids. This one can be summarized by the following diagram:
References
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