Clevudine

J05AF12

Antiviral

184-185 ° C

Template: Infobox chemical / molecular formula search available

Clevudin, L- FMAU (short for 1 - (2 -fluoro -5-methyl - β, L- arabinofuranosyl ) uracil ) is a chemical analogue of the nucleoside thymidine, or its mirror image construction enantiomer telbivudine, since, as this which reverse stereo configuration of thymidine has. It is an antiviral selected from the group of nucleoside reverse transcriptase inhibitors ( NRTI) and is to be used as a drug for treatment of Hepatitis B.

Attempted introduction as drug

The drug was approved in 2006 as Levovir ® in South Korea for use against hepatitis B by the manufacturer Bukwang of the authorities there.

Since late 2009, has been reported on the incidence of myopathy (muscle weakness ) in patients treated for 6-8 months with Clevudin. The Phase III QUASH trials for the treatment of hepatitis B in the United States was then adjusted by Pharmasset Inc.. The majority of cases should have occurred only after one year of treatment. The side effect to occur, because Clevudin is installed not only in viral, but also in mitochondrial DNA.

Pharmacology

The nucleoside Clevudin is phosphorylated in the cell to the nucleotide. In competition with the natural nucleotide deoxythymidine triphosphate ( dTTP ) is Clevudin -triphosphate into the DNA of viruses installed. The incorporation of the fluorine - nucleoside triphosphate to chain termination and leads to the inhibition of the viral reverse transcriptase.