Tedizolid phosphate was approved by the US FDA in June 2014
for treatment of acute bacterial skin and skin structure infections
caused by susceptible gram-positive pathogens, including
MRSA. Tedizolid phosphate was discovered by Dong-A Pharmaceuticals
in South Korea and developed in the USA by Cubist
Pharmaceuticals (acquired from Trius Therapeutics in 2013,
became a wholly owned subsidiary of Merck in 2015). The
worldwide commercialization rights for tedizolid phosphate are
divided between Cubist in the USA, Canada, and EU, and Bayer in
Asia–Pacific, Latin America, and Africa. This second-generation
oxazolidinone prodrug is rapidly converted to the active form tedizolid
in the presence of endogenous phosphatases. It inhibits
bacterial protein synthesis by binding to the 23S ribosomal RNA
of the 50S subunit of the ribosome, preventing formation of the
70S ribosomal initiation complex, and is 4-fold to 16-fold more
potent against staphylococci and enterococci compared to linezolid.
251 With high oral bioavailability (approximately 90%) and
long half-life (approximately 12 hours), tedizolid phosphate is
the first oxazolidinone antibiotic which can be dosed once daily
either orally or intravenously.
Verwenden
Tedizolid, known as TR-700, is an oral and i.v administered intracellular antibacterial drug.
Definition
ChEBI: A phosphate monoester resulting from the formal condensation of equimolar amounts of phosphoric acid with the hydroxy group of tedizolid . It is a prodrug of tedizolid, used for the treatment of acute bacterial skin infections caused by certain susceptibl
bacteria, including Staphylococcus aureus (including methicillin-resistant strains (MRSA) and methicillin-susceptible strains), various Streptococcus species, and Enterococcus faecalis.
Nebenwirkungen
Tedizolid phosphate was well tolerated following the oral administration of a once-daily 200-mg dose for three days. No serious adverse events (AEs) were reported; the most commonly reported AEs were mild bradycardia (n = 2), headache (n = 1), and nausea (n = 1)[1].
Tedizolid Phosphate Upstream-Materialien And Downstream Produkte