테디졸리드인산염

한글명:테디졸리드인산염

카스 번호856867-55-5

상품명:Tedizolid Phosphate

CBNumberCB72676152

분자식C17H16FN6O6P

포뮬러 무게450.32

MOL 파일856867-55-5.mol

동의어(한글)

테디졸리드인산염

화학적 성질

녹는점	>235°C (dec.)
끓는 점	725.6±70.0 °C(Predicted)
밀도	1.75±0.1 g/cm3(Predicted)
저장 조건	under inert gas (nitrogen or Argon) at 2-8°C
용해도	DMSO(약간 초음파 처리)
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	1.81±0.10(Predicted)
색상	흰색에서 황백색까지
안정성	흡습성
InChIKey	QCGUSIANLFXSGE-GFCCVEGCSA-N
SMILES	O1[C@@H](COP(O)(O)=O)CN(C2=CC=C(C3=CC=C(C4=NN(C)N=N4)N=C3)C(F)=C2)C1=O

그림문자(GHS)

테디졸리드인산염 화학적 특성, 용도, 생산

개요
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.
용도
Tedizolid, known as TR-700, is an oral and i.v administered intracellular antibacterial drug.
정의
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.
부작용
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].

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