Clevudine

한글명:Clevudine

카스 번호163252-36-6

상품명:Clevudine

CBNumberCB0839271

분자식C10H13FN2O5

포뮬러 무게260.22

MOL 파일163252-36-6.mol

화학적 성질

녹는점	184-185°
알파	D25 -111.77° (c = 0.23 in methanol)
밀도	1.55±0.1 g/cm3(Predicted)
저장 조건	under inert gas (nitrogen or Argon) at 2-8°C
용해도	DMSO(약간 용해됨), 메탄올(약간 용해됨)
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	9.55±0.10(Predicted)
색상	하얀색
CAS 데이터베이스	163252-36-6

위험 및 안전 성명

독성	LD50 in mice, rats (mg/kg): >5000, >3000 orally (Painter)

그림문자(GHS)

Clevudine 화학적 특성, 용도, 생산

개요
Clevudine is a fluorinated b-L-nucleoside analog launched for the oral treatment of chronic HBV infection. It is the fifth nucleoside or nucleotide analog to be marketed for this indication. The previous drugs from this class include lamivudine, adefovir, entecavir, and telbivudine. In HBV-expressing human hepatoma cell line 2.2.15, clevudine inhibits HBV DNA synthesis with an EC₅₀ of 0.1 μM, and does not show cytotoxicity up to 200 μM. It is phosphorylated by cellular kinases to the active triphosphate derivative, which subsequently inhibits HBV DNA polymerase and HBV replication. 466 Shridhar Hegde and Michelle Schmidt Clevudine-5′-triphosphate has an intracellular half-life of 16.5 h. Interestingly, it is a non-competitive inhibitor of viral polymerase, and inhibits HBV replication without being incorporated into the DNA. The pharmacokinetic profile of clevudine was linear with a plasma half-life of approximately 60 h. Clevudine was undetectable in plasma after 4 weeks following the cessation of dosing.The most common adverse events reported with clevudine treatment include infection, asthenia, dyspepsia, abdominal pain, headache, and diarrhea.
Clevudine is chemically derived from L-ribose by first incorporating acyl protective groups to produce 1-O-acetyl-2,3,5-tri-O-benzoyl-b-L-ribofuranose intermediate, which is then converted to 1,3,5-tri-O-benzoyl-a-L-ribofuranose in two steps by treating To Market, To Market 2007 467 with hydrogen chloride and subsequent hydrolysis and acyl migration. The remaining steps leading to clevudine include conversion of the C2-hydroxy group to C2-fluoro group with triethylamine trihydrofluoride, formation of the corresponding ribofuranosyl bromide intermediate with hydrogen bromide and acetic acid, condensation with silylated thymine, and removal of benzoyl protective groups with methanolic ammonia.
화학적 성질
White Solid
용도
Antiviral drug, used for the treatment of Hepatitis B.

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