Ledipasvir

한글명:Ledipasvir

카스 번호1256388-51-8

상품명:Ledipasvir

CBNumberCB52666650

분자식C49H54F2N8O6

포뮬러 무게889

MOL 파일1256388-51-8.mol

화학적 성질

녹는점	186-190oC
밀도	1.42±0.1 g/cm3(Predicted)
저장 조건	-20°C Freezer
용해도	DMSO(약간 용해됨, 가열), 메탄올(약간 용해됨)
산도 계수 (pKa)	11.20±0.10(Predicted)
물리적 상태	고체
물리적 상태	단단한 모양
색상	흰색에서 옅은 베이지까지

위험 및 안전 성명

안전지침서	24/25
유엔번호(UN No.)	3077
HS 번호	29333990

그림문자(GHS)

Ledipasvir 화학적 특성, 용도, 생산

개요
Ledipasvir is a potent NS5A inhibitor that is approved for use in combination with sofosbuvir, a nucleotide inhibitor of viral polymerase, for the treatment of chronic hepatitis C virus genotype 1 infection. This combination was discovered and developed at Gilead Sciences and is marketed as the fixed combination with brand name of Harvoni.
용도
Ledipasvir is most commonly used in combination with sofosbuvir for treatment in chronic hepatitis C genotype 1 patients. It inhibits an important viral phosphoprotein, NS5A, which is involved in viral replication, assembly, and secretion.
정의
ChEBI: Ledipasvir is a benzimidazole derivative that is used in combination with sofosbuvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection. It has a role as an antiviral drug and a hepatitis C protease inhibitor. It is a carbamate ester, a L-valine derivative, a bridged compound, a carboxamide, a benzimidazole, a member of fluorenes, an organofluorine compound, a member of imidazoles, a N-acylpyrrolidine and an azaspiro compound.
Mode of action
Ledipasvir is a potent inhibitor of HCV nonstructural protein 5A (NS5A), a viral phosphoprotein that plays an important but poorly understood role in viral replication, assembly, and secretion. ;Ledipasvir is approved for the treatment of genotype 1 HCV. Its safety and efficacy have not been fully established for genotypes 2 through 6. NS5A amino acid substitutions Y93H (in genotypes 1a and 1b) and Q30E (in genotype 1a) significantly reduce susceptibility to ledipasvir in cell culture and in clinical studies. Other amino acid substitutions observed in virologic treatment failures are K24R, M28T/V, Q30H/K/L (genotype 1a), and L31V/M/I (genotype 1b). Viruses with these resistance-associated mutations remained susceptible to sofosbuvir.

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