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用途
レジパスビル（Ledipasvir）はC型肝炎ウイルス)(HCV)のNS5A（英語版）阻害効果を持つ化合物である。レジパスビルとソホスブビルを組み合わせて投与すると、HCV複製の直接的阻害効果を示し、インターフェロンまたはリバビリンを併用することなく、ジェノタイプ1aまたは1bのC型肝炎を治療することができる。
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効能
抗ウイルス薬, NS5A阻害薬
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説明
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.
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使用
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.
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定義
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.
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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.
