Zepatier: Difference between revisions
From Proteopedia
Jump to navigationJump to search
No edit summary |
No edit summary |
||
| Line 4: | Line 4: | ||
== Function == | == Function == | ||
Zepatier is a combination drug combating genotypes 1 and 4 of chronic hepatitis C viral (HCV) infections in adults. <scene name='74/746120/Elbasvir_structure3/1'>Elbasvir</scene> inhibits NS5A, a non-enzymatic protein essential for viral replication and assembly of hepatitis C whose exact mechanism of action is unknown. Elbasvir restricts viral production at the early stage of assembly, in turn preventing spread of the virus<ref name="elbasvir">DOI: 10.1002/cmdc.201300343</ref>. | Zepatier is a combination drug combating genotypes 1 and 4 of chronic hepatitis C viral (HCV) infections in adults. It is designed for the treatment of individuals with end stage renal disease on dialysis, typically genotype 1 infected patients. The drug is also utilized to treat genotype 4 patients when other methods of treatment prove ineffective <ref>Petrescu, I. O.; Biciusca, V.; Taisescu, C. I.; Alexandru, D. O.; Taisescu, O.; Comanescu, M. V.; Petrescu, F.; Popescu, I. A.; Trasca, D. M.; ForTofoiu, M. C.; Silosi, C. A.; ForTofoiu, M. Histological factors that predict the liver fibrosis in patients with chronic hepatitis C. Rom. J. Morphol. Embryol. 2016, 57, 759-765.</ref>.<scene name='74/746120/Elbasvir_structure3/1'>Elbasvir</scene> inhibits NS5A, a non-enzymatic protein essential for viral replication and assembly of hepatitis C whose exact mechanism of action is unknown. Elbasvir restricts viral production at the early stage of assembly, in turn preventing spread of the virus<ref name="elbasvir">DOI: 10.1002/cmdc.201300343</ref>. | ||
Grazoprevir is a macrocyclic compound that is able to reversibly bind to the protease, NS3/4A, essential for viral replication. It is responsible for cleavage and processing of the HCV polyprotein. It is hypothesized that the protease is utilized to circumvent immune response at the primary stages of infection <ref>DOI: 10.1021/acschembio.5b00647</ref>. | Grazoprevir is a macrocyclic compound that is able to reversibly bind to the protease, NS3/4A, essential for viral replication. It is responsible for cleavage and processing of the HCV polyprotein. It is hypothesized that the protease is utilized to circumvent immune response at the primary stages of infection <ref>DOI: 10.1021/acschembio.5b00647</ref>. | ||
| Line 14: | Line 14: | ||
While six distinct genotype of HCV were discovered, genotypes 1 is the most prevalent amongst populations and the most difficult to treat. Increased resistance of the virus at the M28, Q30, L31, or Y93 amino acids results in decreased effectiveness of pharmaceuticals against genotype 1. Genotype 1 results from the infection of human lymphoid cells by the virus. Genotype 4 has recently increased in prevalence, resulting in attempts to decrease transmission. | While six distinct genotype of HCV were discovered, genotypes 1 is the most prevalent amongst populations and the most difficult to treat. Increased resistance of the virus at the M28, Q30, L31, or Y93 amino acids results in decreased effectiveness of pharmaceuticals against genotype 1. Genotype 1 results from the infection of human lymphoid cells by the virus. Genotype 4 has recently increased in prevalence, resulting in attempts to decrease transmission. | ||
== Structure and Mechanism of Elbasvir == | == Structure and Mechanism of Elbasvir == | ||