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NS5A Inhibitors
Nonstructural protein 5A (NS5A) is a Zinc-binding protein, zinc-binding and proline-rich Hydrophile, hydrophilic phosphoprotein that plays a key role in Hepatitis C virus RNA replication. It appears to be a dimeric form without ''trans''-membrane helices. Structure NS5A is derived from a large polyprotein that is translated from the HCV genome, and undergoes post-translation processing by NS3 (HCV), nonstructural protein 3 (NS3) viral protease. Despite no inherent enzymatic activity being attributed to NS5A, its function is mediated through interaction with other nonstructural (NS) viral and cellular proteins. NS5A has two phosphorylated forms: p56 and p58, which differ in the electrophoretic mobility. p56 is basally phosphorylated by host cellular protein kinase at the center and near the C terminus, whereas p58 is a form of hyper-phosphorylated NS5A at the center of the serine-rich region. Protein mass spectrometry identified several phosphorylated serine residues in this region ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
HCV Genome
HCV may refer to: Government * Housing choice voucher, US federal rent assistance * Housing Commission of Victoria, Australia (1938–1984) Science * Hepatitis C virus, a human pathogen * Higher calorific value, see Heat of combustion#Higher heating value, Heat of combustion * High conservation value area, in ecology and forestry * Housing choice voucher * Housing Commission of Victoria, in Australia Other uses * Halcyonair, a Cape Verdean airline (2005–2013; ICAO:HCV) {{disambiguation ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NS5B (Hepacivirus)
Nonstructural protein 5B (NS5B) is a viral protein found in the hepatitis C virus (HCV). It is an RNA-dependent RNA polymerase, having the key function of replicating HCV's viral RNA by using the viral positive RNA strand as a template to catalyze the polymerization of ribonucleoside triphosphates (rNTP) during RNA replication. Several crystal structures of NS5B polymerase in several crystalline forms have been determined based on the same consensus sequence BK (HCV-BK, genotype 1). The structure can be represented by a right hand shape with fingers, palm, and thumb. The encircled active site, unique to NS5B, is contained within the palm structure of the protein. Recent studies on NS5B protein genotype 1b strain J4's (HC-J4) structure indicate a presence of an active site where possible control of nucleotide binding occurs and initiation of de-novo RNA synthesis. De-novo adds necessary primers for initiation of RNA replication. Drugs targeting NS5B Several drugs are either on the m ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glecaprevir/pibrentasvir
Glecaprevir/pibrentasvir (G/P), sold under the brand names Mavyret and Maviret, is a fixed-dose combination medication used to treat hepatitis C. It contains glecaprevir and pibrentasvir. It works against all six types of hepatitis C. At twelve weeks following treatment between 81% and 100% of people have no evidence of hepatitis C. It is taken once a day by mouth with food. The most common side effects are headache, diarrhea, and tiredness. In those with a history of hepatitis B, reactivation may occur. It is not recommended in people with moderate to severe liver disease. Glecaprevir works by blocking the protein NS3/ 4A protease, while pibrentasvir works by blocking NS5A. The combination was approved for medical use in the United States and Europe in 2017. It is on the World Health Organization's List of Essential Medicines. Medical uses In the United States, G/P is used to treat adults and children aged 12 years and older or weighing at least 99 pounds with chronic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pibrentasvir
Pibrentasvir is an NS5A inhibitor antiviral agent. In the United States and Europe, it is approved for use with glecaprevir as the combination drug glecaprevir/pibrentasvir (trade name ''Mavyret'' in the US and ''Maviret'' in the EU) for the treatment of hepatitis C. It is sold by Abbvie AbbVie Inc. is an American pharmaceutical company headquartered in North Chicago, Illinois. It is ranked sixth on the list of largest biomedical companies by revenue. In 2023, the company's seat in Forbes Global 2000 was 74, and rank 89 on the .... References {{Antiinfective-drug-stub NS5A inhibitors Fluoroarenes Benzimidazoles Drugs developed by AbbVie Carbamates 4-Fluorophenyl compounds ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sofosbuvir/velpatasvir/voxilaprevir
Sofosbuvir/velpatasvir/voxilaprevir, sold under the brand name Vosevi, is a fixed-dose combination medication for the treatment of hepatitisC. It contains sofosbuvir, a hepatitis C virus (HCV) nucleotide analog NS5B polymerase inhibitor; velpatasvir, an HCV NS5A inhibitor; and voxilaprevir an HCV NS3/4A protease inhibitor. The most common adverse reactions include headache, fatigue, diarrhea, and nausea. The combination was approved for medical use in the United States and in the European Union in July 2017. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged. Vosevi is sold by Gilead Sciences. Medical uses In the US, sofosbuvir/velpatasvir/voxilaprevir is indicated for the treatment of adults with chronic hepatitis C virus infection without cirrhosis (liver disease) or with compensated cirrhosis (Child-Pugh A). In the EU, it is indicated for the treatment of chronic hepatitis C vir ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sofosbuvir/velpatasvir
Sofosbuvir/velpatasvir, sold under the brand name Epclusa among others, is a fixed-dose combination medication for the treatment of hepatitis C in adults. It combines sofosbuvir and velpatasvir. It is more than 90% effective for hepatitis C genotypes one through six. It also works for hepatitis C in those who also have cirrhosis or HIV/AIDS. It is taken by mouth. In March 2020, sofosbuvir/velpatasvir was approved for use in the United States to treat hepatitis C virus (HCV) in children ages six years and older or weighing at least 37 pounds (17 kilograms) with any of the six HCV genotypes—or strains—without cirrhosis (liver disease) or with mild cirrhosis. Sofosbuvir/velpatasvir in combination with ribavirin is indicated for the treatment of children six years and older or weighing at least 37 pounds with severe cirrhosis. The combination is generally well tolerated. Common side effects include headaches, fatigue, trouble sleeping, and nausea. The combination has not been ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Velpatasvir
Velpatasvir is an NS5A inhibitor (by Gilead) which is used together with sofosbuvir in the treatment of hepatitis C infection of all six major genotypes. Side effects Side effects in studies occurred with similar frequencies as in people treated with placebo. Interactions Velpatasvir is both an inhibitor and a substrate of the transporter proteins P-glycoprotein (Pgp), ABCG2, OATP1B1 and OATP1B3. It is partly degraded by the liver enzymes CYP2B6, CYP2C8 and CYP3A4. Substances that are transported or inactivated by these proteins, or interfere with them, can interact with velpatasvir. In studies, this has been found for the HIV combination efavirenz/emtricitabine/tenofovir, which reduces the area under the curve (AUC) of velpatasvir by about 50%, and the CYP3A4 and Pgp inducer rifampicin, which reduces its AUC by about 80%, rendering it likely ineffective. Digoxin is eliminated by Pgp; its AUC is increased by about 30% in combination with velpatasvir and sofosbuvir (althou ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Elbasvir/grazoprevir
Elbasvir/grazoprevir, sold under the brand name Zepatier, is a fixed-dose combination for the treatment of hepatitis C, containing elbasvir (an inhibitor of hepatitis C virus's NS5A protein) and grazoprevir (an NS3/ 4A inhibitor). It is used to treat chronic hepatitis C virus (HCV) genotypes 1 or 4 infection in both treatment-naïve and treatment-experienced patients. Both elbasvir and grazoprevir were developed by Merck & Co. The US Food and Drug Administration (FDA) approved the drug in January 2016. Medical uses Elbasvir/grazoprevir received FDA approval in January 2016. Its indication is for treatment of chronic hepatitis C of the genotypes 1 and 4 for adults. Hepatitis C is a global disease that infects upwards of 150 million people worldwide, especially in older generations. Hepatitis C causes inflammation of the liver that eventually leads to diminished liver function or even failure. Zepatier is indicated for treatment with or without use of ribavirin, as well. Zepatier ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Elbasvir
Elbasvir is a drug approved by the FDA in January 2016 for the treatment of hepatitis C. It was developed by Merck and completed Phase III trials, used in combination with the NS3/ 4A protease inhibitor grazoprevir under the trade name '' Zepatier'', either with or without ribavirin. Elbasvir is a highly potent and selective NS5A inhibitor of the hepatitis C virus NS5A replication complex. It has only been investigated as a combination product with other complementary hepatitis C antiviral drugs such as grazoprevir and MK-3682, and it is unclear whether elbasvir would show robust antiviral activity if it was administered by itself. Nevertheless, combination products of this type represent the most successful approach yet developed for actually curing hepatitis C, rather than merely slowing the progression of the disease. Side effects Side effects have only been assessed in the combination with grazoprevir; see Elbasvir/grazoprevir#Side effects. Interactions Elbasvir i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Daclatasvir
Daclatasvir, sold under the brand name Daklinza, is an antiviral medication used in combination with other medications to treat hepatitis C (HCV). The other medications used in combination include sofosbuvir, ribavirin, and Interferon#Drug formulations, interferon, vary depending on the virus type and whether the person has cirrhosis. It is taken by mouth. Common side effects when used with sofusbivir and daclatasvir include headache, fatigue (medicine), feeling tired, and nausea. With daclatasvir, sofosbuvir, and ribavirin the most common side effects are headache, feeling tired, nausea, and hemolytic anemia, red blood cell breakdown. It should not be used with St. John's wort, rifampin, or carbamazepine. It works by inhibiting the HCV protein NS5A. Daclatasvir was approved for use in the European Union in 2014, and the United States and India in 2015. It is on the WHO Model List of Essential Medicines, World Health Organization's List of Essential Medicines. The brand Dakli ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ombitasvir/paritaprevir/ritonavir
Ombitasvir/paritaprevir/ritonavir, sold under the brand name Technivie among others, is a medication used to treat hepatitis C. It is a fixed-dose combination of ombitasvir, paritaprevir, and ritonavir. Specifically it is used together with dasabuvir or ribavirin for cases caused by hepatitis C virus genotype 1 or 4. Cure rates are around 95%. It is taken by mouth. It is generally well tolerated. Common side effects include nausea, itchiness, rash, and trouble sleeping. Other side effects include allergic reactions and reactivation of hepatitis B among those previously infected. Use is not recommended in those with significant liver problems. While there is no evidence of harm with use during pregnancy, this use has not been well studied. Each of the medications works by a different mechanism. The ritonavir is present to decrease the breakdown of paritaprevir. Ombitasvir/paritaprevir/ritonavir with dasabuvir was approved for medical use in the United States in Decembe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ombitasvir
Ombitasvir is an antiviral drug for the treatment of hepatitis C virus (HCV) infection by AbbVie. In the United States, it is approved by the Food and Drug Administration for use in combination with paritaprevir, ritonavir and dasabuvir in the product Viekira Pak for the treatment of HCV genotype 1, and with paritaprevir and ritonavir Ritonavir, sold under the brand name Norvir, is an antiretroviral medication used along with other medications to treat HIV/AIDS. This combination treatment is known as highly active antiretroviral therapy (HAART). Ritonavir is a protease inhi ... in the product Technivie for the treatment of HCV genotype 4. Ombitasvir is an NS5A inhibitor that acts by inhibiting the HCV protein NS5A. See also * Discovery and development of NS5A inhibitors References Further reading * * Carbamates NS5A inhibitors Pyrrolidines {{Antiinfective-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
