Dasabuvir, sold under the brand name Exviera, is an

antiviral medication Antiviral drugs are a class of medication used for treating viral infections. Most antivirals target specific viruses, while a broad-spectrum antiviral is effective against a wide range of viruses. Unlike most antibiotics, antiviral drugs do ...

for the treatment of

hepatitis C Hepatitis C is an infectious disease caused by the hepatitis C virus (HCV) that primarily affects the liver; it is a type of viral hepatitis. During the initial infection people often have mild or no symptoms. Occasionally a fever, dark urine, a ...

. It is often used together with the combination medication

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 da ...

specifically for

hepatitis C virus The hepatitis C virus (HCV) is a small (55–65 nm in size), enveloped, positive-sense single-stranded RNA virus of the family ''Flaviviridae''. The hepatitis C virus is the cause of hepatitis C and some cancers such as liver cancer ( hepato ...

(HCV) type 1.

Ribavirin Ribavirin, also known as tribavirin, is an antiviral medication used to treat RSV infection, hepatitis C and some viral hemorrhagic fevers. For hepatitis C, it is used in combination with other medications such as simeprevir, sofosbuvir, pegin ...

may also additionally be used. These combinations result in a cure in more than 90% of people. It is taken

by mouth Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are i ...

. Common side effects include trouble sleeping, nausea, itchiness, and feeling tired. It is not recommended in those with liver failure but appears okay in people with

kidney disease Kidney disease, or renal disease, technically referred to as nephropathy, is damage to or disease of a kidney. Nephritis is an inflammatory kidney disease and has several types according to the location of the inflammation. Inflammation can ...

. While there is no evidence of harm if used during

pregnancy Pregnancy is the time during which one or more offspring develops ( gestates) inside a woman's uterus (womb). A multiple pregnancy involves more than one offspring, such as with twins. Pregnancy usually occurs by sexual intercourse, but ca ...

, it has not been well studied. It should not be used with

birth control pills Oral contraceptives, abbreviated OCPs, also known as birth control pills, are medications taken by mouth for the purpose of birth control. Female Two types of female oral contraceptive pill, taken once per day, are widely available: * The combin ...

that contain

ethinylestradiol Ethinylestradiol (EE) is an estrogen medication which is used widely in birth control pills in combination with progestins. In the past, EE was widely used for various indications such as the treatment of menopausal symptoms, gynecological disord ...

. Dasabuvir is in the HCV NS5B polymerase inhibitor class of medication. Dasabuvir was approved for medical use in 2014. It is on the

World Health Organization's List of Essential Medicines The WHO Model List of Essential Medicines (aka Essential Medicines List or EML), published by the World Health Organization (WHO), contains the medications considered to be most effective and safe to meet the most important needs in a health ...

. In the United States, it is approved by the

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respon ...

(FDA) only for use in combination with ombitasvir/paritaprevir/ritonavir. , the ability to get these medications in many areas of the world is poor.

Medical uses

Dasabuvir is used in the treatment of chronic Hepatitis C infection. It is used in the following HCV subtypes: genotype 1a, genotype 1b, genotype 1 of unknown subtype, and genotype 1 mixed infection without cirrhosis or with compensated cirrhosis. In the European Union, dasabuvir (Exviera) is always used in combination with another medicine,

(Viekirax) for the treatment of hepatitis C virus genotypes 1a and 1b. Some people taking dasabuvir are also treated with another antiviral medicine, ribavirin, in addition to ombitasvir/paritaprevir/ritonavir. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provided the source is acknowledged. In the United States, dasabuvir is co-packaged with ombitasvir/paritaprevir/ritonavir (Viekira Pak) and the combination is

indicated In medicine, an indication is a valid reason to use a certain test, medication, procedure, or surgery. There can be multiple indications to use a procedure or medication. An indication can commonly be confused with the term diagnosis. A diagnosis ...

for the treatment of adults with chronic hepatitis C virus genotype 1b without cirrhosis or with compensated cirrhosis. The co-packaged dasabuvir and ombitasvir/paritaprevir/ritonavir is used in combination with ribavirin for the treatment of adults with chronic hepatitis C virus genotype 1a without cirrhosis or with compensated cirrhosis.

Contraindications

People should not be taking dasabuvir if they meet any of the following criteria: * They have a hypersensitivity to it or any of the substances in the tablet. * They are taking any hormonal contraception that contain ethinylestradiol (often found in combined oral contraceptives or vaginal rings). * They are also taking medications that are strong or moderate enzyme inducers such as carbamazepine, phenytoin, phenobarbital, efavirenz, nevirapine, etravirine, mitotane, rifampicin, enzalutamide, and St. John's Wort (''Hypercium perforatum''). * They are also taking medications that are strong CYP2C8 inhibitors (gemfibrozil). * They meet contraindication criteria for ombitasivir, paritaprevir, and ritonavir since dasabuvir is used in combination with those three medications. In October 2015, the U.S.

(FDA) required the manufacturer to add a warning to the drug label that hepatitis C treatments Viekira Pak and Technivie can cause serious liver injury mostly in people with underlying advanced liver disease.

Adverse effects

The FDA approved combination of dasabuvir used with

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 p ...

paritaprevir Paritaprevir (previously known as ABT-450) is an acylsulfonamide inhibitor of the NS3- 4A serine protease manufactured by Abbott Laboratories that shows promising results as a treatment of hepatitis C. When given in combination with ritonavir ...

, and

ritonavir Ritonavir, sold under the brand name Norvir, is an antiretroviral drug used along with other medications to treat HIV/AIDS. This combination treatment is known as highly active antiretroviral therapy (HAART). Ritonavir is a protease inhibitor a ...

in the product

Viekira Pak 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 da ...

can cause a number of adverse effects. When Viekira Pak was used without

ribavirin Ribavirin, also known as tribavirin, is an antiviral medication used to treat RSV infection, hepatitis C and some viral hemorrhagic fevers. For hepatitis C, it is used in combination with other medications such as simeprevir, sofosbuvir, pegin ...

, nausea, severe itching, and insomnia occurred in more than 5% of the subjects. Less commonly, patients experienced increases in liver enzymes, such as AST and ALT, to greater than five times the upper limit of normal (occurred in 1% of patients). Usually this was asymptomatic. However, this is notable because females who are taking ethinylestradiol are at an increased risk for this side effect (25%). Dasabuvir could cause hepatitis B re-activation in people co-infected with hepatitis B and C viruses. The

European Medicines Agency The European Medicines Agency (EMA) is an agency of the European Union (EU) in charge of the evaluation and supervision of medicinal products. Prior to 2004, it was known as the European Agency for the Evaluation of Medicinal Products or Euro ...

recommended screening all people for hepatitis B before starting dasabuvir for hepatitis C in order to minimize the risk of hepatitis B reactivation.

Mechanism of action

Dasabuvir works by inhibiting the action of

NS5B 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 ...

palm

polymerase A polymerase is an enzyme ( EC 2.7.7.6/7/19/48/49) that synthesizes long chains of polymers or nucleic acids. DNA polymerase and RNA polymerase are used to assemble DNA and RNA molecules, respectively, by copying a DNA template strand using base- ...

, effectively terminating RNA polymerization and stopping the replication of the HCV's genome. By blocking NS5B polymerase, the virus can no longer multiply and infect new cells.

History

The U.S. FDA approved regimen of ombitasvir-paritaprevir-ritonavir and dasabuvir on December 19, 2014, to be used in the treatment of genotype 1 chronic hepatitis C infection in adults, which includes those with compensated cirrhosis.

Administration and storage

The two tablets of ombitasvir, paritaprevir, ritonavir will be taken in the morning and the one dasabuvir tablet taken twice a day in the morning and in the evening with a meal. The combination pack is packaged in a monthly package for 28 days of treatment.

References

External links

* {{Portal bar , Medicine , Viruses NS5B (polymerase) inhibitors Carbamates Naphthalenes Sulfonamides Pyrimidinediones World Health Organization essential medicines Wikipedia medicine articles ready to translate Tert-butyl compounds