Dasabuvir
Chemical compound
From Wikipedia, the free encyclopedia
Dasabuvir, sold under the brand name Exviera, is an antiviral medication for the treatment of hepatitis C.[3] It is often used together with the combination medication ombitasvir/paritaprevir/ritonavir specifically for hepatitis C virus (HCV) type 1.[3] Ribavirin may also additionally be used.[1][2] These combinations result in a cure in more than 90% of people.[4] It is taken by mouth.[3]
Dasabuvir UK Drug Information
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| Clinical data | |
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| Trade names | Exviera, Viekira Pak, Viekira XR |
| Other names | ABT-333 |
| AHFS/Drugs.com | Viekira Pak Monograph Dasabuvir UK Drug Information |
| MedlinePlus | a616040 |
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| Routes of administration | By mouth |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.232.246 |
| Chemical and physical data | |
| Formula | C26H27N3O5S |
| Molar mass | 493.58 g·mol−1 |
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Common side effects include trouble sleeping, nausea, itchiness, and feeling tired.[4] It is not recommended in those with liver failure but appears okay in people with kidney disease.[3] While there is no evidence of harm if used during pregnancy, it has not been well studied.[3] It should not be used with birth control pills that contain ethinylestradiol.[4] Dasabuvir is in the HCV NS5B polymerase inhibitor class of medication.[3]
Dasabuvir was approved for medical use in 2014.[5] It is on the World Health Organization's List of Essential Medicines.[6] In the United States, it is approved by the Food and Drug Administration (FDA) only for use in combination with ombitasvir/paritaprevir/ritonavir.[3] As of 2015[update], the ability to get these medications in many areas of the world is poor.[7]
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.[8]
In the European Union, dasabuvir (Exviera) is always used in combination with another medicine, ombitasvir/paritaprevir/ritonavir (Viekirax) for the treatment of hepatitis C virus genotypes 1a and 1b.[2] Some people taking dasabuvir are also treated with another antiviral medicine, ribavirin, in addition to ombitasvir/paritaprevir/ritonavir.[2]
In the United States, dasabuvir is co-packaged with ombitasvir/paritaprevir/ritonavir (Viekira Pak) and the combination is indicated for the treatment of adults with chronic hepatitis C virus genotype 1b without cirrhosis or with compensated cirrhosis.[1] 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.[1]
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.[4]
- They are taking any hormonal contraception that contain ethinylestradiol (often found in combined oral contraceptives or vaginal rings).[4]
- 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).[4]
- They are also taking medications that are strong CYP2C8 inhibitors (gemfibrozil).[4]
- They meet contraindication criteria for ombitasvir, paritaprevir, and ritonavir since dasabuvir is used in combination with those three medications.[4]
In October 2015, the U.S. Food and Drug Administration (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.[9]
Adverse effects
The FDA approved combination of dasabuvir used with ombitasvir, paritaprevir, and ritonavir in the product Viekira Pak can cause a number of adverse effects. When Viekira Pak was used without ribavirin, nausea, severe itching, and insomnia occurred in more than 5% of the subjects.[1] 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).[1] Usually this was asymptomatic. However, this is notable because females who are taking ethinylestradiol are at an increased risk for this side effect (25%).[1]
Dasabuvir could cause hepatitis B re-activation in people co-infected with hepatitis B and C viruses. The European Medicines Agency recommended screening all people for hepatitis B before starting dasabuvir for hepatitis C in order to minimize the risk of hepatitis B reactivation.[10]
Mechanism of action
Dasabuvir works by inhibiting the action of NS5B palm polymerase, effectively terminating RNA polymerization and stopping the replication of the HCV's genome.[11] By blocking NS5B polymerase, the virus can no longer multiply and infect new cells.[4]
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.[12]
