Dasabuvir

Oral
Chronic hepatitis C

Moderate (Child-Pugh B): Not recommended. Severe (Child-Pugh C): Contraindicated.

HIV co-infection w/o suppressive antiretroviral therapy. Severe hepatic impairment. Co-admin w/ ethinylestradiol-containing products, strong or moderate enzyme inducers, strong CYP2C8 inhibitors, systemic tacrolimus, sirolimus, or everolimus.

Patient w/ hepatitis B virus infection. Moderate hepatic impairment. Not intended for admin as monotherapy.

Significant: Elevated ALT.
Nervous: Insomnia, fatigue, asthenia.
GI: Nausea.
Haematologic: Anaemia.
Dermatologic: Pruritus, angioedema.
Potentially Fatal: Hepatic decompensation and hepatic failure.

May affect the efficacy of vit K antagonists. Increases exposure to rosuvastatin. Decreased exposure to CYP2C19 substrate (e.g. lansoprazole). Increased plasma concentration w/ teriflunomide, deferasirox.
Potentially Fatal: Increased risk of ALT elevations w/ ethinylestradiol-containing products. Decreased plasma levels and therapeutic effect w/ strong or moderate enzyme inducers (e.g. carbamazepine, efavirenz, rifampicin). Increased plasma levels w/ strong CYP2C8 inhibitors (e.g. gemfibrozil). Increases the concentration of systemic tacrolimus, sirolimus, or everolimus.

Increased absorption w/ food. Decreased plasma levels w/ St. John’s wort.

Description:
Mechanism of Action: Dasabuvir is a non-nucleoside inhibitor of non-structural protein 5B (NS5B), an RNA-dependent RNA polymerase which is an essential component of the hepatitis C virus replication process.
Pharmacokinetics:
Absorption: Absorbed from the GI tract. Increased absorption w/ food. Time to peak plasma concentration: 4-5 hr.
Distribution: Plasma protein binding: >99.5% (dasabuvir); 94.5% (M1 metabolite).
Metabolism: Metabolised mainly by CYP2C8, and to a lesser extent by CYP3A.
Excretion: Elimination half-life: Approx 6 hr.

Source: National Center for Biotechnology Information. PubChem Database. Dasabuvir, CID=56640146, https://pubchem.ncbi.nlm.nih.gov/compound/Dasabuvir (accessed on Jan. 20, 2020)

Store below 30°C.
Any unused portions should be disposed of in accordance w/ local requirements.

Antivirals

J05AP09 - dasabuvir ; Belongs to the class of antivirals for treatment of HCV infections. Used in the treatment of hepatitis C viral infections.

Buckingham R (ed). Dasabuvir. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/06/2017.

Joint Formulary Committee. Dasabuvir. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/06/2017.