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H413 (100%): May cause long lasting harmful effects to aquatic life [Hazardous to the aquatic environment, long-term hazard]

P273, and P501 (click each P-code to see the statement)

Aggregated GHS information provided per 2 reports by companies from 1 notifications to the ECHA C&L Inventory.

J - Antiinfectives for systemic use

QJ - Antiinfectives for systemic use

Dasabuvir is a non-nucleoside inhibitor of the HCV RNA-dependent RNA polymerase encoded by the NS5B gene, which is essential for replication of the viral genome. Based on drug resistance mapping studies of HCV genotypes 1a and 1b, dasabuvir targets the palm domain of the NS5B polymerase, and is therefore referred to as a non-nucleoside NS5B-palm polymerase inhibitor. The EC50 values of dasabuvir against genotype 1a-H77 and 1b-Con1 strains in HCV replicon cell culture assays were 7.7 nM and 1.8 nM, respectively. By binding to NS5b outside of the active site of the enzyme, dasabuvir induces a conformational change thereby preventing further elongation of the nascent viral genome. A limitation of binding outside of the active site is that these binding sites are poorly preserved across the viral genotypes. This results in a limited potential for cross-genotypic activity and increased potential for development of resistance. Dasabuvir is therefore limited to treating genotypes 1a and 1b, and must be used in combination with other antiviral products.

DE54EQW8T1

DASABUVIR

Established Pharmacologic Class [EPC] - Hepatitis C Virus Non-Nucleoside NS5B Palm Polymerase Inhibitor

Mechanisms of Action [MoA] - RNA Replicase Inhibitors

Mechanisms of Action [MoA] - UGT1A1 Inhibitors

Mechanisms of Action [MoA] - Breast Cancer Resistance Protein Inhibitors

Dasabuvir reaches peak plasma concentration 4 hours after administration. The absolute bioavailability of Dasabuvir is 70%.

Dasabuvir is mainly excreted in the feces (94.4%) with very little excreted in the urine (2%). 26.2% and 0.03% of the drug excreted in the feces and urine respectively was present as the parent compound suggesting metabolism as the major elimination pathway.

Dasabuvir has a volume of distribution at steady state of 149 liters.

Clearance of Dasabuvir has not been determined.