Differential inhibition features of direct-acting anti-hepatitis C virus agents against human organic anion transporting polypeptide 2B1

Highlights • Simeprevir (SMV) and asunaprevir (ASV) are potent inhibitors of OATP2B1. • SMV and ASV also show long-lasting OATP2B1 inhibitory effects. • The two inhibitory effects of the drugs can work in a co-operative manner. • These drugs have a drug–drug interaction risk potential with OATP2B1 s...

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Published in:International journal of antimicrobial agents 2015-10, Vol.46 (4), p.381-388
Main Authors: Furihata, Tomomi, Fu, Zhongguo, Suzuki, Yuki, Matsumoto, Shogo, Morio, Hanae, Tsubota, Akihito, Matsumoto, Sayaka, Chiba, Kan
Format: Article
Language:English
Subjects:
Antiviral Agents - metabolism
Biological Transport
Cells, Cultured
Direct-acting antivirals
Drug Interactions
Drug–drug interaction
Estrone - analogs & derivatives
Estrone - metabolism
Hepatitis C virus
Humans
Infectious Disease
Inhibitory Concentration 50
Long-lasting inhibition
Organic Anion Transporters - metabolism
Organic anion transporting polypeptide 2B1
Transporter
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Summary:Highlights • Simeprevir (SMV) and asunaprevir (ASV) are potent inhibitors of OATP2B1. • SMV and ASV also show long-lasting OATP2B1 inhibitory effects. • The two inhibitory effects of the drugs can work in a co-operative manner. • These drugs have a drug–drug interaction risk potential with OATP2B1 substrates.
ISSN:0924-8579
1872-7913
DOI:10.1016/j.ijantimicag.2015.05.013