Clemizole Clemizole 442-52-4
Clemizole is a H1 histamine receptor antagonist.Recently, researchers have identified that clemizole hydrochloride can inhibit NS4B's RNA binding and hepatitis C virus (HCV) replication.
IC50 Value: 8 mM (NS4B) [1]
Target: H1 receptor; Anti-HCV
in vitro: Although significant, clemizole's antiviral effect is moderate (50% effective concentration of 8 microM against an HCV genotype 2a clone). Combinations of clemizole with either interferon, ribavirin, or the nucleoside (NM283) and nonnucleoside (HCV796) HCV polymerase inhibitors were additive [1]. The differences in the rodent and human pathways for clemizole metabolism were of importance, because the predominant human metabolite was found to have synergistic anti-HCV activity [2].
in vivo: Clemizole and reserpine treatment did not produce any modification of the dose-response curve to histamine [3].
Clinical trial: Safety and Tolerability Study of Clemizole Hydrochloride to Treat Hepatitis C in Subjects Who Are Treatment-Naive (CLEAN-1). NCT00945880. Phase 1
Clemizole is a H1 histamine receptor antagonist.Recently, researchers have identified that clemizole hydrochloride can inhibit NS4B's RNA binding and hepatitis C virus (HCV) replication.
IC50 Value: 8 mM (NS4B) [1]
Target: H1 receptor; Anti-HCV
in vitro: Although significant, clemizole's antiviral effect is moderate (50% effective concentration of 8 microM against an HCV genotype 2a clone). Combinations of clemizole with either interferon, ribavirin, or the nucleoside (NM283) and nonnucleoside (HCV796) HCV polymerase inhibitors were additive [1]. The differences in the rodent and human pathways for clemizole metabolism were of importance, because the predominant human metabolite was found to have synergistic anti-HCV activity [2].
in vivo: Clemizole and reserpine treatment did not produce any modification of the dose-response curve to histamine [3].
Clinical trial: Safety and Tolerability Study of Clemizole Hydrochloride to Treat Hepatitis C in Subjects Who Are Treatment-Naive (CLEAN-1). NCT00945880. Phase 1
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