Drug intelligence / Profile preview

simeprevir + methadone

Development stage
Unknown
Lead developer
Janssen Pharmaceutica
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

**Simeprevir + methadone** is a combination of two pharmaceuticals: simeprevir, a direct-acting antiviral used primarily to treat chronic hepatitis C virus (HCV) infection by inhibiting the HCV NS3/4A protease[1][4], and methadone, a synthetic opioid agonist used for the treatment of opioid dependence and chronic pain. Simeprevir blocks viral replication by targeting NS3/4A serine protease essential for HCV polyprotein cleavage, preventing maturation of viral proteins[1]. Methadone acts primarily as a mu-opioid receptor agonist, producing analgesia and suppressing opioid withdrawal symptoms. The combination is not a marketed co-formulation but refers to concomitant use for patients who require antiviral therapy for HCV while on opioid substitution therapy. There is no known direct pharmacodynamic interaction between simeprevir and methadone; clinical studies indicate that simeprevir (a weak CYP3A inhibitor) does not alter methadone exposure significantly[2]. However, clinical caution is warranted due to potential additive central nervous system depressant effects and CYP-mediated drug-drug interactions, so patients must be monitored closely for adverse effects[3][4].

Other names
simeprevirmethadone
02

Targets

NS3/4A (Hepatitis C virus nonstructural protein 3/4A serine protease)MOR (Mu opioid receptor)

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