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Simeprevir

OLYSIO

Pronunciation: sim-E-pre-veer

Simeprevir ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Simeprevir ballicule

What it isA second-generation HCV NS3/4A protease inhibitor that blocks the polyprotein processing essential for hepatitis C replication.

Why this oneCombined with sofosbuvir or peginterferon/ribavirin for genotype 1/4 HCV, it is now largely obsolete and retained mainly for interaction data.

What limits itA boxed warning for HBV reactivation, plus photosensitivity, rash, and reduced efficacy with the Q80K polymorphism, limit its use.

Simeprevir molecular structure (skeletal formula)
Molecular structure: Simeprevir

Simeprevir prescription history

Animated chart of estimated U.S. prescriptions per year, Hepatitis C meds (1987–2026). Simeprevir enters in 2013 (estimated).

⚠ BOXED WARNING

Principal riskBoxed warning: risk of hepatitis B virus reactivation, including fulminant hepatitis and death, in patients coinfected with HCV and HBV.

Sulfonamide

Sulfonamide-derived drug (non-antibacterial) — label warns

An acyl sulfonamide with no N4 aromatic amine and no N1 heterocycle; the label warns on sulfonamide allergy. Not named by Khan; the evidence for the non-antimicrobials as a group says cross-reactivity is unlikely.

Open the sulfonamide hypersensitivity presentation → · sources [n] are on its References slide.

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger1 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

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