Drug reference

voxilaprevir

NS3 protease inhibitor · Antiviral, Hepatitis C agent

NS3 protease inhibitorAntiviral, Hepatitis C agent

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

7 major

incl. contraindicated

PREGNANCY

—

not curated

Top interactionssee all 12 →

Potent Oatp1b1 InhibitorsContraindicatedTextbookG&G 14e · p1240, p1242
AtazanavirSevereDatabaseDDInter
CyclosporineSevereDatabaseDDInter
EdoxabanSevereDatabaseDDInter

Mechanism

Voxilaprevir is an inhibitor of the non-structural protein 3 (NS3) protease of the hepatitis C virus, which is crucial for viral polyprotein processing and replication.

Indications

HCV genotypes 1 to 6 for second-line treatment in patients who have previously failed a DAA regimen (as part of fixed-dose combination with sofosbuvir and velpatasvir)Genotype 3 and cirrhosis with ribavirin (as part of fixed-dose combination with sofosbuvir and velpatasvir)

Dosing

Adult: 100 mg (as part of fixed-dose combination with sofosbuvir and velpatasvir) once daily for 12 weeks for all genotypes
Renal adjustment: Exposures are 71% higher in eGFR <30 mL/min/1.73 m2, but unlikely to be clinically relevant unless combined with other risk factors

Pharmacokinetics

Half-life

33 h

Protein binding

More than 99% bound to plasma proteins

Excretion

Primarily through biliary excretion (94% in feces, 40% as parent drug)

Contraindications

Decompensated cirrhosis
Moderate or severe hepatic impairment
Concomitant use with potent OATP1B1 inhibitors (e.g., cyclosporine)
Concomitant use with BCRP substrates (e.g., methotrexate, mitoxantrone, imatinib, irinotecan, lapatinib, rosuvastatin, sulfasalazine, topotecan)
Concomitant use with potent P-gp or CYP3A inducers

Side effects

Common

HeadacheFatigueDiarrheaNausea

Drug interactions

Potent Oatp1b1 Inhibitors

Contraindicated

Textbook

Significantly increased voxilaprevir exposures, potentially leading to hepatotoxicity.

Potent OATP1B1 inhibitors (e.g., cyclosporine) should not be used with voxilaprevir. Do not use with potent OATP1B1 inhibitors.

Source: G&G 14e · p1240, p1242

Atazanavir

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Cyclosporine

Severe

Database

Clinical effect not specified

Source: DDInter

Edoxaban

Severe

Database

Clinical effect not specified

Source: DDInter

Pitavastatin

Severe

Database

Clinical effect not specified

Source: DDInter

Pravastatin

Severe

Database

Clinical effect not specified

Source: DDInter

Rosuvastatin

Severe

Database

Increased exposures of rosuvastatin.

Should be avoided with voxilaprevir. Do not use with BCRP substrates with narrow therapeutic indices.

Source: DDInter

Cyp3a Inducers

Moderate

Textbook

Reduced plasma levels and potential loss of efficacy of voxilaprevir.

No specific management stated, but likely requires careful consideration if co-administering.

Source: Harrison 22e · unknown

Ethinyl Estradiol Containing Hormonal Contraception

Moderate

Textbook

Liver enzyme elevations and potential hepatotoxicity.

Caution is needed. Avoid during and for 2 weeks after treatment due to potential hepatotoxicity.

Source: G&G 14e · p1240, p1242

Imatinib

Moderate

Textbook

Increased exposures of imatinib.

Should be avoided with voxilaprevir. Do not use with BCRP substrates with narrow therapeutic indices.

Source: G&G 14e · p1240, p1242

Irinotecan

Moderate

Textbook

Increased exposures of irinotecan.

Should be avoided with voxilaprevir. Do not use with BCRP substrates with narrow therapeutic indices.

Source: G&G 14e · p1240, p1242

Methotrexate

Moderate

Textbook

Increased exposures of methotrexate.

Should be avoided with voxilaprevir. Do not use with BCRP substrates with narrow therapeutic indices.

Source: G&G 14e · p1240, p1242

Related guidelines

Hepatitis B — chronic infection

INASL · Gastroenterology · 2023

Hepatitis B — chronic infection

WHO · Hepatology · 2025

Cirrhosis

OTHER · Hepatology · 2021

Hepatitis B — chronic infection

EASL · Gastroenterology · 2025

Hepatitis C — chronic infection

EASL · Gastroenterology · 2020

Other NS3 protease inhibitor drugs

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Sources: Goodman & Gilman 14e, Harrison 22e·Verified: 2026-05-10 · House clinical team