Glecaprevir – NS3/4A Protease Inhibitor for Hepatitis C
Glecaprevir is an innovative direct-acting antiviral agent, which is a pangenotypic inhibitor of the hepatitis C virus (HCV) NS3/4A protease. The drug is a product of advanced molecular biology and is designed for the complete cure of chronic hepatitis C. Glecaprevir effectively blocks the enzyme required by the virus to cleave the polyprotein and subsequently assemble new viral particles, making further spread of the infection within the body impossible.
The mechanism of action of glecaprevir involves highly selective binding to the active site of the NS3/4A serine protease. A unique feature of the molecule is its high efficacy against a wide range of viral genetic variants, including those that have developed resistance to first-generation protease inhibitors. The drug exhibits potent antiviral activity against all major HCV genotypes (1 through 6), allowing its use as a universal solution without mandatory prior genotyping in certain protocols. Glecaprevir is characterized by a high degree of plasma protein binding and primary excretion via the intestines, ensuring a stable therapeutic concentration in the liver tissues—the primary site of viral replication.
The drug is always used in a fixed-dose combination with pibrentasvir, providing a double-strike against the viral replication cycle.
Indications
Glecaprevir is indicated for the treatment of chronic hepatitis C in adults and children over 3 years of age in the following cases:
- All HCV Genotypes (1–6): therapy for patients without cirrhosis or with compensated cirrhosis (Child-Pugh Class A).
- Patients with Renal Impairment: the drug is a priority choice for individuals at any stage of kidney disease, including those on dialysis.
- Prior Treatment Experience: treatment for patients previously treated with interferon-based regimens or sofosbuvir who did not achieve a cure.
- Special Groups: therapy for individuals with HIV-1 co-infection who have similar hepatitis treatment protocols.
Dosage and administration
The glecaprevir dosing regimen (in combination with pibrentasvir) is standardized to ensure the highest sustained virologic response (SVR) rate.
- Standard Dosage: daily intake of three tablets (each containing 100 mg of glecaprevir and 40 mg of pibrentasvir), taken simultaneously.
- Administration Method: the drug must be taken orally once daily strictly with food. Food significantly increases the bioavailability of the active substance.
- Course Duration: lasts 8 weeks for most treatment-naive patients without cirrhosis and may be extended to 12–16 weeks depending on clinical history.
- Missed Dose: if less than 18 hours have passed since the usual time, the dose should be taken immediately. If more than 18 hours, the dose is skipped.
- Therapy Monitoring: viral load assessment is conducted 12 weeks after completion of the course to confirm a total cure.
