Glecaprevir Intermediate 1360828-80-3

China [CN]

Glecaprevir (ABT-493) is a hepatitis C virus (HCV) NS3/4A serine protease inhibitor developed by AbbVie.  It is clinically used in a fixed-dose combination with pibrentasvir (GLE/PIB, brand name: Mavyret®), providing a pan-genotypic, short-course, and highly effective first-line treatment for hepatitis C. I. Basic Information

Generic Name: Glecaprevir

Code: ABT-493

CAS Number: 1365970-03-1

Molecular Formula: C₃₈H₄₆F₄N₆O₉S

Originator: Enanta Pharmaceuticals (Research), AbbVie (Development/Commercialization)

Clinical Form: Fixed-dose combination (GLE 100 mg + PIB 40 mg/tablet)

II. Mechanism of Action

Target: HCV NS3/4A protease (a key enzyme essential for viral replication)

Mechanism: Inhibits NS3/4A protease activity, blocking the cleavage and maturation of HCV polyproteins, preventing viral replication and assembly.

Combination Synergy: Used in combination with Pibrentasvir (PIB, an NS5A inhibitor), providing dual-target blockade, significantly improving cure rates and reducing the risk of resistance.

III. Core Indications (GLE/PIB Combination)

For patients aged 3 years and older with HCV genotypes 1–6, without cirrhosis or with compensated cirrhosis (Child-Pugh A):

Treatment-naïve patients: All genotypes (1–6), 8-week treatment course, SVR₁₂ ≈ 95%–100%

Treatment-experienced patients: Genotype 1, previously treated with only NS5A inhibitors or NS3/4A inhibitors (not both simultaneously), 16-week treatment course

Special populations: Renal impairment/dialysis, children (3–17 years), HIV/HCV co-infection, acute HCV

IV. Dosage and Administration (Adults / Children ≥45 kg)

Dosage: 3 tablets per dose, once daily, taken with food (GLE 300 mg + PIB 120 mg)

Treatment Duration:

Treatment-naïve (without/compensated cirrhosis): 8 weeks

Treatment-experienced (GT1, NS5A or PI failure): 16 weeks

Children (3–12 years, 12–45 kg): [Dosage information for children in this weight range is missing in the original text.] kg): Oral granules, administered according to body weight

V. Pharmacokinetics (GLE)

Absorption: Bioavailability is increased when taken with food.

Protein binding rate: 97.5%

Metabolism: Primarily metabolized by CYP3A

Half-life: Approximately 6 hours

Excretion: 92.1% in feces, 0.7% in urine (no dose adjustment needed for renal impairment)