Comparative Pharmacology
Head-to-head clinical analysis: INCIVEK versus REBETOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: INCIVEK versus REBETOL.
INCIVEK vs REBETOL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Inhibitor of the HCV NS3/4A serine protease, preventing cleavage of the HCV polyprotein, thereby inhibiting viral replication.
Ribavirin, a guanosine analog, inhibits viral RNA-dependent RNA polymerase and inosine monophosphate dehydrogenase, leading to a decrease in intracellular guanosine triphosphate pools and impairment of viral RNA synthesis.
Incivek (telaprevir) is administered orally at a dose of 750 mg (two 375 mg tablets) three times daily (every 7-9 hours) with food (not low-fat).
Oral: 400-600 mg twice daily (800-1200 mg/day) based on body weight (≤75 kg: 400 mg twice daily; >75 kg: 600 mg twice daily) in combination with interferon alfa or peginterferon alfa.
None Documented
None Documented
Terminal elimination half-life ranges from 4 to 13 hours (mean ~7 hours) in healthy volunteers; prolonged to 10-20 hours in HCV-infected patients.
Terminal elimination half-life: 120-200 hours (multiple doses, due to extensive accumulation in erythrocytes). Single dose: 24-36 hours. Clinically, steady state is reached in approximately 4 weeks.
Approximately 91% of the radiolabeled dose is recovered in feces (79% as unchanged drug) and 9% in urine (1% as unchanged drug).
Renal: 10-15% unchanged; biliary/fecal: 60-70% as metabolites; pulmonary excretion of CO2 contributes to elimination of ribavirin's triazole moiety. Approximately 10-20% excreted in feces as unchanged drug and metabolites.
Category C
Category C
Antiviral
Antiviral