Comparative Pharmacology
Head-to-head clinical analysis: INCIVEK versus VALGANCICLOVIR HYDROCHLORIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: INCIVEK versus VALGANCICLOVIR HYDROCHLORIDE.
INCIVEK vs VALGANCICLOVIR HYDROCHLORIDE
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.
Valganciclovir is an L-valyl ester prodrug of ganciclovir. After oral administration, it is rapidly hydrolyzed to ganciclovir, which is a synthetic guanosine analog. Ganciclovir is phosphorylated to ganciclovir triphosphate, which competitively inhibits viral DNA polymerase and incorporates into viral DNA, causing termination of viral DNA elongation.
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: 900 mg twice daily for cytomegalovirus (CMV) retinitis induction in immunocompromised patients; for prevention in transplant recipients: 900 mg once daily starting within 10 days of transplant.
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 of ganciclovir after valganciclovir administration is approximately 4-5 hours in patients with normal renal function. In renal impairment, half-life is significantly prolonged, up to 30-40 hours in severe impairment (CrCl <10 mL/min).
Approximately 91% of the radiolabeled dose is recovered in feces (79% as unchanged drug) and 9% in urine (1% as unchanged drug).
Primarily renal excretion of unchanged drug (approximately 90%), with the remainder as ganciclovir. Biliary/fecal elimination accounts for <5%.
Category C
Category D/X
Antiviral
Antiviral