Comparative Pharmacology
Head-to-head clinical analysis: GANCICLOVIR SODIUM versus INCIVEK.
Head-to-head clinical analysis: GANCICLOVIR SODIUM versus INCIVEK.
GANCICLOVIR SODIUM vs INCIVEK
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Ganciclovir is a synthetic guanine derivative that inhibits viral DNA synthesis. It is phosphorylated to ganciclovir triphosphate by viral thymidine kinase (CMV UL97 gene product) and cellular kinases. Ganciclovir triphosphate competitively inhibits viral DNA polymerase (CMV UL54 gene product) and incorporates into viral DNA, causing chain termination.
Inhibitor of the HCV NS3/4A serine protease, preventing cleavage of the HCV polyprotein, thereby inhibiting viral replication.
5 mg/kg IV every 12 hours for 14-21 days for induction; 5 mg/kg IV once daily or 6 mg/kg IV once daily 5 days per week for maintenance. Oral ganciclovir not available as sodium salt.
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).
None Documented
None Documented
Terminal half-life: 2.5-3.6 hours in normal renal function; prolonged in renal impairment (up to 30 hours in severe cases). Dosage adjustment required for CrCl <80 mL/min.
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.
Renal: >90% unchanged drug via glomerular filtration and tubular secretion. Biliary/fecal: <1%.
Approximately 91% of the radiolabeled dose is recovered in feces (79% as unchanged drug) and 9% in urine (1% as unchanged drug).
Category D/X
Category C
Antiviral
Antiviral