Comparative Pharmacology
Head-to-head clinical analysis: CIDOFOVIR versus INCIVEK.
Head-to-head clinical analysis: CIDOFOVIR versus INCIVEK.
CIDOFOVIR vs INCIVEK
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Cidofovir is a nucleotide analog that inhibits viral DNA polymerase by competing with deoxycytidine triphosphate for incorporation into viral DNA, resulting in chain termination and inhibition of viral replication.
Inhibitor of the HCV NS3/4A serine protease, preventing cleavage of the HCV polyprotein, thereby inhibiting viral replication.
5 mg/kg intravenously once weekly for 2 weeks, then 5 mg/kg every 2 weeks. Administer with probenecid 2 g orally 3 hours before dose, then 1 g at 2 and 8 hours after dose. Hydrate with 1 L normal saline before infusion.
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
Clinical Note
moderateCidofovir + Teriflunomide
"The serum concentration of Teriflunomide can be increased when it is combined with Cidofovir."
Clinical Note
moderateTenofovir disoproxil + Cidofovir
"Tenofovir disoproxil may decrease the excretion rate of Cidofovir which could result in a higher serum level."
Terminal elimination half-life is approximately 2.5 hours. However, the intracellular half-life of the active diphosphate metabolite is >48 hours, supporting once-weekly dosing.
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 excretion of unchanged drug via glomerular filtration and tubular secretion accounts for approximately 90% of the administered dose. Biliary/fecal elimination is minimal (<5%).
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