Adefovir Dipivoxil

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Absorption Approximate oral bioavailability is 59%.
Volume of distribution
  • 392 ± 75 mL/kg [intravenous administration of 1.0 mg/kg/day]
  • 352 ± 9 mL/kg [intravenous administration of 3.0 mg/kg/day]
Protein binding ≤4% over the adefovir concentration range of 0.1 to 25 μg/mL
Metabolism
Following oral administration, adefovir dipivoxil is rapidly converted to adefovir. Forty-five percent of the dose is recovered as adefovir in the urine over 24 hours at steady state following 10 mg oral doses. Adefovir is not a substrate of the cytochrome P450 enzymes.
Route of elimination Adefovir is renally excreted by a combination of glomerular filtration and active tubular secretion.
Half life Terminal elimination half-life of 7.48 ± 1.65 hours
Clearance
  • 469 +/- 99.0 mL/min [Patients with Unimpaired renal Function receiving a 10 mg single dose]
  • 356 +/- 85.6 mL/min [Patients with mild renal impairement receiving a 10 mg single dose]
  • 237 +/- 118 mL/min [Patients with moderate renal impairement receiving a 10 mg single dose]
  • 91.7+/- 51.3 mL/min [Patients with severe renal impairement receiving a 10 mg single dose]
Toxicity Renal tubular nephropathy characterized by histological alterations and/or increases in BUN and serum creatinine was the primary dose-limiting toxicity associated with administration of adefovir dipivoxil in animals. Nephrotoxicity was observed in animals at systemic exposures approximately 3–10 times higher than those in humans at the recommended therapeutic dose of 10 mg/day.
Affected organisms
  • Hepatitis B virus
Pathways
Pathway Name SMPDB ID
Smp00418 Adefovir Dipivoxil Pathway SMP00418

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