Enfuvirtide does not require dose adjustment in patients with chronic kidney failure: results of a pharmacokinetic study of enfuvirtide in HIV-1-infected patients with impaired kidney function

J Acquir Immune Defic Syndr. 2008 Mar 1;47(3):342-5. doi: 10.1097/QAI.0b013e31816237f0.

Abstract

Objective: The aim of this study was to examine the influence of kidney disease and hemodialysis on the pharmacokinetics ofenfuvirtide.

Design: An open-label, multicenter, parallel group study of HIV-1-infected patients with varying degrees of kidney dysfunction.

Methods: A 90-mg dose of enfuvirtide was administered by subcutaneous injection to 3 groups of patients: group A, patients with normal kidney function; group B, patients with chronic kidney disease; and group C, patients with end-stage renal disease (ESRD) requiring dialysis. Patients with ESRD requiring dialysis received the 90-mg dose of enfuvirtide on 2 separate occasions; a dialysis day and a nondialysis day. After each dose, a full 48-hour pharmacokinetic profile was collected and pharmacokinetic parameters were estimated using model-independent techniques.

Results: Enfuvirtide area under the curve (AUCinfinity) and maximum observed enfuvirtide plasma concentration (Cmax) for patients with normal kidney function (group A) was 49.6 microg h/mL and 3.79 microg/mL, respectively. Patients with chronic kidney disease (group B) had higher AUCinfinity (80.3 microg h/mL) and Cmax (5.72 microg/mL), which was similar to patients with ESRD (group C) on both nondialysis days (AUCinfinity 71.1 microg h/mL; Cmax 5.34 microg/mL) and dialysis days (AUCinfinity 66.9 microg h/mL; Cmax 6.31 microg/mL). An average of< 13% of enfuvirtide was removed during the dialysis procedure. The incidence of adverse events was comparable for all study groups.

Conclusion: Enfuvirtide exposure observed in patients with ESRD requiring dialysis or chronic kidney disease was slightly higher than in patients with normal kidney function and similar to historical Cmax and AUC values from studies in patients with normal kidney function. Thus, enfuvirtide does not require dosage adjustment in patients with impaired kidney function.

Publication types

  • Clinical Trial
  • Comparative Study
  • Multicenter Study
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Area Under Curve
  • Dose-Response Relationship, Drug
  • Enfuvirtide
  • Female
  • HIV Envelope Protein gp41 / pharmacokinetics*
  • HIV Envelope Protein gp41 / therapeutic use
  • HIV Fusion Inhibitors / pharmacokinetics
  • HIV Fusion Inhibitors / therapeutic use
  • HIV Infections / drug therapy*
  • HIV Infections / metabolism
  • HIV-1 / drug effects*
  • Humans
  • Kidney / metabolism
  • Kidney / physiopathology
  • Kidney Failure, Chronic / physiopathology*
  • Kidney Failure, Chronic / therapy
  • Male
  • Metabolic Clearance Rate
  • Peptide Fragments / pharmacokinetics*
  • Peptide Fragments / therapeutic use
  • Renal Dialysis

Substances

  • HIV Envelope Protein gp41
  • HIV Fusion Inhibitors
  • Peptide Fragments
  • Enfuvirtide