A single-dose study of denosumab in patients with various degrees of renal impairment

J Bone Miner Res. 2012 Jul;27(7):1471-9. doi: 10.1002/jbmr.1613.

Abstract

This 16-week study evaluated pharmacokinetics and pharmacodynamics of denosumab in 55 subjects with renal function ranging from normal to dialysis-dependent kidney failure. Participants received a single 60-mg subcutaneous dose of denosumab. Kidney function groups were based on calculations using the Cockcroft-Gault equation and U.S. Food and Drug Administration (FDA) guidance in place when the study was designed. Renal function did not have a significant effect on denosumab pharmacokinetics or pharmacodynamics. These findings suggest denosumab dose adjustment based on glomerular filtration rate is not required. Rapid decreases in serum C-telopeptide in all groups were sustained throughout the study. The most common adverse events were hypocalcemia (15%), pain in extremity (15%), and nausea (11%). Most adverse events were mild to moderate in severity. Calcium and vitamin D supplementation was not initially required by the study protocol, but was added during the trial. No subject who received adequate calcium and vitamin D supplementation became hypocalcemic. Seven subjects had nadir serum calcium concentrations between 7.5 and <8.0 mg/dL (1.9 and <2.0 mmol/L), and 5 subjects (4 with advanced renal disease) had nadir serum calcium <7.5 mg/dL (<1.9 mmol/L). Two subjects (1 symptomatic, 1 asymptomatic) were hospitalized for intravenous calcium gluconate treatment. At the recommended dose, denosumab is a useful therapeutic option for patients with impaired renal function. Supplementation of calcium and vitamin D is strongly recommended when patients initiate denosumab therapy, particularly in patients with reduced renal function.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Antibodies, Monoclonal, Humanized / pharmacokinetics*
  • Antibodies, Monoclonal, Humanized / pharmacology*
  • Area Under Curve
  • Calcium / metabolism
  • Calcium Gluconate / metabolism
  • Collagen Type I / blood
  • Denosumab
  • Female
  • Glomerular Filtration Rate / drug effects
  • Humans
  • Kidney / metabolism
  • Male
  • Middle Aged
  • Peptides / blood
  • Renal Dialysis
  • Renal Insufficiency / drug therapy*
  • United States
  • United States Food and Drug Administration
  • Vitamin D / metabolism

Substances

  • Antibodies, Monoclonal, Humanized
  • Collagen Type I
  • Peptides
  • collagen type I trimeric cross-linked peptide
  • Vitamin D
  • Denosumab
  • Calcium Gluconate
  • Calcium