Effect of Tenapanor on Serum Phosphate in Patients Receiving Hemodialysis

J Am Soc Nephrol. 2017 Jun;28(6):1933-1942. doi: 10.1681/ASN.2016080855. Epub 2017 Feb 3.

Abstract

Hyperphosphatemia is common among patients with CKD stage 5D and is associated with morbidity and mortality. Current guidelines recommend lowering serum phosphate concentrations toward normal. Tenapanor is a minimally absorbed small molecule inhibitor of the sodium/hydrogen exchanger isoform 3 that functions in the gut to reduce sodium and phosphate absorption. This randomized, double-blind, placebo-controlled trial assessed the effects of tenapanor on serum phosphate concentration in patients with hyperphosphatemia receiving hemodialysis. After a 1- to 3-week washout of phosphate binders, we randomly assigned 162 eligible patients (serum phosphate =6.0 to <10.0 mg/dl and a 1.5-mg/dl increase from before washout) to one of six tenapanor regimens (3 or 30 mg once daily or 1, 3, 10, or 30 mg twice daily) or placebo for 4 weeks. The primary efficacy end point was change in serum phosphate concentration from baseline (randomization) to end of treatment. In total, 115 patients (71%) completed the study. Mean serum phosphate concentrations at baseline (after washout) were 7.32-7.92 mg/dl for tenapanor groups and 7.87 mg/dl for the placebo group. Tenapanor provided dose-dependent reductions in serum phosphate level from baseline (least squares mean change: tenapanor =0.47-1.98 mg/dl; placebo =0.54 mg/dl; P=0.01). Diarrhea was the most common adverse event (tenapanor =18%-68%; placebo =12%) and frequent at the highest tenapanor doses. In conclusion, tenapanor treatment resulted in statistically significant, dose-dependent reductions in serum phosphate concentrations in patients with hyperphosphatemia receiving hemodialysis. Additional studies are required to clarify the optimal dosing of tenapanor in patients with CKD-related hyperphosphatemia.

Keywords: NHE3; chronic kidney disease; hemodialysis; hyperphosphatemia; sodium–hydrogen exchanger 3; tenapanor.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Double-Blind Method
  • Female
  • Humans
  • Hyperphosphatemia / blood
  • Hyperphosphatemia / drug therapy*
  • Isoquinolines / pharmacology*
  • Male
  • Middle Aged
  • Phosphates / blood
  • Renal Dialysis*
  • Sulfonamides / pharmacology*

Substances

  • Isoquinolines
  • Phosphates
  • Sulfonamides
  • tenapanor