Current and potential treatment options for hyperphosphatemia

Expert Opin Drug Saf. 2018 Jun;17(6):597-607. doi: 10.1080/14740338.2018.1476487. Epub 2018 May 21.

Abstract

Introduction: Hyperphosphatemia is common in late stages of chronic kidney disease and is often associated with elevated parathormone levels, abnormal bone mineralization, extra-osseous calcification, and increased risk of cardiovascular events and death. Several classes of oral phosphate binders are available to help control plasma phosphorus levels. Although effective at lowering serum phosphorus, they all have safety, tolerability, and compliance issues that need to be considered when selecting which one to use.

Areas covered: This paper reviews the most established treatment options for hyperphosphatemia, in patients with chronic kidney disease, focusing on the new inhibitors of active phosphate absorption.

Expert opinion: The prevention and the treatment of hyperphosphatemia is today far to be satisfactory. Nonetheless, an extending range of phosphate binders are now available. Aluminum has potentially serious toxic risks. Calcium-based binders are very effective but can lead to hypercalcemia and/or positive calcium balance and progression of cardiovascular calcification. No long-term data are available for the new calcium acetate/magnesium combination product. Lanthanum is an effective phosphate binder, and long-term effects of tissue deposition seem clinically irrelevant. Sevelamer, appear to have profiles that would lead to pleiotropic effects and reduced progression of vascular calcification, and the main adverse events seen with these agents are gastrointestinal. Iron has a powerful capability of binding phosphate, thus numerous preparations are available, both with and without significant systemic absorption of the iron component. The inhibitors of active intestinal phosphate transport, with their very selective mechanism of action and low pill burden seem the most interesting approach; however, do not seem at present to be effective alone, in reducing serum phosphorus levels.

Keywords: Chronic kidney disease; hyperphosphatemia; non-calcium phosphate binders; phosphate binder; safety; tolerability.

Publication types

  • Review

MeSH terms

  • Animals
  • Chelating Agents / adverse effects
  • Chelating Agents / pharmacology
  • Chelating Agents / therapeutic use*
  • Drug Design
  • Humans
  • Hyperphosphatemia / drug therapy*
  • Hyperphosphatemia / etiology
  • Iron / pharmacology
  • Iron / therapeutic use
  • Lanthanum / adverse effects
  • Lanthanum / pharmacology
  • Lanthanum / therapeutic use
  • Phosphates / metabolism
  • Renal Insufficiency, Chronic / complications*
  • Sevelamer / adverse effects
  • Sevelamer / pharmacology
  • Sevelamer / therapeutic use

Substances

  • Chelating Agents
  • Phosphates
  • Lanthanum
  • Sevelamer
  • Iron