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K+ binders are not all the same

Physical and chemical properties of K+ binders1,2

Physical and chemical properties of K+ binders1,2
  VELTASSA (patiromer) Kayexalate (sodium polystyrene sulfonate) Lokelma® (sodium zirconium cyclosilicate)
Counterion Calcium (Ca++) Sodium (Na+) Sodium (Na+) Hydrogen (H+)
Na+ per dose — 1500–6000 mg 40‍0–1200 mg
Dosage strengths 8.4 g, 16.8 g, 25.2 g 15–60 g 5 g, 10 g, 15 g
Description Spherical, free-flowing beads Powdered form of resin Insoluble white powder
Chemical structure Polymer Resin Crystal
Microscopic view VELTASSA (patiromer)VELTASSA (patiromer) Kayexalate (sodium polystyrene sulfonate)Kayexalate (sodium polystyrene sulfonate) Lokelma (sodium zirconium cyclosilicate)Lokelma (sodium zirconium cyclosilicate)
Indication VELTASSA is indicated for the treatment of hyperkalemia Kayexalate is indicated for the treatment of hyperkalemia Lokelma® is indicated for the treatment of hyperkalemia in adults
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Kayexalate was a registered trademark of Concordia Pharmaceuticals, Inc. Lokelma is a registered trademark of the AstraZeneca group of companies.

The uniform spherical shape, defined particle size, and low swelling ratio of VELTASSA are believed to contribute to patient tolerability.3,4

Due to their delayed onset of action, these K+ binders should not be used as monotherapy for the emergency treatment of life-threatening hyperkalemia.

No head-to-head clinical trials have been conducted between sodium polystyrene sulfonate, sodium zirconium cyclosilicate, and patiromer; therefore, no safety or efficacy comparisons can be made.

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INDICATION

VELTASSA is indicated for the treatment of hyperkalemia in adults and pediatric patients ages 12 years and older.

Limitation of Use: VELTASSA should not be used as an emergency treatment for life-threatening hyperkalemia because of its delayed onset of action.

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INDICATION & Important Safety Information

Important Safety Information

VELTASSA is indicated for the treatment of hyperkalemia.

Limitation of Use: VELTASSA should not be used as an emergency treatment for life-threatening hyperkalemia because of its delayed onset of action.

CONTRAINDICATIONS

VELTASSA is contraindicated in patients with a history of a hypersensitivity reaction to VELTASSA or any of its components.

INDICATION

VELTASSA is indicated for the treatment of hyperkalemia in adults and pediatric patients ages 12 years and older.

Limitation of Use: VELTASSA should not be used as an emergency treatment for life-threatening hyperkalemia because of its delayed onset of action.

IMPORTANT SAFETY INFORMATION

CONTRAINDICATIONS

VELTASSA is contraindicated in patients with a history of a hypersensitivity reaction to VELTASSA or any of its components.

WARNINGS AND PRECAUTIONS

Worsening of Gastrointestinal Motility: Avoid use of VELTASSA in patients with severe constipation, bowel obstruction or impaction, including abnormal post-operative bowel motility disorders, because VELTASSA may be ineffective and may worsen gastrointestinal conditions. Patients with a history of bowel obstruction or major gastrointestinal surgery, severe gastrointestinal disorders, or swallowing disorders were not included in clinical studies.

Hypomagnesemia: VELTASSA binds to magnesium in the colon, which can lead to hypomagnesemia. In clinical studies, hypomagnesemia was reported as an adverse reaction in 5.3% of adult patients treated with VELTASSA. Approximately 9% of adult patients in clinical trials developed hypomagnesemia with a serum magnesium value < 1.4 mg/dL. Monitor serum magnesium. Consider magnesium supplementation in patients who develop low serum magnesium levels.

MOST COMMON ADVERSE REACTIONS

The most common adverse reactions (incidence ≥  2%) in adult patients treated with VELTASSA were constipation (7.2%), hypomagnesemia (5.3%), diarrhea (4.8%), nausea (2.3%), abdominal discomfort (2.0%) and flatulence (2.0%). Mild to moderate hypersensitivity reactions were reported in 0.3% of patients treated with VELTASSA and included edema of the lips.The safety profile of VELTASSA in a study of 14 pediatric patients ages 12 to 17 years was generally similar to that observed in adult patients.

  1. References:
  2. Kayexalate (sodium polystyrene sulfonate) [product information]. Bridgewater, NJ: Sanofi Aventis US LLC; 2017.
  3. Lokelma® (sodium zirconium cyclosilicate) [package insert]. Wilmington, DE: AstraZeneca Pharmaceuticals LP; 2022.
  4. Li L, Harrison SD, Cope MJ, et al. Mechanism of action and pharmacology of patiromer, a nonabsorbed cross-linked polymer that lowers serum potassium concentration in patients with hyperkalemia. J Cardiovasc Pharmacol Ther. 2016;21(5):456–465. doi:10.1177/1074248416629549
  5. Hatakeyama S, Murasawa H, Narita T, et al. Switching hemodialysis patients from sevelamer hydrochloride to bixalomer: a single-center, non-randomized analysis of efficacy and effects on gastrointestinal symptoms and metabolic acidosis. BMC Nephrol. 2013;14:222. doi:10.1186/1471-2369-14-222