Tolerability, safety and efficacy of a novel phosphate binder VS-505 (AP301): a Phase 2 dose-escalation and dose-ranging study in patients undergoing maintenance hemodialysis

Nephrol Dial Transplant. 2024 Sep 27;39(10):1649-1661. doi: 10.1093/ndt/gfae053.

Abstract

Background: VS-505 (AP301), an acacia and ferric oxyhydroxide polymer, is a novel fiber-iron-based phosphate binder. This two-part Phase 2 study evaluated the tolerability, safety and efficacy of oral VS-505 administered three times daily with meals in treating hyperphosphatemia in chronic kidney disease (CKD) patients receiving maintenance hemodialysis (MHD).

Methods: In Part 1, patients received dose-escalated treatment with VS-505 2.25, 4.50 and 9.00 g/day for 2 weeks each, guided by serum phosphorus levels. In Part 2, patients received randomized, open-label, fixed-dosage treatment with VS-505 (1.50, 2.25, 4.50 or 6.75 g/day) or sevelamer carbonate 4.80 g/day for 6 weeks. The primary efficacy endpoint was the change in serum phosphorus.

Results: The study enrolled 158 patients (Part 1: 25; Part 2: 133), with 130 exposed to VS-505 in total. VS-505 was well tolerated. The most common adverse events were gastrointestinal disorders, mainly feces discolored (56%) and diarrhea (15%; generally during Weeks 1-2 of treatment). Most gastrointestinal disorders resolved without intervention, and none was serious. In Part 1, serum phosphorus significantly improved (mean change -2.0 mg/dL; 95% confidence interval -2.7, -1.4) after VS-505 dose escalation. In Part 2, serum phosphorus significantly and dose-dependently improved in all VS-505 arms, with clinically meaningful reductions with VS-505 4.50 and 6.75 g/day, and sevelamer carbonate 4.80 g/day [mean change -1.6 (-2.2, -1.0), -1.8 (-2.4, -1.2) and -1.4 (-2.2, -0.5) mg/dL, respectively]. In both parts, serum phosphorus reductions occurred within 1 week of VS-505 initiation, returning to baseline within 2 weeks of VS-505 discontinuation.

Conclusion: VS-505, a novel phosphate binder, was well tolerated with a manageable safety profile, and effectively and dose-dependently reduced serum phosphorus in CKD patients with hyperphosphatemia receiving MHD.

Clinical trial registration number: NCT04551300 .

Keywords: VS-505; clinical study; hemodialysis; hyperphosphatemia; phosphate binder.

Publication types

  • Clinical Trial, Phase II
  • Randomized Controlled Trial
  • Multicenter Study

MeSH terms

  • Adult
  • Aged
  • Chelating Agents* / administration & dosage
  • Chelating Agents* / adverse effects
  • Chelating Agents* / therapeutic use
  • Dose-Response Relationship, Drug
  • Female
  • Ferric Compounds / administration & dosage
  • Ferric Compounds / adverse effects
  • Ferric Compounds / therapeutic use
  • Follow-Up Studies
  • Humans
  • Hyperphosphatemia* / drug therapy
  • Hyperphosphatemia* / etiology
  • Kidney Failure, Chronic / complications
  • Kidney Failure, Chronic / therapy
  • Male
  • Middle Aged
  • Phosphates / blood
  • Renal Dialysis* / adverse effects
  • Renal Insufficiency, Chronic / complications
  • Renal Insufficiency, Chronic / therapy
  • Sevelamer / administration & dosage
  • Sevelamer / therapeutic use

Substances

  • Chelating Agents
  • Phosphates
  • Ferric Compounds
  • Sevelamer

Associated data

  • ClinicalTrials.gov/NCT04551300