Intermittent Administration of Nitroglycerin Sublingual Powder Compared with Placebo in Outpatients with Peripheral Artery Disease: Results of a Randomised Proof of Concept Study

Eur J Vasc Endovasc Surg. 2021 Mar;61(3):457-465. doi: 10.1016/j.ejvs.2020.11.024. Epub 2020 Dec 23.

Abstract

Objective: Treatment of peripheral artery disease (PAD), Fontaine Stage IIb with vasoactive substances is of limited efficacy and does not last beyond the active treatment. Glyceryl trinitrate (GTN) is a vasodilating agent that relaxes vascular smooth muscle cells. The aim was to prove the concept that GTN sublingual powder has sustained clinical efficacy and adequate safety in these patients.

Methods: This was a multicentre, randomised, double blind, placebo controlled, forced titration, proof of concept study (phase IIa). Patients had a treadmill test at baseline, after 12 weeks of GTN/placebo administration, and at 19 and 26 weeks (without treatment). Primary objectives were an increase in initial claudication distance (ICD) and absolute claudication distance (ACD) at 12 weeks.

Results: Ninety-five patients were screened and 73 randomised, of which 53 patients completed the 12 week treatment phase (GTN 26, placebo 27). At a baseline ICD of 59.2 ± 32.8 m (GTN) and 57.5 ± 39.7 m (placebo), GTN led to a placebo corrected ICD increase of 23.2% vs. baseline (p = .35). Baseline ACD was 105.3 ± 52.9 m (GTN) and 106.1 ± 95.0 m (placebo), and GTN led to a placebo corrected increase of 3.6% (p = .44), with substantial interindividual variation. The change in claudication distance was greater in patients with an ICD of ≥50 m at baseline (ΔICD 29.3%; p = .19), and an ACD ≥ 100 m (ΔACD 8.5%; p = .40). The effect lasted beyond the active treatment period as shown by a 49.3% increase in ICD (p = .31) and a 20.6% increase in ACD (p = .21) by week 26. GTN sublingual powder was well tolerated.

Conclusion: Intermittent treatment with nitroglycerin sublingual powder may represent a potential treatment option for patients with PAD stage Fontaine IIb, with an immediate and a sustained effect. The observed increases in ACD and ICD were however not statistically significant in this phase IIa proof of concept study. Further studies are required.

Keywords: Arteriogenesis; Claudication; Glyceryl trinitrate; Nitroglycerin; Peripheral artery disease; Sublingual powder.

Publication types

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

MeSH terms

  • Administration, Sublingual
  • Adult
  • Aged
  • Aged, 80 and over
  • Ambulatory Care*
  • Double-Blind Method
  • Drug Administration Schedule
  • Exercise Tolerance / drug effects*
  • Female
  • Germany
  • Humans
  • Intermittent Claudication / diagnosis
  • Intermittent Claudication / drug therapy*
  • Intermittent Claudication / physiopathology
  • Male
  • Middle Aged
  • Nitroglycerin / administration & dosage*
  • Nitroglycerin / adverse effects
  • Outpatients
  • Peripheral Arterial Disease / diagnosis
  • Peripheral Arterial Disease / drug therapy*
  • Peripheral Arterial Disease / physiopathology
  • Powders
  • Proof of Concept Study
  • Recovery of Function
  • Time Factors
  • Treatment Outcome
  • Vasodilator Agents / administration & dosage*
  • Vasodilator Agents / adverse effects

Substances

  • Powders
  • Vasodilator Agents
  • Nitroglycerin