Riociguat for pulmonary arterial hypertension and chronic thromboembolic pulmonary hypertension: Results from a phase II long-term extension study

Respir Med. 2017 Jul:128:50-56. doi: 10.1016/j.rmed.2017.05.008. Epub 2017 May 16.

Abstract

Background: Riociguat was well tolerated and improved exercise and functional capacity in patients with pulmonary arterial hypertension (PAH) and inoperable chronic thromboembolic pulmonary hypertension (CTEPH) in a 12-week Phase II trial. We present final data from the long-term extension phase of this study.

Methods: During this multicenter, open-label, uncontrolled long-term extension study, riociguat dose could be changed at the physician's discretion (range 0.5-2.5 mg three times daily). The primary outcome was long-term safety and tolerability of riociguat; secondary outcomes included 6-minute walking distance, World Health Organization functional class, survival, and clinical worsening-free survival.

Results: Sixty-eight patients (inoperable CTEPH, n = 41; PAH, n = 27) entered the long-term extension. Median treatment duration at the final data cut-off was 77 months. The most common adverse events were nasopharyngitis (57%) and peripheral edema (37%). Three patients (4%) experienced serious adverse events of hemoptysis: two moderate, one severe, none fatal or considered drug-related. At Month 48, 6-minute walking distance increased from baseline by 69 ± 105 m, and World Health Organization functional class improved/stabilized/worsened versus baseline in 50/45/5% of patients. Three-year survival and clinical worsening-free survival were 91% and 49%, respectively (with patients censored if they withdrew without experiencing an event). Starting a new PAH treatment was the most frequent clinical worsening event.

Conclusions: Improvements in exercise and functional capacity were maintained at 4 years in patients remaining on treatment, with no new safety signals identified. These data support riociguat as a long-term treatment option for PAH and inoperable CTEPH.

Trial registered at: ClinicalTrials.gov.

Registration number: NCT00454558.

Keywords: Clinical study; Pulmonary hypertension; Riociguat; Soluble guanylate cyclase stimulator.

Publication types

  • Clinical Trial, Phase II
  • Multicenter Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aged
  • Antihypertensive Agents / administration & dosage
  • Antihypertensive Agents / pharmacology
  • Disease-Free Survival
  • Enzyme Activators / administration & dosage
  • Enzyme Activators / adverse effects
  • Enzyme Activators / pharmacology
  • Exercise / physiology
  • Female
  • Humans
  • Hypertension, Pulmonary / drug therapy*
  • Hypertension, Pulmonary / mortality
  • Male
  • Middle Aged
  • Pulmonary Embolism / complications
  • Pulmonary Embolism / drug therapy*
  • Pulmonary Embolism / mortality
  • Pyrazoles / administration & dosage*
  • Pyrazoles / adverse effects
  • Pyrazoles / pharmacology
  • Pyrimidines / administration & dosage*
  • Pyrimidines / adverse effects
  • Pyrimidines / pharmacology
  • Soluble Guanylyl Cyclase / metabolism
  • Treatment Outcome
  • Walk Test / statistics & numerical data

Substances

  • Antihypertensive Agents
  • Enzyme Activators
  • Pyrazoles
  • Pyrimidines
  • Soluble Guanylyl Cyclase
  • riociguat

Associated data

  • ClinicalTrials.gov/NCT00454558