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Safety and Efficacy of APD811 in Pulmonary Arterial Hypertension

Phase 2
Completed
Conditions
Pulmonary Arterial Hypertension
Interventions
Drug: Placebo
Registration Number
NCT02279160
Lead Sponsor
United Therapeutics
Brief Summary

The study was conducted as a placebo-controlled, randomized, 22-week double-blind study which included a dose titration period. An additional transition period occurred for those patients who elected to enroll into the open-label extension study, APD811-007. A total of 61 patients with PAH were enrolled.

Detailed Description

Study APD811-003 was a 22-week, randomized, double-blind, parallel-group, placebo-controlled study in subjects with symptomatic WHO Group 1 PAH. The study consisted of a dose titration period of up to 9 weeks, a 13-week maintenance period, and a follow-up visit that was to occur approximately 3 weeks after the end of the maintenance period (Week 25). The transition period of 3 weeks (±1 week) was to occur for those subjects who elected to enroll into the open-label extension (OLE) Study APD811-007.

Approximately 60 subjects with PAH were planned to be enrolled (61 actual). After screening, eligible subjects were randomized 2:1 to ralinepag (APD811) or to placebo. Randomization was stratified by baseline WHO/NYHA functional class (II versus III or IV). Subjects randomized to active therapy were given ralinepag at a starting dose of 0.01 mg BID. Subjects randomized to the placebo arm received matching placebo capsules to preserve the blind. Subjects were instructed to take the study drug (ralinepag or placebo) with food. Dosage was then uptitrated, as tolerated, over the course of the 9-week dose-titration period to a maximum dose of 0.3 mg BID. Although doses could be reduced based on tolerability, the final dosage reached was required to be stable during the 13-week treatment period prior to evaluation at Week 22.

Subjects could receive concomitant oral disease-specific PAH therapy consisting of an ERA and/or an agent acting on the nitric oxide pathway, a PDE-5 inhibitor or a sGC stimulator, provided the dose had remained stable for at least 3 months prior to the start of screening. It was recommended that subjects continue the same dose and regimen of these medications for the duration of the study. With the exception of prostanoids, the use of other supporting therapies, which may affect PAH, was also permitted.

During the study, assessments of efficacy were performed including PVR and other hemodynamic parameters as determined by RHC, the 6MWT, assessment of clinical worsening, BNP and NT-proBNP levels, WHO/NYHA functional class assessment of PAH. Safety assessments included standard evaluations of AEs, clinical laboratory values, vital signs, and ECG measurements.

At the end of the maintenance period, subjects who did not choose to participate in the OLE study were to discontinue study drug (ralinepag or placebo). All subjects that chose to continue in the OLE study were to remain on study drug until the follow-up visit at Week 25. This visit served as the baseline visit for the OLE study if the subject was eligible and chose to participate.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
61
Inclusion Criteria
  • Males or females aged 18-75 years, inclusive

  • Symptomatic WHO Group 1 PAH classified by one of the following subgroups:

    • Idiopathic pulmonary arterial hypertension (IPAH);
    • Heritable pulmonary arterial hypertension (HPAH);
    • Drugs and toxins induced;
    • Associated pulmonary arterial hypertension (APAH); specifically connective tissue diseases, HIV infection and congenital heart disease.
  • Has had the diagnosis of PAH confirmed by cardiac catheterization

  • Has WHO/NYHA functional class II- IV symptomatology

  • Previously diagnosed with PAH and on stable oral disease-specific PAH therapy with either an ERA and/or an agent acting on the nitric oxide pathway, i.e. a PDE5 inhibitor or a soluble guanylate cyclase stimulator. Stable is defined as no change in dose within 3 months of the start of Screening and for the duration of the study

  • Has 6MWT distances of 100-500 m, and within 15% of each other on 2 consecutive tests done on different days at Screening

  • Has pulmonary function tests (PFTs) within 6 months prior to the start of Screening with no evidence of significant parenchymal lung disease

  • Has a ventilation-perfusion (V/Q) lung scan or pulmonary angiogram within 5 years prior to Screening and concomitant with or following diagnosis of PAH that shows no evidence of thromboembolic disease

  • If on vasodilators (including calcium channel blockers), digoxin, spironolactone, or L-Arginine supplementation; the patient must be on a stable dose for at least 1 month prior to the start of Screening

Exclusion Criteria
  • Newly diagnosed with PAH and on no disease-specific PAH therapy
  • Previous participation in any clinical study with an investigational drug, biologic, or device within 2 months prior to the Screening visit
  • Acutely decompensated heart failure within 1 month prior to start of Screening
  • Systolic blood pressure <90 mm Hg at Screening
  • Evidence or history of left-sided heart disease and/or clinically significant cardiac disease
  • Use or chronic administration (defined as >30 days) of a prostacyclin or prostacyclin analogue within 3 months of Screening
  • Any previous use of a prostacyclin or prostacyclin analogue that was stopped for safety or tolerability issues associated with pharmacology/mechanism of action
  • Other severe acute or chronic medical or laboratory abnormality that may increase the risk associated with study participation or investigational product administration or may interfere with the interpretation of study results and, in the judgment of the investigator, would make the patient inappropriate for entry into this study

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
APD811APD811Multiple dose titration to maximum tolerated dose.
PlaceboPlaceboMultiple dose titration to maximum tolerated dose.
Primary Outcome Measures
NameTimeMethod
Change From Baseline in Pulmonary Vascular Resistance (PVR)Baseline and 22 Weeks

Measurements of PVR from right heart catheterization were obtained prior to Day 1 of the dose titration period and at the end of the maintenance period (Week 22), approximately 4 hours after the last dose of study drug.

Change From Baseline in 6-minute Walk Distance (6MWD) in Patients With PAHBaseline and 22 Weeks

The 6MWT was conducted according to the modified guidelines issued by the American Thoracic Society prior to Day 1 of the dose titration period and at the end of the maintenance period (Week 22).

Secondary Outcome Measures
NameTimeMethod

Trial Locations

Locations (34)

UT Southwestern

🇺🇸

Dallas, Texas, United States

Boston University Medical Center

🇺🇸

Boston, Massachusetts, United States

University of Cincinnati

🇺🇸

Cincinnati, Ohio, United States

Ohio State University Medical Center

🇺🇸

Columbus, Ohio, United States

University of Pittsburg Medical Center

🇺🇸

Pittsburgh, Pennsylvania, United States

University of Texas, Houston Center for Clinical and Translational Sciences

🇺🇸

Houston, Texas, United States

Klinički Centar Srbije (KCS), Klinika za kardiologiju

🇷🇸

Belgrade, Serbia

Krakowski Szpital Specjalistyczny im. Jana Pawła II w Krakowie

🇵🇱

Krakow, Poland

Многопрофилна болница за активно лечение "Света Анна" София АД, Клиника по кардиология

🇧🇬

Sofia, Bulgaria

University of Iowa Hospitals and Clinics

🇺🇸

Iowa City, Iowa, United States

Royal Hobart Hospital

🇦🇺

Hobart, Australia

Fiona Stanley Hospital

🇦🇺

Murdoch, Australia

Cedars-Sinai Medical Center

🇺🇸

Los Angeles, California, United States

University of Maryland

🇺🇸

Baltimore, Maryland, United States

Semmelweis Egyetem Pulmonológiai Klinika

🇭🇺

Budapest, Hungary

Pécsi Tudományegyetem Klinikai Központ, Szívgyógyászati Klinika

🇭🇺

Pecs, Hungary

Uniwersytecki Szpital Kliniczny w Białymstoku

🇵🇱

Bialystok, Poland

University of Alabama at Birmingham

🇺🇸

Birmingham, Alabama, United States

UC Davis Medical Center

🇺🇸

Sacramento, California, United States

"Многопрофилната болница за активно лечение "Национална кардиологична болница "" ЕАД

🇧🇬

Sofia, Bulgaria

II. interní klinika - klinika kardiologie a angiologie, 1. lékařská fakulta, Univerzita Karlova v Praze a Všeobecná fakultní nemocnice v Praze

🇨🇿

Prague, Czechia

Kliničko-bolnički centar (KBC) Zemun,Klinika za internu medicinu,Sluzba kardiologije

🇷🇸

Belgrade, Serbia

Hospital Clinic de Barcelona, Departamento de Pneumologia

🇪🇸

Barcelona, Spain

Institutul de Urgență pentru Boli Cardiovasculare, Secția Clinică Cardiologie III

🇷🇴

Bucharest, Romania

Hospital 12 de Octubre, Departamento de Cardiologia

🇪🇸

Madrid, Spain

St Vincent's Hospital

🇦🇺

Fitzroy, Australia

UCLA Medical Center

🇺🇸

Torrance, California, United States

Institutul de Pneumoftiziologie "Marius Nasta", Secția Clinică Pneumoftiziologie IV

🇷🇴

Bucharest, Romania

Hospital Universitari General Vall d'Hebron, Servicio de Neumología

🇪🇸

Barcelona, Spain

The Prince Charles Hospital

🇦🇺

Chermside, Australia

Wojewódzki Szpital Specjalistyczny im. W. Biegańskiego w Łodzi

🇵🇱

Lodz, Poland

Spitalul Clinic de Boli Infectioase si Pneumoftiziologie, Sectia Clinica Pneumologie II

🇷🇴

Timisoara, Romania

Institut za plućne bolesti Vojvodine Sremska Kamenica (IPBVSK),

🇷🇸

Sremska Kamenica, Serbia

Gottsegen György Országos Kardiologiai Intézet, Felnőtt Kardiológia

🇭🇺

Budapest, Hungary

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