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In the treatment of pulmonary arterial hypertension (PAH, WHO Group I)

Create a foundation based on clinical results

Start with OPSUMIT to reduce the risk of disease progression in PAH1,2

OPSUMIT is the only ERA approved to reduce the risks of disease progression and PAH-related hospitalization as both monotherapy AND in combination with PDE-5is or inhaled prostanoids* in PAH (WHO Group I) patients with FC II and III symptoms.1

*OPSUMIT is approved in combination with PDE-5is or inhaled prostanoids, but not oral prostanoids.

Expert guidelines and recommendations for OPSUMIT

OPSUMIT added to sildenafil received the highest class recommendation (Class I, Level B) in PAH (WHO Group I) FC II-III patients for sequential combination therapy from the 2015 Guidelines of the European Society of Cardiology (ESC) and European Respiratory Society (ERS).2 Several other therapies also received a Class I, Level B recommendation in FC II-III patients.

Classes of recommendations

Class
Definition
Class I
Evidence and/or general agreement that a given treatment or procedure is beneficial, useful, and effective
Class II
Conflicting evidence and/or a divergence of opinion about the usefulness/efficacy of the given treatment or procedure
Class IIa
Weight of evidence/opinion is in favor of usefulness/efficacy
Class IIb
Usefulness/efficacy is less well established by evidence/opinion
Class III
Evidence or general agreement that the given treatment or procedure is not useful/effective, and in some cases may be harmful

Levels of evidence

Level
Definition
A
Data derived from multiple randomized clinical trials or meta-analyses
B
Data derived from a single randomized clinical trial or large nonrandomized studies
C
Consensus of opinion of the experts and/or small studies, retrospective studies, or registries

Adapted from Eur Resp J. 2015;46:903-975.

SERAPHIN: The largest long-term, outcomes-based pivotal trial of an ERA in PAH

The effect of OPSUMIT on disease progression in patients with PAH (WHO Group I) was studied in SERAPHIN, a large (N=742), event-driven, multicenter, long-term (average treatment duration 2 years), phase 3 trial. At study baseline, 36% of patients were not using PAH-specific background therapy and 64% were using background therapy with PDE-5is or inhaled/oral prostanoids.1†

Trial demographics:

  • Patients had predominantly WHO FC II-III symptoms

  • Etiologies included IPAH/HPAH (57%), PAH-CTD (31%), PAH-CHD with repaired shunts (8%), PAH associated with drugs and toxins (3%), and PAH-HIV (1%)

  • Mean patient age was 46 years, and 77% of patients were female

  • 25% of patients were recently diagnosed (<6 months) and 75% were previously diagnosed (≥6 months)3

OPSUMIT is approved in combination with PDE-5is or inhaled prostanoids, but not oral prostanoids.

Well-established experience

More than 22,000 patients have been prescribed OPSUMIT in the US since its approval in 2013.3‡

As of April 2018.

ERA=endothelin receptor antagonist; FC=functional class; HPAH=heritable PAH; IPAH=idiopathic PAH; PAH-CHD=PAH associated with congenital heart disease; PAH-CTD=PAH associated with connective tissue disorders; PAH-HIV=PAH associated with human immunodeficiency virus; PDE-5i=phosphodiesterase type 5 inhibitor; SERAPHIN=Study with an Endothelin Receptor Antagonist in Pulmonary Arterial Hypertension to Improve CliNical Outcome; WHO=World Health Organization.

References: 1. OPSUMIT [prescribing information]. South San Francisco, CA: Actelion Pharmaceuticals US, Inc. 2. Galiè N, Humbert M, Vachiery J-L, et al. 2015 ESC/ERS Guidelines for the diagnosis and treatment of pulmonary hypertension: Eur Respir J. 2015;46(4):903-975. 3. Data on file, Actelion Pharmaceuticals.

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IMPORTANT SAFETY INFORMATION

BOXED WARNING: EMBRYO-FETAL TOXICITY

  • Do not administer OPSUMIT to a pregnant female because it may cause fetal harm.
  • Females of reproductive potential: Exclude pregnancy before the start of treatment, monthly during treatment, and 1 month after stopping treatment. Prevent pregnancy during treatment and for one month after stopping treatment by using acceptable methods of contraception.
  • For all female patients, OPSUMIT is available only through a restricted program called the OPSUMIT Risk Evaluation and Mitigation Strategy (REMS).

INDICATION

OPSUMIT is an endothelin receptor antagonist (ERA) indicated for the treatment of pulmonary arterial hypertension (PAH, WHO Group I) to reduce the risks of disease progression and hospitalization for PAH.

Effectiveness was established in a long-term study in PAH patients with predominantly WHO Functional Class II-III symptoms treated for an average of 2 years. Patients had idiopathic and heritable PAH (57%), PAH caused by connective tissue disorders (31%), and PAH caused by congenital heart disease with repaired shunts (8%).

CONTRAINDICATIONS

Pregnancy: OPSUMIT may cause fetal harm when administered to a pregnant woman. OPSUMIT is contraindicated in females who are pregnant. If OPSUMIT is used during pregnancy, advise the patient of the potential risk to a fetus.

WARNINGS AND PRECAUTIONS

Embryo-fetal Toxicity and OPSUMIT REMS Program

Due to the risk of embryo-fetal toxicity, OPSUMIT is available for females only through a restricted program called the OPSUMIT REMS Program. For females of reproductive potential, exclude pregnancy prior to initiation of therapy, ensure use of acceptable contraceptive methods, and obtain monthly pregnancy tests.

Notable requirements of the OPSUMIT REMS Program include:

Hepatotoxicity

Fluid Retention

Hemoglobin Decrease

Pulmonary Edema with Pulmonary Veno-occlusive Disease (PVOD)

Should signs of pulmonary edema occur, consider the possibility of associated PVOD. If confirmed, discontinue OPSUMIT.

Decreased Sperm Counts

OPSUMIT, like other ERAs, may have an adverse effect on spermatogenesis. Counsel men about potential effects on fertility.

ADVERSE REACTIONS

Most common adverse reactions (more frequent than placebo by ≥3%) were anemia (13% vs 3%), nasopharyngitis/pharyngitis (20% vs 13%), bronchitis (12% vs 6%), headache (14% vs 9%), influenza (6% vs 2%), and urinary tract infection (9% vs 6%).

DRUG INTERACTIONS

Please see accompanying full Prescribing Information, including BOXED WARNING for embryo-fetal toxicity.