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OPSUMIT® (macitentan) has a well-studied safety and tolerability profile

Adverse reactions in the SERAPHIN study1

Adverse reactions more frequent with OPSUMIT® 10 mg vs placebo by ≥3% OPSUMIT® 10 mg
(n=242)
Placebo
(n=249)
Anemia 13% 3%
Nasopharyngitis/pharyngitis 20% 13%
Bronchitis 12% 6%
Headache 14% 9%
Influenza 6% 2%
Urinary tract infection 9% 6%

The overall incidence of treatment discontinuations due to adverse events with OPSUMIT® (approximately 11%) was similar to placebo (approximately 12%)1,2

Additional adverse events of special interest1-3

  OPSUMIT® 10 mg
(n=242)
Placebo
(n=249)
Hypotension 7.0% 4.4%
Edema 21.9% 20.5%
Peripheral edema 18.2% 18.1%

Incidence of elevated aminotransferases/decreases in hemoglobin1,2

  OPSUMIT® 10 mg
(n=242)
Placebo
(n=249)
ALT/AST elevations >3 x ULN 3.4% 4.5%
ALT/AST elevations >8 x ULN 2.1% 0.4%
Patients with Hgb <10 g/dL 8.7% 3.4%

Drug-drug interactions1

MEDICATION EFFECT
Strong inducers of CYP3A4 (eg, rifampin)
  • Significantly reduce macitentan exposure
  • Concomitant use of OPSUMIT® with strong CYP3A4 inducers should be avoided
Strong inhibitors of CYP3A4 (eg, ketoconazole)
  • Approximately double macitentan exposure
  • Concomitant use of OPSUMIT® with strong CYP3A4 inhibitors should be avoided
  • Use other PAH treatment options when strong CYP3A4 inhibitors are needed as part of HIV treatment (eg, ritonavir)
Moderate dual inhibitors of CYP3A4 and CYP2C9 (eg, fluconazole and amiodarone)
  • Predicted to increase macitentan exposure
  • Concomitant use of OPSUMIT® with moderate dual inhibitors of CYP3A4 and CYP2C9 should be avoided
Combined moderate CYP3A4 inhibitor and moderate CYP2C9 inhibitor
  • Concomitant use of OPSUMIT® with both a moderate CYP3A4 inhibitor and moderate CYP2C9 inhibitor should be avoided

Postmarketing experience with OPSUMIT®1

Because these following adverse reactions are reported voluntarily during post-approval use of OPSUMIT® from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

  • Hypersensitivity reactions (angioedema, pruritus, and rash)
  • Flushing
  • Nasal congestion
  • Elevations of liver aminotransferases (ALT, AST) and liver injury; in most cases alternative causes could be identified (heart failure, hepatic congestion, autoimmune hepatitis). Endothelin receptor antagonists have been associated with elevations of aminotransferases, hepatotoxicity, and cases of liver failure
  • Edema/fluid retention. Cases of edema and fluid retention occurred within weeks of starting OPSUMIT®, some requiring intervention with a diuretic, fluid management, or hospitalization for decompensated heart failure
  • Symptomatic hypotension

Review the
REPAIR study

DISCOVER THE DATA

SERAPHIN PAH-related hospitalization results

View the Data

View SERAPHIN PAH-CTD subgroup data

See the Data

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ALT=alanine aminotransferase; AST=aspartate aminotransferase; CYP=cytochrome P450; Hgb=hemoglobin; HIV=human immunodeficiency virus; PAH=pulmonary arterial hypertension; SERAPHIN=Study with an Endothelin Receptor Antagonist in Pulmonary Arterial Hypertension to Improve CliNical Outcome; ULN=upper limit of normal.
References: 1. OPSUMIT® [prescribing information]. Actelion Pharmaceuticals US, Inc. 2. Pulido T, Adzerikho I, Channick RN, et al; SERAPHIN Investigators. Macitentan and morbidity and mortality in pulmonary arterial hypertension. N Engl J Med. 2013;369(9):809-818 and suppl 1-21. doi:10.1056/NEJMoa1213917 3. US Dept of Health and Human Services, US Food and Drug Administration, Center for Drug Evaluation and Research. Opsumit® (macitentan) NDA 204410. Accessed October 14, 2022. http://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/204410Orig1s000MedR.pdf

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