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OPSUMIT®

(macitentan)

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This information is intended for US healthcare professionals to access current scientific information about J&J Innovative Medicine products. It is prepared by Medical Information and is not intended for promotional purposes, nor to provide medical advice.

OPSUMIT® (macitentan)

Medical Information

OPSUMIT – Pharmaceutical Research to Develop an Intravenous Formulation

Last Updated: 09/22/2025

SUMMARY

  • OPSUMIT is currently available in the United States (US) as a 10 mg film-coated tablet for oral administration.1,2 
  • Poor aqueous solubility and stability presented barriers to designing a macitentan intravenous (IV) formulation.3,4 

CLINICAL DATA

Development of Macitentan Intravenous Formulation

OPSUMIT is currently available in the US as a 10 mg film-coated tablet for oral administration.1,2 Poor aqueous solubility and stability presented barriers to designing a macitentan IV formulation.4Macitentan is insoluble in water and aqueous media with pH in the range of 1.2 to 9.3,5Macitentan is sensitive to hydrolysis of the sulfamide group, which leads to poor stability in liquid state.6 Photostability testing found degradation of the active substance, macitentan, was observed in solution in all solvents tested.3 As macitentan has very low solubility (≤1 mcg/mL) and poor stability in aqueous media at physiological pH, attempts to develop an IV formulation for human use had failed despite exploration of several potential solvent systems.4,6Subsequently, an absolute bioavailability study for macitentan was not carried out because the chemical instability of macitentan presented obstacles to the development of an IV formulation.4,7 

Literature Search

A literature search of MEDLINE®, EMBASE®, BIOSIS Previews®, DERWENT® (and/or other resources, including internal/external databases) was conducted on 17 September 2025.

References

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1 US Food and Drug Administration (FDA). New Drug Application (NDA) Number 204410: OPSUMIT (macitentan). US Food and Drug Administration (FDA); https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=204410 Accessed September 17, 2025.  
2 OPSUMIT (macitentan) [Prescribing Information]. Titusville, NJ: Actelion Pharmaceuticals US, Inc.; https://www.janssenlabels.com/package-insert/product-monograph/prescribing-information/OPSUMIT-pi.pdf
3 European Medicines Agency (EMA). EMA Assessment Report for Opsumit. October 2013. European Medicines Agency (EMA); 2013. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/002697/WC500160900.pdf
4 Therapeutic Goods Administration (TGA). Australian Public Assessment Report for macitentan. Australian Government Therapeutic Goods Administration (TGA); 2014. https://www.tga.gov.au/sites/default/files/auspar-macitentan-140428.pdf
5 US Food and Drug Administration (FDA). Opsumit FDA Drug Approval Package - Clinical Pharmacology and Biopharmaceutics Review. US Food and Drug Administration (FDA); 2013. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/204410Orig1s000ClinPharmR.pdf Accessed September 17, 2025.  
6 Therapeutic Goods Administration (TGA). Australian Public Assessment Report Attachment 2: Extract from the Clinical Evaluation Report (AusPAR-CER) for macitentan. Australian Government Therapeutic Goods Administration (TGA); 2013.  
7 Kanter R de, Sidharta PN, Delahaye S, et al. Physiologically-Based Pharmacokinetic Modeling of Macitentan: Prediction of Drug–Drug Interactions. Clin Pharmacokinet. 2016;55(3):369-380.