Chemistry:Treprostinil

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Treprostinil, sold under the brand names Remodulin for infusion, Orenitram for oral, and Tyvaso for inhalation among others, is a vasodilator that is used for the treatment of pulmonary arterial hypertension.[1]

Treprostinil was approved for use in the United States in May 2002.[2]

Medical uses

Treprostinil is indicated for the treatment of pulmonary arterial hypertension in people with NYHA Class II-IV symptoms to diminish symptoms associated with exercise.[3]

Treprostinil inhalation solution and treprostinil inhalation powder are indicated for the treatment of people with pulmonary arterial hypertension (WHO Group 1) to improve exercise ability; and people with pulmonary hypertension associated with interstitial lung disease (WHO Group 3) to improve exercise ability.[4][5]

In the European Union, treprostinil (Trepulmix) is indicated for the treatment of adults with WHO Functional Class III or IV and inoperable chronic thromboembolic pulmonary hypertension;[6] or persistent or recurrent chronic thromboembolic pulmonary hypertension after surgical treatment to improve exercise capacity.[6]

Adverse effects

  • Since treprostinil is a vasodilator, its antihypertensive effect may be compounded by other medications that affect the blood pressure, including calcium channel blockers, diuretics, and other vasodilating agents.[7]
  • Because of treprostinil's inhibiting effect on platelet aggregation, there is an increased risk of bleeding, especially among patients who are also taking anticoagulants.[7]

Common side effects depending on route of administration:

  • 85% of patients report pain or other reaction at the infusion site.[7]

History

In 1976, the first paper on prostacyclin was published.[8]

Treprostinil (Remodulin) was approved for medical use in the United States in May 2002,[2] and again in July 2018.[9]

Treprostinil (Tyvaso), as inhalation solution, was approved for medical use in the United States in July 2009,[10] and again in April 2021.[11]

Treprostinil (Orenitram), as extended release tablets, was approved for medical use in the United States in December 2013.[12]

Treprostinil (Trepulmix) was authorized for medical use in the European Union in April 2020.[6] Trepulmix is a hybrid medicine that is similar to the reference medicine Remodulin.[6] It contains the same active substance, but it is used for treating a different form of pulmonary hypertension.[6]

Treprostinil (Tyvaso DPI), as inhalation powder, was approved for medical use in the United States in May 2022.[13][14]

Treprostinil (Yutrepia), as inhalation powder, was approved for medical use in the United States in June 2025.[15][16][17]

Research

Treprostinil therapy may be effective in treating Degos disease.[18]

References

  1. ↑ "Treprostinil for the treatment of pulmonary arterial hypertension". Expert Review of Cardiovascular Therapy 11 (1): 13–25. January 2013. doi:10.1586/erc.12.160. PMID 23259441. 
  2. ↑ 2.0 2.1 "Drug Approval Package: Remodulin (Treprostinil Sodium) NDA #021272". 31 July 2002. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/21-272_Remodulin.cfm. 
  3. ↑ Cite error: Invalid <ref> tag; no text was provided for refs named Remodulin FDA label
  4. ↑ Cite error: Invalid <ref> tag; no text was provided for refs named Tyvaso FDA label
  5. ↑ Cite error: Invalid <ref> tag; no text was provided for refs named Tyvaso DPI FDA label
  6. ↑ 6.0 6.1 6.2 6.3 6.4 "Trepulmix EPAR". 29 January 2020. https://www.ema.europa.eu/en/medicines/human/EPAR/trepulmix.  Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  7. ↑ 7.0 7.1 7.2 "A Comprehensive Review of Treprostinil Pharmacokinetics via Four Routes of Administration". Clinical Pharmacokinetics 55 (12): 1495–1505. December 2016. doi:10.1007/s40262-016-0409-0. PMID 27286723. 
  8. ↑ "An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation". Nature 263 (5579): 663–665. October 1976. doi:10.1038/263663a0. PMID 802670. Bibcode: 1976Natur.263..663M. 
  9. ↑ "Drug Approval Package: Remodulin". 7 February 2019. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208276Orig1s000TOC.cfm. 
  10. ↑ "Drug Approval Package: Tyvaso (Treprostinil) Inhalation Solution NDA #022387". 27 September 2017. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022387s000TOC.cfm. 
  11. ↑ "United Therapeutics Announces FDA Approval and Launch of Tyvaso for the Treatment of Pulmonary Hypertension Associated with Interstitial Lung Disease" (Press release). United Therapeutics. 1 April 2021. Retrieved 20 June 2025 – via PR Newswire.
  12. ↑ "Drug Approval Package: Orenitram (Treprostinil) Extended Release Tablets NDA #203496". 23 July 2014. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/203496Orig1s000TOC.cfm. 
  13. ↑ "Drug Approval Package: Tyvaso DPI". 6 July 2022. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214324Orig1s000TOC.cfm. 
  14. ↑ "United Therapeutics Announces FDA Approval of Tyvaso DPI" (Press release). United Therapeutics. 24 May 2022. Retrieved 20 June 2025 – via Business Wire.
  15. ↑ Cite error: Invalid <ref> tag; no text was provided for refs named Yutrepia FDA label
  16. ↑ "Letter to Kristan Amicone about NDA Approval for Yutrepia". 2025-05-23. https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2025/213005Orig1s000ltr.pdf. 
  17. ↑ "U.S. FDA Approves Liquidia's Yutrepia (treprostinil) Inhalation Powder for Patients with Pulmonary Arterial Hypertension (PAH) and Pulmonary Hypertension Associated with Interstitial Lung Disease (PH-ILD)" (Press release). Liquidia Technologies. 23 May 2025. Archived from the original on 24 May 2025. Retrieved 25 May 2025 – via GlobeNewswire.
  18. ↑ "Effective treatment of malignant atrophic papulosis (Köhlmeier-Degos disease) with treprostinil--early experience". Orphanet Journal of Rare Diseases 8: 52. April 2013. doi:10.1186/1750-1172-8-52. PMID 23557362. 

Further reading

  • "Cost-minimization analysis of treprostinil vs. epoprostenol as an alternate to oral therapy non-responders for the treatment of pulmonary arterial hypertension". Current Medical Research and Opinion 21 (12): 2007–2016. December 2005. doi:10.1185/030079905X75104. PMID 16368052.