Treprostinil

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Treprostinil
Treprostinil.svg
Treprostinil2.png
Clinical data
Trade names Remodulin, Orenitram, Tyvaso, others
AHFS/Drugs.com Monograph
MedlinePlus a622038
License data
Pregnancy
category
  • AU:B3
Routes of
administration 		Subcutaneous, intravenous, inhalation, by mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability ~100%
Metabolism Substantially metabolized by the liver
Elimination half-life 4 hours
Excretion Urine (79% of administered dose is excreted as 4% unchanged drug and 64% as identified metabolites); feces (13%)
Identifiers
  • (1R,2R,3aS,9aS)-[[2,3,3a,4,9,9a-Hexahydro-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-1H-benz[f]inden-5-yl]oxy]acetic acid
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard 100.236.149 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C23H34O5
Molar mass 390.520 g·mol−1
  • InChI=1S/C23H34O5/c1-2-3-4-7-17(24)9-10-18-19-11-15-6-5-8-22(28-14-23(26)27)20(15)12-16(19)13-21(18)25/h5-6,8,16-19,21,24-25H,2-4,7,9-14H2,1H3,(H,26,27)/t16-,17-,18+,19-,21+/m0/s1 Yes check.svgY
  • Key:PAJMKGZZBBTTOY-ZFORQUDYSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

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. [7]

Contents

Treprostinil was approved for use in the United States in May 2002. [8]

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. [1]

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. [3] [4]

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

Common side effects depending on route of administration:

History

In 1976, the first paper on prostacyclin was published. [10]

Treprostinil (Remodulin) was approved for medical use in the United States in May 2002, [8] and again in July 2018. [11]

Treprostinil (Tyvaso), as inhalation solution, was approved for medical use in the United States in July 2009, [12] and again in April 2021. [13]

Treprostinil (Orenitram), as extended release tablets, was approved for medical use in the United States in December 2013. [14]

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. [15] [16]

Treprostinil (Yutrepia), as inhalation powder, was approved for medical use in the United States in June 2025. [5] [17] [18]

Research

Treprostinil therapy may be effective in treating Degos disease. [19]

References

  1. 1 2 "Remodulin- treprostinil injection, solution; Sterile diluent for remodulin- water injection, solution". DailyMed. 9 October 2023. Archived from the original on 21 May 2024. Retrieved 21 May 2024.
  2. ↑ "Orenitram- treprostinil tablet, extended release; Orenitram- treprostinil kit". DailyMed. 7 November 2023. Archived from the original on 21 May 2024. Retrieved 21 May 2024.
  3. 1 2 "Tyvaso- treprostinil inhalant". DailyMed. 8 December 2023. Retrieved 21 May 2024.
  4. 1 2 "Tyvaso DPI- treprostinil inhalant; Tyvaso DPI- treprostinil kit". DailyMed. 26 January 2024. Archived from the original on 21 May 2024. Retrieved 21 May 2024.
  5. 1 2 "Yutrepia- treprostinil capsule". DailyMed. 2 June 2025. Retrieved 6 July 2025.
  6. 1 2 3 4 5 6 "Trepulmix EPAR". European Medicines Agency (EMA). 29 January 2020. Archived from the original on 3 August 2020. Retrieved 9 April 2020. Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  7. ↑ Torres F, Rubin LJ (January 2013). "Treprostinil for the treatment of pulmonary arterial hypertension". Expert Review of Cardiovascular Therapy. 11 (1): 13–25. doi:10.1586/erc.12.160. PMID   23259441. S2CID   29661141.
  8. 1 2 "Drug Approval Package: Remodulin (Treprostinil Sodium) NDA #021272". U.S. Food and Drug Administration (FDA). 31 July 2002. Archived from the original on 12 March 2020. Retrieved 9 April 2020.
  9. 1 2 3 Kumar P, Thudium E, Laliberte K, Zaccardelli D, Nelsen A (December 2016). "A Comprehensive Review of Treprostinil Pharmacokinetics via Four Routes of Administration". Clinical Pharmacokinetics. 55 (12): 1495–1505. doi:10.1007/s40262-016-0409-0. PMC   5107196 . PMID   27286723.
  10. ↑ Moncada S, Gryglewski R, Bunting S, Vane JR (October 1976). "An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation". Nature. 263 (5579): 663–665. Bibcode:1976Natur.263..663M. doi:10.1038/263663a0. PMID   802670. S2CID   4279030.
  11. ↑ "Drug Approval Package: Remodulin". U.S. Food and Drug Administration (FDA). 7 February 2019. Archived from the original on 29 March 2021. Retrieved 9 April 2020.
  12. ↑ "Drug Approval Package: Tyvaso (Treprostinil) Inhalation Solution NDA #022387". U.S. Food and Drug Administration (FDA). 27 September 2017. Archived from the original on 31 March 2021. Retrieved 9 April 2020.
  13. ↑ "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.
  14. ↑ "Drug Approval Package: Orenitram (Treprostinil) Extended Release Tablets NDA #203496". U.S. Food and Drug Administration (FDA). 23 July 2014. Archived from the original on 14 August 2020. Retrieved 9 April 2020.
  15. ↑ "Drug Approval Package: Tyvaso DPI". U.S. Food and Drug Administration (FDA). 6 July 2022. Archived from the original on 28 September 2024. Retrieved 20 June 2025.
  16. ↑ "United Therapeutics Announces FDA Approval of Tyvaso DPI" (Press release). United Therapeutics. 24 May 2022. Retrieved 20 June 2025– via Business Wire.
  17. ↑ "Letter to Kristan Amicone about NDA Approval for Yutrepia" (PDF). www.accessdata.fda.gov. 23 May 2025.
  18. ↑ "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.
  19. ↑ Shapiro LS, Toledo-Garcia AE, Farrell JF (April 2013). "Effective treatment of malignant atrophic papulosis (Köhlmeier-Degos disease) with treprostinil--early experience". Orphanet Journal of Rare Diseases. 8: 52. doi: 10.1186/1750-1172-8-52 . PMC   3636001 . PMID   23557362.

Further reading

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