Treprostinil

Overview

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] WP

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

Uses, dosage and effects

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] WP

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] WP

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; or persistent or recurrent chronic thromboembolic pulmonary hypertension after surgical treatment to improve exercise capacity.[6] WP

Risks and side effects

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] WP
• 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] WP

Common side effects depending on route of administration: WP

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

Research

Research

Treprostinil therapy may be effective in treating Degos disease.[8] WP

History

History

In 1976, the first paper on prostacyclin was published.[9] WP

Treprostinil (Remodulin) was approved for medical use in the United States in May 2002, and again in July 2018.[2][10] WP

Treprostinil (Tyvaso), as inhalation solution, was approved for medical use in the United States in July 2009, and again in April 2021.[11][12] WP

Treprostinil (Orenitram), as extended release tablets, was approved for medical use in the United States in December 2013.[13] WP

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

Treprostinil (Tyvaso DPI), as inhalation powder, was approved for medical use in the United States in May 2022.[14][15] WP

Treprostinil (Yutrepia), as inhalation powder, was approved for medical use in the United States in June 2025.[16][17][18] WP

Chemistry

Formula

C23H34O5 PC

CAS number

81846-19-7 PC

Molar mass (g/mol)

390.5 PC

IUPAC name (computed by PubChem)

2-[[(1R,2R,3aS,9aS)-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[g]naphthalen-5-yl]oxy]acetic acid PC

SMILES

CCCCC[C@@H](CC[C@H]1[C@@H](C[C@H]2[C@@H]1CC3=C(C2)C(=CC=C3)OCC(=O)O)O)O PC

InChIKey

PAJMKGZZBBTTOY-ZFORQUDYSA-N PC

PubChem CID

6918140

Harm reduction information

No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.

User reports

Pop culture

No references added yet.

Sources

1. Journal / agency Torres F, Rubin LJ. Treprostinil for the treatment of pulmonary arterial hypertension. Expert Review of Cardiovascular Therapy. January 2013. doi:10.1586/erc.12.160 · PMID 23259441
2. Journal / agency Drug Approval Package: Remodulin (Treprostinil Sodium) NDA #021272. 31 July 2002
3. Journal / agency Remodulin- treprostinil injection, solution; Sterile diluent for remodulin- water injection, solution. 9 October 2023
4. Journal / agency Tyvaso- treprostinil inhalant. 8 December 2023
5. Journal / agency Tyvaso DPI- treprostinil inhalant; Tyvaso DPI- treprostinil kit. 26 January 2024
6. Journal / agency Trepulmix EPAR. 29 January 2020
7. Journal / agency Kumar P, Thudium E, Laliberte K, Zaccardelli D, Nelsen A. A Comprehensive Review of Treprostinil Pharmacokinetics via Four Routes of Administration. Clinical Pharmacokinetics. December 2016. doi:10.1007/s40262-016-0409-0 · PMID 27286723 · PMC5107196
8. Journal / agency Shapiro LS, Toledo-Garcia AE, Farrell JF. Effective treatment of malignant atrophic papulosis (Köhlmeier-Degos disease) with treprostinil--early experience. Orphanet Journal of Rare Diseases. April 2013. doi:10.1186/1750-1172-8-52 · PMID 23557362 · PMC3636001
9. Journal / agency Moncada S, Gryglewski R, Bunting S, Vane JR. An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation. Nature. October 1976. doi:10.1038/263663a0 · PMID 802670
10. Journal / agency Drug Approval Package: Remodulin. 7 February 2019
11. Journal / agency Drug Approval Package: Tyvaso (Treprostinil) Inhalation Solution NDA #022387. 27 September 2017
12. Other United Therapeutics Announces FDA Approval and Launch of Tyvaso for the Treatment of Pulmonary Hypertension Associated with Interstitial Lung Disease. 1 April 2021
13. Journal / agency Drug Approval Package: Orenitram (Treprostinil) Extended Release Tablets NDA #203496. 23 July 2014
14. Journal / agency Drug Approval Package: Tyvaso DPI. 6 July 2022
15. Other United Therapeutics Announces FDA Approval of Tyvaso DPI. 24 May 2022
16. Journal / agency Yutrepia- treprostinil capsule. 2 June 2025
17. Journal / agency Letter to Kristan Amicone about NDA Approval for Yutrepia. 2025-05-23
18. Other 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). 23 May 2025

Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.