Treprostinil, sold under the brand names Remodulin for infusion, Orenitram for oral, and Tyvaso for inhalation, is a

vasodilator Vasodilation, also known as vasorelaxation, is the widening of blood vessels. It results from relaxation of smooth muscle cells within the vessel walls, in particular in the large veins, large arteries, and smaller arterioles. Blood vessel wal ...

that is used for the treatment of

pulmonary arterial hypertension Pulmonary arterial hypertension (PAH) is a syndrome in which the blood pressure in the pulmonary arteries and pulmonary arterioles (the blood vessels located proximal to the capillary bed, the site of oxygen exchange in the lungs) is elevated. T ...

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

Medical uses

Treprostinil is

indicated In medicine, an indication is a valid reason to use a certain test, medication, procedure, or surgery. There can be multiple indications to use a procedure or medication. An indication can commonly be confused with the term diagnosis. A diagnosis ...

for the treatment of

in people with NYHA Class II-IV symptoms to diminish symptoms associated with exercise. In 2022, the

FDA The United States Food and Drug Administration (FDA or US FDA) is a federal agency of the Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food ...

approved Tyvaso DPI (treprostinil) inhalation powder for patients with

(PAH) and

pulmonary hypertension Pulmonary hypertension (PH or PHTN) is a condition of increased blood pressure in the pulmonary artery, arteries of the lungs. Symptoms include dypsnea, shortness of breath, Syncope (medicine), fainting, tiredness, chest pain, pedal edema, swell ...

associated with interstitial lung disease (PH-ILD).

Administration

For infusion

Treprostinil may be administered as a continuous subcutaneous infusion or continuous intravenous infusion.

Inhaled form

The inhaled form of treprostinil was approved by the FDA in July 2009, and is sold under the brand name Tyvaso.

Oral form

The oral form of treprostinil was approved by the FDA in December 2013, and is sold under the brand name Orenitram.

History

{{main, Prostacyclin#History During the 1960s a UK research team, headed by Professor

John Vane Sir John Robert Vane (29 March 1927 – 19 November 2004) was a British pharmacologist who was instrumental in the understanding of how aspirin produces pain-relief and anti-inflammatory effects and his work led to new treatments for heart ...

began to explore the role of

prostaglandin Prostaglandins (PG) are a group of physiology, physiologically active lipid compounds called eicosanoids that have diverse hormone-like effects in animals. Prostaglandins have been found in almost every Tissue (biology), tissue in humans and ot ...

s in

anaphylaxis Anaphylaxis (Greek: 'up' + 'guarding') is a serious, potentially fatal allergic reaction and medical emergency that is rapid in onset and requires immediate medical attention regardless of the use of emergency medication on site. It typicall ...

and respiratory diseases. Working with a team from the Royal College of Surgeons, Vane discovered that aspirin and other oral anti-inflammatory drugs worked by inhibiting the synthesis of prostaglandins. This finding opened the door to a broader understanding of the role of prostaglandins in the body. Vane and a team from the

Wellcome Foundation The Wellcome Trust is a charitable foundation focused on health research based in London, United Kingdom. It was established in 1936 with legacies from the pharmaceutical magnate Henry Wellcome (founder of Burroughs Wellcome, one of the predeces ...

had identified a lipid mediator they called “PG-X,” which inhibited platelet aggregation. PG-X, which later would become known as prostacyclin, was 30 times more potent than any other known anti-aggregatory agent.{{citation needed, date=December 2015 By 1976, Vane and fellow researcher

Salvador Moncada Sir Salvador Enrique Moncada Seidner (born 3 December 1944) is a Honduran-British pharmacologist and professor. He is currently Research Domain Director for Cancer at the University of Manchester. In the past, he was the Research Director of ...

published the first paper on prostacyclin, in the scientific journal ''Nature''.{{cite journal , vauthors = Moncada S, Gryglewski R, Bunting S, Vane JR , title = An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation , journal = Nature , volume = 263 , issue = 5579 , pages = 663–665 , date = October 1976 , pmid = 802670 , doi = 10.1038/263663a0 , s2cid = 4279030 , bibcode = 1976Natur.263..663M Treprostinil (Remodulin) was approved for use in the United States in May 2002, and again in July 2018. Tyvaso, the inhaled form of treprostinil, was approved for use in the United States in July 2009. Orenitram was approved in December 2013.{{cite web , title=Drug Approval Package: Orenitram (Treprostinil) Extended Release Tablets NDA #203496 , website=U.S.

Food and Drug Administration The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is respo ...

(FDA) , date=24 December 1999 , url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/2013/203496Orig1s000TOC.cfm , access-date=9 April 2020 Treprostinil (Trepulmix) was approved for use in the European Union in April 2020.{{cite web , title=Trepulmix EPAR , website=

European Medicines Agency The European Medicines Agency (EMA) is an agency of the European Union (EU) in charge of the evaluation and supervision of pharmaceutical products. Prior to 2004, it was known as the European Agency for the Evaluation of Medicinal Products ...

(EMA) , date=29 January 2020 , url=https://www.ema.europa.eu/en/medicines/human/EPAR/trepulmix , access-date=9 April 2020

Research

Treprostinil therapy may be effective in treating Degos disease.{{cite journal , vauthors = Shapiro LS, Toledo-Garcia AE, Farrell JF , title = Effective treatment of malignant atrophic papulosis (Köhlmeier-Degos disease) with treprostinil--early experience , journal = Orphanet Journal of Rare Diseases , volume = 8 , pages = 52 , date = April 2013 , pmid = 23557362 , pmc = 3636001 , doi = 10.1186/1750-1172-8-52 , doi-access = free

References

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