Treprostinil
Chemical compound
From Wikipedia, the free encyclopedia
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]
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| Trade names | Remodulin, Orenitram, Tyvaso, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a622038 |
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| Routes of administration | Subcutaneous, intravenous, inhalation, by mouth |
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| 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%) |
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| ECHA InfoCard | 100.236.149 |
| Chemical and physical data | |
| Formula | C23H34O5 |
| Molar mass | 390.520 g·mol−1 |
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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
- 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.[9]
- Because of treprostinil's inhibiting effect on platelet aggregation, there is an increased risk of bleeding, especially among patients who are also taking anticoagulants.[9]
Common side effects depending on route of administration:
- 85% of patients report pain or other reaction at the infusion site.[9]
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]
