Treprostinil

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Treprostinil
Clinical data
Trade namesRemodulin, Orenitram, Tyvaso, others
AHFS/Drugs.comMonograph
MedlinePlusa622038
License data
Pregnancy
category
  • AU: B3
Routes of
administration
Subcutaneous, intravenous, inhalation, by mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability~100%
MetabolismSubstantially metabolized by the liver
Elimination half-life4 hours
ExcretionUrine (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
E number{{#property:P628}}
CompTox Dashboard (EPA)
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Chemical and physical data
FormulaC23H34O5
Molar mass390.520 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 checkY
  • Key:PAJMKGZZBBTTOY-ZFORQUDYSA-N checkY
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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.[7]

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

Medical uses

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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

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  • 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

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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

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

References

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Further reading

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  • Clinical trial number NCT03399604 for "Investigation of the Safety and Pharmacology of Dry Powder Inhalation of Treprostinil (INSPIRE)" at ClinicalTrials.gov

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