Treprostinil Explained

Verifiedfields:changed
Watchedfields:changed
Verifiedrevid:477864833
Width:250
Tradename:Remodulin, Orenitram, Tyvaso, others
Dailymedid:Treprostinil
Pregnancy Au:B3
Routes Of Administration:Subcutaneous, intravenous, inhalation, by mouth
Atc Prefix:B01
Atc Suffix:AC21
Legal Us:Rx-only
Legal Us Comment:[1] [2] [3] [4]
Legal Eu:Rx-only
Legal Status:Rx-only
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%)
Cas Number:81846-19-7
Pubchem:6918140
Iuphar Ligand:5820
Drugbank:DB00374
Chemspiderid:5293353
Unii:RUM6K67ESG
Kegg:D06213
Kegg2:D08628
Chebi:50861
Chembl:1201254
Iupac Name:(1R,2R,3aS,9aS)-2,3,3a,4,9,9a-Hexahydro-2-hydroxy-1-[(3''S'')-3-hydroxyoctyl]-1H-benz[f]inden-5-yloxy]acetic acid
C:23
H:34
O:5
Stdinchi: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
Stdinchikey:PAJMKGZZBBTTOY-ZFORQUDYSA-N

Treprostinil, sold under the brand names Remodulin for infusion, Orenitram for oral, and Tyvaso for inhalation, is a vasodilator that is used for the treatment of pulmonary arterial hypertension.[5]

Treprostinil was approved for use in the United States in May 2002.[6]

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.

Adverse effects

Common side effects depending on route of administration:

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

During the 1960s a UK research team, headed by Professor John Vane began to explore the role of prostaglandins in anaphylaxis 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 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.

By 1976, Vane and fellow researcher Salvador Moncada published the first paper on prostacyclin, in the scientific journal Nature.[8]

Treprostinil (Remodulin) was approved for use in the United States in May 2002, and again in July 2018.[9] Tyvaso, the inhaled form of treprostinil, was approved for use in the United States in July 2009.[10] Orenitram was approved in December 2013.[11]

Treprostinil (Trepulmix) was approved for use in the European Union in April 2020.[12]

Research

Treprostinil therapy may be effective in treating Degos disease.[13]

Further reading

Notes and References

  1. Web site: Remodulin- treprostinil injection, solution; Sterile diluent for remodulin- water injection, solution . DailyMed . 9 October 2023 . 21 May 2024.
  2. Web site: Orenitram- treprostinil tablet, extended release; Orenitram- treprostinil kit . DailyMed . 7 November 2023 . 21 May 2024.
  3. Web site: Tyvaso- treprostinil inhalant . DailyMed . 8 December 2023 . 21 May 2024.
  4. Web site: Tyvaso DPI- treprostinil inhalant; Tyvaso DPI- treprostinil kit . DailyMed . 26 January 2024 . 21 May 2024.
  5. Torres F, Rubin LJ . Treprostinil for the treatment of pulmonary arterial hypertension . Expert Review of Cardiovascular Therapy . 11 . 1 . 13–25 . January 2013 . 23259441 . 10.1586/erc.12.160 . 29661141 .
  6. Web site: Drug Approval Package: Remodulin (Treprostinil Sodium) NDA #021272 . U.S. Food and Drug Administration (FDA) . 24 December 1999 . 9 April 2020.
  7. Kumar P, Thudium E, Laliberte K, Zaccardelli D, Nelsen A . A Comprehensive Review of Treprostinil Pharmacokinetics via Four Routes of Administration . Clinical Pharmacokinetics . 55 . 12 . 1495–1505 . December 2016 . 27286723 . 5107196 . 10.1007/s40262-016-0409-0 .
  8. 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 . 263 . 5579 . 663–665 . October 1976 . 802670 . 10.1038/263663a0 . 4279030 . 1976Natur.263..663M .
  9. Web site: Drug Approval Package: Remodulin . U.S. Food and Drug Administration (FDA) . 7 February 2019 . 9 April 2020.
  10. Web site: Drug Approval Package: Tyvaso (Treprostinil) Inhalation Solution NDA #022387 . U.S. Food and Drug Administration (FDA) . 24 December 1999 . 9 April 2020.
  11. Web site: Drug Approval Package: Orenitram (Treprostinil) Extended Release Tablets NDA #203496 . U.S. Food and Drug Administration (FDA) . 24 December 1999 . 9 April 2020.
  12. Web site: Trepulmix EPAR . European Medicines Agency (EMA) . 29 January 2020 . 9 April 2020.
  13. 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 . 8 . 52 . April 2013 . 23557362 . 3636001 . 10.1186/1750-1172-8-52 . free .

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Treprostinil".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.