Treprostinil 10mg/10ml solution for infusion vials
Requires a prescription from a doctor or prescriber
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Safety monitoring data
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Suspected adverse reactions reported for Treprostinil
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
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Suspected adverse reactions reported for Treprostinil
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2 branded products available
MHRA licensed products
View all licensed products for Treprostinil on the MHRA register
Treposuvi 10mg/10ml solution for infusion vials
Trepulmix 10mg/10ml solution for infusion vials
Therapeutically similar medicines
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
Clinical guidelines and formulary information
British National Formulary
Treprostinil
Source: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
Check stock at pharmacies and supply information
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Supply & product information
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Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
Browse tools
SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
7 found
Half-life
4 hours
Mechanism
Treprostinil is a stable analogue of prostacyclin[L41855,L41860,L41865], a prost…
Food interactions
1 warning
Human targets
5 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
100%
[L41860]…
Half-life
4 hours
[L41855][L41860]
Protein binding
000 μg/L
Volume of distribution
14 L
[L41855][L41860]
Metabolism
1 thr
[L41855][L41860][L41865]…
Elimination
79%
[L41855][L41860]…
Clearance
30 L/h
[L41860]
In patients with mild to moderate hepatic insufficiency, clearance is reduced up to 80%.
[L41855]…
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Treprostinil was approved by the FDA in 2002 for the treatment of pulmonary arterial hypertension.[L41860] It is available in the following routes of administration: subcutaneous, intravenous, inhaled and oral. The first generic form of treprostinil became available in 2019.[A248775]
[L41860]
The Health Canada label specifies that treprostinil is indicated for the long-term treatment of pulmonary arterial hypertension in NYHA Class III and IV patients who did not respond adequately to conventional therapy.
[L24244]
L24244
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 1298 interactions
[L41860]
These include flushing, headache, hypotension, nausea, vomiting, and diarrhea.
[L41855][L41860][L41865]
Most overdose events were self-limiting and resolved by reducing or withholding treprostinil.
[L41860]
In studies where treprostinil was infused using an external pump, several patients received an overdose due to an accidental bolus administration, errors in the programmed delivery rate and incorrect prescriptions. Only two cases of of substantial hemodynamic concern were detected among patients that received an excess of treprostinil.
[L41860]
A pediatric patient that accidentally received 7.5 mg of treprostinil via a central venous catheter presented flushing, headache, nausea, vomiting, hypotension, and seizure-like activity with loss of consciousness for several minutes.
[L41860]
A rat study that evaluated the carcinogenic effects of inhaled treprostinil, found no evidence of carcinogenicity in levels up to 35 times the clinical exposure obtained with a maintenance dose of 54 μg.
[L41855]
The infusion of treprostinil sodium did not affect fertility or mating performance in rats given subcutaneous treprostinil.
[L41860]
Treprostinil did not show mutagenic or clastogenic effects in in vitro or in vivo studies.
[L41855][L41860]
There was no significant increase of tumors in rats given up to 10 mg/kg/day of oral treprostinil diolamine.
[L41865]
Treprostinil binds and activates the prostacyclin receptor, the prostaglandin D2 receptor 1, and the prostaglandin E2 receptor 2.[A248770] The activation of these receptors leads to the elevation of intracellular cyclic adenosine monophosphate (cAMP) levels, which consequently promotes the opening of calcium-activated potassium channels that lead to cell hyperpolarization.[A248770] This mechanism promotes the direct vasodilation of pulmonary and systemic arterial vascular beds and the inhibition of platelet aggregation[A248735][L41855][L41860][L41865]. In addition to its direct vasodilatory effects, treprostinil inhibits inflammatory pathways.[A248765]
Due to its ability to inhibit platelet aggregation, treprostinil can increase the risk of bleeding, and patients with low systemic arterial pressure taking treprostinil may experience symptomatic hypotension.[L41855][L41860] The abrupt withdrawal of treprostinil or drastic changes in dose may worsen the symptoms of pulmonary arterial hypertension (PAH).[L41860][L41865] The inhalation of treprostinil can also cause bronchospasms in patients with asthma, chronic obstructive pulmonary disease (COPD), or bronchial hyperreactivity.[L41855] When given intravenously, treprostinil can lead to infusion complications and increase the risk of bloodstream infections.[L41860]
How the body processes this drug — absorption, distribution, metabolism, and elimination
[L41860]
The pharmacokinetics of treprostinil follow a two-compartment model and are linear between 2.5 and 125 ng/kg/min.
[L41860]
Subcutaneous and intravenous doses of treprostinil are bioequivalent at 10 ng/kg/min. Compared to healthy subjects, patients with mild and moderate hepatic insufficiency had a corresponding Cmax 2- and 4-times higher and an AUC0-∞ 3- and 5-times higher when given a subcutaneous treprostinil dose of 10 ng/kg/min for 150 min.
[L41860]
When given orally at doses between 0.5 and 15 mg twice a day, treprostinil follows a dose-proportional pharmacokinetic profile.
[L41865]
The oral bioavailability of treprostinil is 17%, and drug concentration reaches its highest level between 4 and 6 hours after oral administration.
[L41865]
The oral absorption of treprostinil is affected by food. The AUC and Cmax of oral treprostinil increase 49% and 13%, respectively, when this drug is administered with a high-fat, high-calorie meal.
[L41865]
The AUC and Cmax of inhaled treprostinil were proportional to the doses administered (18 to 90 μg).
[L41855]
The bioavailability of inhaled treprostinil was 64% in patients receiving 2 doses of 18 μg, and 72% in patients receiving two doses of 36 μg.
[L41855]
Two separate studies that evaluated the pharmacokinetics of inhaled treprostinil at a maintenance dose of 54 μg found that the mean Cmax was 0.91 and 1.32 ng/mL, respectively, with a corresponding Tmax of 0.25 and 0.12 hr and a mean AUC of 0.81 and 0.97 hr⋅ng/mL.
[L41855]
[L41855][L41860]
[L41240][L41860]
[L41855][L41860]
[L41855][L41860][L41865]
Treprostinil does not have a single major metabolite. The five metabolites detected in urine (HU1 through HU5) accounted for 13.8, 14.3, 15.5, 10.6 and 10.2% of the dose, respectively.
[L41880]
One of the metabolites (HU5) is the glucuronide conjugate of treprostinil. HU1, HU2, HU3 and HU4 are formed through the oxidation of the 3-hydroxyloctyl side chain.
[L41855][L41860][L41865][L41880]
None of the metabolites of treprostinil appear to be active. In vitro studies suggest that treprostinil does not inhibit or induce any major CYP enzymes.
[L41855][L41860]
[L41855][L41860]
Only a small proportion of treprostinil is excreted unchanged. When administered orally, 1.13% and 0.19% of unchanged treprostinil diolamine are found in urine and feces, respectively.
[L41865]
When administered subcutaneously, intravenously or by inhalation, 4% of unchanged treprostinil is found in urine.
[L41855][L41860]
[L41860]
In patients with mild to moderate hepatic insufficiency, clearance is reduced up to 80%.
[L41855]
Proteins and enzymes this drug interacts with in the body
Involved in PLA2G3-dependent maturation of mast cells. PLA2G3 is secreted by immature mast cells and acts on nearby fibroblasts upstream to PTDGS to synthesize PGD2, which in turn promotes mast cell maturation and degranulation via PTGDR (By similarity)
PMID:35675826
Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Has a preference for poly-unsaturated fatty acids, such as gamma-linoleic acid and eicosapentanoic acid. Once activated by a ligand, the receptor binds to promoter elements of target genes.
Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the acyl-CoA oxidase gene. Decreases expression of NPC1L1 once activated by a ligand
Enzymes involved in drug metabolism — important for understanding drug interactions
ATC B01AC21
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Treprostinil
Additional database identifiers
Drugs Product Database (DPD)
12594
ChemSpider
5293353
PDB
Y9J
ZINC
ZINC000003800475
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9602
GenAtlas
PTGIR
GeneCards
PTGIR
GenBank Gene Database
L29016
GenBank Protein Database
495043
Guide to Pharmacology
345
UniProt Accession
PI2R_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9594
GenAtlas
PTGER2
GeneCards
PTGER2
GenBank Gene Database
U19487
GenBank Protein Database
632650
Guide to Pharmacology
341
UniProt Accession
PE2R2_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9591
GenAtlas
PTGDR
GeneCards
PTGDR
GenBank Gene Database
U31332
GenBank Protein Database
940379
Guide to Pharmacology
338
UniProt Accession
PD2R_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9235
GenAtlas
PPARD
GeneCards
PPARD
GenBank Gene Database
L07592
GenBank Protein Database
190230
Guide to Pharmacology
594
UniProt Accession
PPARD_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:18124
GenAtlas
P2RY12
GeneCards
P2RY12
GenBank Gene Database
AF313449
GenBank Protein Database
12083902
Guide to Pharmacology
328
UniProt Accession
P2Y12_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2622
GenAtlas
CYP2C8
GeneCards
CYP2C8
GenBank Gene Database
M17397
Guide to Pharmacology
1325
UniProt Accession
CP2C8_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:2623
GenAtlas
CYP2C9
GeneCards
CYP2C9
GenBank Gene Database
AY341248
Guide to Pharmacology
1326
UniProt Accession
CP2C9_HUMAN
International reference pricing
Reference pricing from DrugBank. Prices are indicative and may not reflect current UK costs.
Source: DrugBank. Used under CC BY-NC 4.0 academic licence for non-commercial purposes.
Patent information
26 active patents, 14 expired
Source: DrugBank · CC BY-NC 4.0. Patent data sourced from national patent offices. Expiry dates may not reflect extensions, regulatory exclusivity periods, or legal challenges.
DrugBank citations
If you use DrugBank data in your research, please cite the following publications: