Treprostinil
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2002
- First approval year
- 2002
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Treprostinil
- Molecular weight
- 390.52
- Structure (SMILES)
- CCCCC[C@H](O)CC[C@@H]1[C@H]2Cc3cccc(OCC(=O)O)c3C[C@H]2C[C@H]1O
- remodulin
- Remodulin
- tyvaso
- Tyvaso
- tyvaso dpi
- Tyvaso dpi
- [(1R,2R,3aS,9aS)-2-Hydroxy-1-((3S)-3-hydroxyoctyl)-2,3,3a,4,9,9a-hexahydro-1H-cylopent[b]naphthalen-5-yl]oxy]acetate
- 15 au 81
- 15-AU-81
- 15au81
- 15AU81
- 1r 2r 3as 9as 2 hydroxy 1 3s 3 hydroxyoctyl 2 3 3a 4 9 9a hexahydro 1h cylopent b naphthalen 5 yl oxy acetate
- iv remodulin
- IV Remodulin
- l 606
- L-606
- l606
- L606
- LRX -15
- lrx 15
- LRX-15
- remodulin
- Remodulin
- rumodolin
- Rumodolin
- treprostinil
- Treprostinil
- treprostinil [INN]
- TREPROSTINIL [JAN]
- TREPROSTINIL [MART.]
- TREPROSTINIL [MI]
And 22 more, listed on the interactive page.
- ATC classification codes
- B01AC21
Sources for recorded values
- CAS registry numbers
- 81846-19-7
- ChEMBL ID
- CHEMBL1237119
- InChIKey
- PAJMKGZZBBTTOY-ZFORQUDYSA-N
- PubChem compound IDs
- 6918140
- RxNorm IDs (RxCUI)
- 343048
- FDA ingredient codes (UNII)
- RUM6K67ESG
- Applicant
- UNITED THERAP
- Approval date
- 21 May 2002
- Application number
- NDA021272
- Status
- Authorised
- Status date
- 3 Apr 2020
- Authorisation date
- 3 Apr 2020
- Approved indications
- Treatment of adult patients with WHO Functional Class (FC) III or IV and: inoperable chronic thromboembolic pulmonary hypertension (CTEPH), or persistent or recurrent CTEPH after surgical treatment to improve exercise capacity.
- Product number
- EMEA/H/C/005207
- Authorisation holder
- SciPharm Sàrl
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Hypertension, Pulmonary
European medicines record
- Patents
- 18
- Designations
- 2
- Earliest recorded loss of exclusivity
- 3 Feb 2042
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- Yes
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- United States (FDA)
- Approved
- European Union (EMA)
- Authorised
- Pharmacology name
- treprostinil
- Type
- Synthetic organic
- Drug name stem
- -prost-
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Parenteral
- topical
- Action
- Agonist
- Action type
- Agonist
- Target
- EP4 receptor
- Gene symbol
- PTGER4
- Protein identifier
- P35408
- Median affinity
- 6.7
- Affinity units
- pEC50
- Action
- Agonist
- Action type
- Agonist
- Target
- EP4 receptor
- Gene symbol
- PTGER4
- Protein identifier
- P35408
- Median affinity
- 6.1
- Affinity units
- pKi
- Mechanism
- Prostanoid IP receptor agonist
- Action type
- Agonist
- Target
- Prostacyclin receptor
- Protein identifier
- P43119
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- EP1 receptor
- Gene symbol
- PTGER1
- Protein identifier
- P34995
- Median affinity
- 6.7
- Affinity units
- pKi
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- EP3 receptor
- Gene symbol
- PTGER3
- Protein identifier
- P43115
- Median affinity
- 5.6
- Affinity units
- pKi
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- EP2 receptor
- Gene symbol
- PTGER2
- Protein identifier
- P43116
- Median affinity
- 8.4
- Affinity units
- pKi
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- IP receptor
- Gene symbol
- PTGIR
- Protein identifier
- P43119
- Median affinity
- 8.72
- Affinity units
- pEC50
- Primary target
- Yes
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- IP receptor
- Gene symbol
- PTGIR
- Protein identifier
- P43119
- Median affinity
- 7.49
- Affinity units
- pKi
- Primary target
- Yes
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- DP1 receptor
- Gene symbol
- PTGDR
- Protein identifier
- Q13258
- Median affinity
- 8.4
- Affinity units
- pKi
Open Targets mechanisms
- Mechanism
- Prostanoid IP receptor agonist
- Action type
- Agonist
- Target
- Prostacyclin receptor
- Action type
- Agonist
- Gene symbol
- PTGER1
- Protein identifier
- P34995
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Agonist
- Gene symbol
- PTGER4
- Protein identifier
- P35408
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Agonist
- Gene symbol
- PTGER3
- Protein identifier
- P43115
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Agonist
- Gene symbol
- PTGER2
- Protein identifier
- P43116
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Agonist
- Gene symbol
- PTGIR
- Protein identifier
- P43119
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Agonist
- Gene symbol
- PTGDR
- Protein identifier
- Q13258
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Pulmonary Disease, Chronic Obstructive
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000341
- Subject identifier
- D029424
- Condition
- Ischemia
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000556
- Subject identifier
- D007511
- Condition
- Scleroderma, Systemic
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000717
- Subject identifier
- D012595
- Condition
- Idiopathic Pulmonary Fibrosis
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000768
- Subject identifier
- D054990
- Condition
- Pulmonary Arterial Hypertension
- Highest recorded phase
- 4
- Condition identifier
- EFO:0001361
- Subject identifier
- D000081029
- Condition
- Hypertension, Pulmonary
- Highest recorded phase
- 4
- Condition identifier
- EFO:0001361
- Subject identifier
- D006976
- Condition
- Reperfusion Injury
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002687
- Subject identifier
- D015427
- Condition
- Peripheral Vascular Diseases
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003875
- Subject identifier
- D016491
- Condition
- Lung Diseases, Interstitial
- Highest recorded phase
- 3
- Condition identifier
- EFO:0004244
- Subject identifier
- D017563
- Condition
- Hernias, Diaphragmatic, Congenital
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005207
- Subject identifier
- D065630
- Condition
- Pulmonary Fibrosis
- Highest recorded phase
- 3
- Condition identifier
- EFO:0009448
- Subject identifier
- D011658
- Condition
- Persistent Fetal Circulation Syndrome
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001103
- Subject identifier
- D010547
- Condition
- Raynaud Disease
- Highest recorded phase
- 0.5
- Condition identifier
- EFO:1001145
- Subject identifier
- D011928
- Condition
- Diabetic Foot
- Highest recorded phase
- 1
- Condition identifier
- EFO:1001459
- Subject identifier
- D017719
- Condition
- Thrombosis
- Highest recorded phase
- 4
- Condition identifier
- HP:0004419
- Subject identifier
- D013927
- Condition
- Familial Primary Pulmonary Hypertension
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0001999
- Subject identifier
- D065627
- Condition
- Diabetes Mellitus, Type 1
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0005147
- Subject identifier
- D003922
- Condition
- Hypertension, Pulmonary
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0005149
- Subject identifier
- D006976
- Condition
- Respiratory Distress Syndrome
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0100130
- Subject identifier
- D012128
- Condition identifier
- EFO_0000341
- Highest recorded phase
- 3
- Condition identifier
- EFO_0000556
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000717
- Condition identifier
- EFO_0000768
- Highest recorded phase
- 3
- Condition identifier
- EFO_0001361
- Condition identifier
- EFO_0002687
- Condition identifier
- EFO_0003837
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003875
- Condition identifier
- EFO_0004244
- Highest recorded phase
- 3
- Condition identifier
- EFO_0005207
- Highest recorded phase
- 2
- Condition identifier
- EFO_0009197
- Condition identifier
- EFO_0009448
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001103
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001145
- Condition identifier
- EFO_1001459
- Condition identifier
- EFO_1001459
- Highest recorded phase
- 1
- Condition identifier
- HP_0001750
- Condition identifier
- HP_0003546
- Highest recorded phase
- 2
- Condition identifier
- HP_0004419
- Condition identifier
- HP_0004419
- Highest recorded phase
- 4
- Condition identifier
- HP_0012418
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0001999
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002123
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002771
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005002
- Highest recorded phase
- 2
And 10 more, listed on the interactive page.
- Event
- abdominal discomfort
- Reports
- 444
- Reporting signal score
- 277.472
- Event
- abdominal distension
- Reports
- 339
- Reporting signal score
- 253.235
- Event
- ascites
- Reports
- 225
- Reporting signal score
- 234.468
- Event
- blood pressure decreased
- Reports
- 373
- Reporting signal score
- 357.478
- Event
- chest discomfort
- Reports
- 399
- Reporting signal score
- 259.354
- Event
- chest pain
- Reports
- 950
- Reporting signal score
- 805.829
- Event
- cough
- Reports
- 1,276
- Reporting signal score
- 1,124.88
- Event
- decreased appetite
- Reports
- 577
- Reporting signal score
- 280.216
- Event
- dermatitis contact
- Reports
- 349
- Reporting signal score
- 927.188
- Event
- device infusion issue
- Reports
- 110
- Reporting signal score
- 341.441
- Event
- diarrhoea
- Reports
- 2,292
- Reporting signal score
- 1,455.42
- Event
- dizziness
- Reports
- 1,449
- Reporting signal score
- 723.491
- Event
- dyspnoea
- Reports
- 3,508
- Reporting signal score
- 3,879.55
- Event
- dyspnoea exertional
- Reports
- 649
- Reporting signal score
- 1,215.25
- Event
- epistaxis
- Reports
- 328
- Reporting signal score
- 227.463
- Event
- fatigue
- Reports
- 1,411
- Reporting signal score
- 347.503
- Event
- feeling abnormal
- Reports
- 571
- Reporting signal score
- 354.571
- Event
- fluid overload
- Reports
- 599
- Reporting signal score
- 1,595.15
- Event
- fluid retention
- Reports
- 879
- Reporting signal score
- 1,816.54
- Event
- flushing
- Reports
- 765
- Reporting signal score
- 1,019.68
- Event
- haemoptysis
- Reports
- 204
- Reporting signal score
- 219.695
- Event
- headache
- Reports
- 2,715
- Reporting signal score
- 2,375.28
- Event
- heart rate increased
- Reports
- 353
- Reporting signal score
- 296.432
- Event
- hypotension
- Reports
- 925
- Reporting signal score
- 534.583
- Event
- hypoxia
- Reports
- 337
- Reporting signal score
- 404.381
And 35 more, listed on the interactive page.
- NCT00004497
- NCT00147199
- NCT00325403
- NCT00325442
- NCT00760916
- NCT00887978
- NCT01104870
- NCT03496623
- NCT05176951
- NCT00067041
- NCT00439946
- NCT00494533
- NCT00741819
- NCT01027949
- NCT01268553
- NCT01305252
- NCT01477333
- NCT01557647
- NCT01557660
- NCT01588405
- NCT01615627
- NCT01934582
- NCT02882126
- NCT02893995
- NCT02999906
And 28 more, listed on the interactive page.
- Dose
- 18 mcg per treatment session (initial), titrating up to 9-12 breaths per session
- Route
- Inhalation
- How often
- 4 times daily approximately 4 hours apart during waking hours
- Administer undiluted
- Do not mix with other medications in the device
- Use only with the Tyvaso Inhalation System
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 3
- Polar surface area
- 86.99
- Calculated partition coefficient (ALogP)
- 3.58
- Calculated partition coefficient (XLogP)
- 4.5
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 10
- Heavy atoms
- 28
- Molecular formula
- C23H34O5
- Monoisotopic mass
- 390.24062418
- Natural product
- Yes
- 0703-0666
- 0703-0676
- 0703-0686
- 0703-0696
- 0781-3420
- 0781-3425
- 0781-3427
- 0781-3430
- 0781-6021
- 43598-126
- 43598-646
- 43598-647
- 43598-648
- 43598-649
- 62332-514
- 62332-515
- 62332-516
- 62332-517
- 66302-101
- 66302-102
- 66302-105
- 66302-110
- 66302-114
- 66302-150
- 66302-206
And 26 more, listed on the interactive page.
- Recorded assays
- 117
- Active assays
- 12
- Confirmatory
- Other
- Antihypertensive Agents
Related records
Trials (78)
- A 48-week Study of the Effect of Dual Therapy (Inhaled Treprostinil and Tadafafil) Versus Monotherapy (Tadalafil).
- A Phase 3 Adaptive Study to Evaluate the Safety and Efficacy of Inhaled Treprostinil in Participants With Pulmonary Hypertension (PH) Due to Chronic Obstructive Pulmonary Disease (COPD)
- A Phase 3 Study to Evaluate the Safety and Efficacy L606 in Participants With PH-ILD
- A Phase 3 Study to Evaluate the Safety and Tolerability of L606 in Subjects With PAH or PH-ILD
- A Study of a Mean Pulmonary Artery Pressure-Targeted Approach With Early and Rapid Treprostinil Therapy to Reverse Right Ventricular Remodeling in Participants With Pulmonary Arterial Hypertension
- A Study of Infusion Site Pain After Infusion of Excipients in Participants With Type 1 Diabetes Mellitus
- A Study of Inhaled Treprostinil (LIQ861) in Adults With Pulmonary Arterial Hypertension Transitioning From Oral Selexipag
- A Study of Treprostinil and a New Formulation of LY900014 in Healthy Japanese Participants
- A Study of Treprostinil to Treat Interstitial Lung Disease Pulmonary Hypertension
- A Study to Assess the Safety and Efficacy of Treprostinil to Facilitate Liver Transplantation in Patients With Portopulmonary Hypertension
- A Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of C16TR for Inhalation With Tyvaso® Cohort in Healthy Participants
- A Study to Observe the Safety, Tolerability, and Efficacy of Remodulin
- Acute Effects of Inhaled Treprostinil in Fontan Patients
- ADAPT - A Patient Registry of the Real-world Use of Orenitram®
- Addition of UT-15C SR to Pulmonary Arterial Hypertension Patients Currently Receiving Tyvaso®
- An Open Label Extension Study to Evaluate Inhaled Treprostinil in Adult PH With ILD Including CPFE
- An Open Label Extension Study to Evaluate the Safety of Continued Therapy of Subcutanous Remodulin® in Pulmonary Arterial Hypertension
- An Open-Label Extension Trial of UT-15C Sustained-release (SR) in Subjects With Pulmonary Arterial Hypertension
- Assess Efficacy of of Oral Treprostinil in Patients With Symptomatic Primary or Secondary Raynaud's Phenomenon
- Clinical Investigation Into Inhaled Treprostinil Sodium in Patients With Severe Pulmonary Arterial Hypertension (PAH)
Approved for (3)
- Pulmonary arterial hypertension
- Pulmonary hypertension
- Thrombotic disease
In development for (15)
- Adult acute respiratory distress syndrome Phase 2
- Calcinosis Phase 2
- Chronic obstructive pulmonary disease Phase 2
- Congenital heart disease Phase 2
- Idiopathic pulmonary arterial hypertension Phase 3
- Idiopathic pulmonary fibrosis Phase 3
- Interstitial lung disease Phase 3
- Ischemia reperfusion injury Phase 1
- Ischemic disease Phase 2
- Peripheral vascular disease Phase 2
- Persistent fetal circulation syndrome Phase 2
- Pulmonary fibrosis Phase 3
- Raynaud disease Early phase 1
- Systemic sclerosis Phase 1
- Type 1 diabetes mellitus Phase 1