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Identification
Name Treprostinil
Accession Number DB00374 (APRD01272)
Type small molecule
Groups approved
Description

Treprostinil is a synthetic analogue of prostacyclin, used to treat pulmonary hypertension. Treprostinil is marketed as Remodulin®. [Wikipedia]
Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms Not Available
Salts Not Available
Brand names
Name Company
Remodulin
Viveta
Brand mixtures Not Available
Categories
  • Antithrombotic Agents
  • Antihypertensive Agents
  • Vitamin K antagonists
CAS number 81846-19-7
Weight Average: 390.5131
Monoisotopic: 390.240624198
Chemical Formula C23H34O5
InChI Key InChIKey=PAJMKGZZBBTTOY-ZFORQUDYSA-N
InChI
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
Plain Text
IUPAC Name
2-{[(1R,2R,3aS,9aS)-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-1H,2H,3H,3aH,4H,9H,9aH-cyclopenta[b]naphthalen-5-yl]oxy}acetic acid
SMILES
[H][C@]12C[C@@H](O)[C@H](CC[C@@H](O)CCCCC)[C@@]1([H])CC1=C(C2)C(OCC(O)=O)=CC=C1
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Not Available
Classes Not Available
Substructures Not Available
Pharmacology
Indication For use as a continuous subcutaneous infusion or intravenous infusion (for those not able to tolerate a subcutaneous infusion) for the treatment of pulmonary arterial hypertension in patients with NYHA Class II-IV symptoms to diminish symptoms associated with exercise.
Pharmacodynamics Pulmonary arterial hypertension (PAH) is a disease in which blood pressure is abnormally high in the arteries between the heart and lungs. PAH is characterized by symptoms of shortness of breath during physical exertion. The condition can ultimately lead to heart failure. Treprostinil is a potent oral antiplatelet agent. The major pharmacologic actions of treprostinil are direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation. In animals, the vasodilatory effects reduce right and left ventricular afterload and increase cardiac output and stroke volume. Other studies have shown that treprostinil causes a dose-related negative inotropic and lusitropic effect. No major effects on cardiac conduction have been observed.
Mechanism of action The major pharmacological actions of treprostinil are direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation. In addition to treprostinil's direct vasodilatory effects, it also inhibits inflammatory cytokine. As a synthetic analogue of prostacyclin, it binds to the prostacyclin receptor, which subsequently induces the aforementioned downstream effects.
Absorption Relatively rapid and complete after subcutaneous infusion, with an absolute bioavailability approximately 100%. In patients with mild (n=4) or moderate (n=5) hepatic insufficiency and portopulmonary hypertension following a subcutaneous dose of 10 ng per kg of body weight per min for 150 mins the AUC 0-∞ was increased 3-fold and 5-fold respectively.
Volume of distribution
  • 14 L/70 kg
Protein binding Human plasma protein binding is approximately 91% in in vitro concentrations ranging from 330 to 10,000 µ/L.
Metabolism Substantially metabolized by the liver, but the precise enzymes responsible are unknown. Five metabolites have been described (HU1 through HU5) however, the biological activity and metabolic fate of these are unknown. The chemical structure of HU1 is unknown. The metabolite HU5 is the glucuronide conjugate of treprostinil. The other metabolites are formed by oxidation of the 3-hydroxyoctyl side chain (HU2) and subsequent additional oxidation (HU3) or dehydration (HU4). Study results of in vitro human hepatic cytochrome P450 demonstrates that treprostinil does not inhibit CYP-1A2, 2C9, 2C19, 2D6, 2E1, or 3A. Whether treprostinil induces these enzymes has not been studied.
Route of elimination Not Available
Half life Terminal elimination half-life is approximately 2 to 4 hours. Plasma half-life is 34 and 85 minutes for intravenous and subcutaneous infusion of the drug, respectively.
Clearance Not Available
Toxicity Symptoms of overdose are extensions of its dose-limiting pharmacologic effects and include flushing, headache, hypotension, nausea, vomiting, and diarrhea. Most events were self-limiting and resolved with reduction or withholding of treprostinil.
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers
  • United therapeutics corp
Packagers
Dosage forms
Form Route Strength
Solution Intravenous
Prices
Unit description Cost Unit
Remodulin 10 mg/ml vial 737.0 USD ml
Remodulin 5 mg/ml vial 368.5 USD ml
Tyvaso inhalation starter kit 185.8 USD ml
Remodulin 2.5 mg/ml vial 184.25 USD ml
Tyvaso 1.74 mg/2.9 ml solution 174.55 USD ml
Tyvaso inhalation refill kit 165.68 USD ml
Remodulin 1 mg/ml vial 73.7 USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Country Patent Number Approved Expires (estimated)
United States 6521212 1998-11-13 2018-11-13
United States 5153222 1994-10-06 2014-10-06
Properties
State solid
Experimental Properties
Property Value Source
water solubility Insoluble at 25°C Not Available
logP 4.1 Not Available
Predicted Properties
Property Value Source
water solubility 7.31e-03 g/l ALOGPS
logP 3.53 ALOGPS
logP 4 ChemAxon
logS -4.7 ALOGPS
pKa (strongest acidic) 3.76 ChemAxon
pKa (strongest basic) -1.3 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 5 ChemAxon
hydrogen donor count 3 ChemAxon
polar surface area 86.99 ChemAxon
rotatable bond count 10 ChemAxon
refractivity 108 ChemAxon
polarizability 45.74 ChemAxon
References
Synthesis Reference Not Available
General Reference Not Available
External Links
Resource Link
ChEBI 50861 Link_out
ChEMBL 50861 Link_out
Therapeutic Targets Database DAP001214 Link_out
PharmGKB PA164768801 Link_out
Drug Product Database 2246552 Link_out
RxList http://www.rxlist.com/cgi/generic/remodulin.htm Link_out
Drugs.com http://www.drugs.com/cdi/treprostinil-inhalation-solution.html Link_out
Wikipedia http://en.wikipedia.org/wiki/Treprostinil Link_out
ATC Codes
  • B01AC21
AHFS Codes
  • 24:12.92
PDB Entries Not Available
FDA label show (223 KB)
MSDS show (17.4 KB)
Interactions
Drug Interactions
Drug Interaction
Abciximab The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Abciximab. Monitor for increased bleeding during concomitant thearpy.
Acebutolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Acenocoumarol The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Acenocoumarol. Monitor for increased bleeding during concomitant thearpy.
Acetazolamide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Acetylsalicylic acid The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Acetylsalicylic acid. Monitor for increased bleeding during concomitant thearpy.
Aliskiren Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Amiloride Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Aminosalicylic Acid The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the salicylate, Aminosalicylic acid. Monitor for increased bleeding during concomitant thearpy.
Amlodipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Amyl Nitrite Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Anagrelide The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Anagrelide. Monitor for increased bleeding during concomitant thearpy.
Apraclonidine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Argatroban The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Argatroban. Monitor for increased bleeding during concomitant thearpy.
Atenolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Benazepril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Bendroflumethiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Betaxolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Bisoprolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Bivalirudin The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Bivalirudin. Monitor for increased bleeding during concomitant thearpy.
Brimonidine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Bumetanide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Candesartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Captopril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Carteolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Carvedilol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Celecoxib The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Celecoxib. Monitor for increased bleeding during concomitant thearpy.
Celiprolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Chlorothiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Chlorthalidone Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Cilazapril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Cilostazol The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Cilostazol. Monitor for increased bleeding during concomitant thearpy.
Citalopram The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Citalopram. Monitor for increased bleeding during concomitant thearpy.
Clevidipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Clonidine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Clopidogrel The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Clopidogrel. Monitor for increased bleeding during concomitant thearpy.
Cyclandelate Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Dexmedetomidine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Dichlorphenamide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Diclofenac The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Diclofenac. Monitor for increased bleeding during concomitant thearpy.
Diflunisal The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Diflunisal. Monitor for increased bleeding during concomitant thearpy.
Diltiazem Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Dipyridamole The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Dipyridamole. Monitor for increased bleeding during concomitant thearpy. Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Doxazosin Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Drospirenone Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Drotrecogin alfa The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Drotrecogin alfa. Monitor for increased bleeding during concomitant thearpy.
Enalapril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Enoxaparin The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Exoxaparin. Monitor for increased bleeding during concomitant thearpy.
Eplerenone Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Eprosartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Eptifibatide The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Eptifibatide. Monitor for increased bleeding during concomitant thearpy.
Escitalopram The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Escitalopram. Monitor for increased bleeding during concomitant thearpy.
Esmolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Ethacrynic acid Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Etodolac The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Etodolac. Monitor for increased bleeding during concomitant thearpy.
Felodipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Fenoprofen The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Fenoprofen. Monitor for increased bleeding during concomitant thearpy.
Fluoxetine The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Fluoxetine. Monitor for increased bleeding during concomitant thearpy.
Flurbiprofen The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Flurbiprofen. Monitor for increased bleeding during concomitant thearpy.
Fluvoxamine The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Fluvoxamine. Monitor for increased bleeding during concomitant thearpy.
Fosinopril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Furosemide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Guanabenz Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Guanfacine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Heparin The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Heparin. Monitor for increased bleeding during concomitant thearpy.
Hydralazine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Hydrochlorothiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Hydroflumethiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Ibuprofen The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ibuprofen. Monitor for increased bleeding during concomitant thearpy.
Indapamide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Indomethacin The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Indomethacin. Monitor for increased bleeding during concomitant thearpy.
Irbesartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Isosorbide Dinitrate Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Isosorbide Mononitrate Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Isradipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Ketoprofen The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ketoprofen. Monitor for increased bleeding during concomitant thearpy.
Ketorolac The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Ketorolac. Monitor for increased bleeding during concomitant thearpy.
Labetalol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Lepirudin The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Lepirudin. Monitor for increased bleeding during concomitant thearpy.
Levobunolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Lisinopril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Losartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Lumiracoxib The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Lumiracoxib. Monitor for increased bleeding during concomitant thearpy.
Mannitol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Meclofenamic acid The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Meclofenamate. Monitor for increased bleeding during concomitant thearpy.
Mefenamic acid The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Mefenamic acid. Monitor for increased bleeding during concomitant thearpy.
Meloxicam The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Meloxicam. Monitor for increased bleeding during concomitant thearpy.
Methazolamide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Methyclothiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Metipranolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Metolazone Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Metoprolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Minoxidil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Moexipril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nabumetone The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Nabumetone. Monitor for increased bleeding during concomitant thearpy.
Nadolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Naproxen The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Naproxen. Monitor for increased bleeding during concomitant thearpy.
Nebivolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nesiritide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nicardipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nifedipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nimodipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nisoldipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nitrendipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nitroglycerin Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Nitroprusside Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Olmesartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Oxaprozin The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Oxaprozin. Monitor for increased bleeding during concomitant thearpy.
Oxprenolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Papaverine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Paroxetine The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Paroxetine. Monitor for increased bleeding during concomitant thearpy.
Penbutolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Perindopril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Phenoxybenzamine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Phentolamine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Pindolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Piroxicam The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Piroxicam. Monitor for increased bleeding during concomitant thearpy.
Polythiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Prazosin Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Quinapril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Ramipril Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Reserpine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Rivaroxaban The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Rivaroxaban. Monitor for increased bleeding during concomitant thearpy.
Salsalate The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the salicylate, Salsalate. Monitor for increased bleeding during concomitant thearpy.
Sertraline The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Sertraline. Monitor for increased bleeding during concomitant thearpy.
Sotalol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Spironolactone Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Sulindac The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Sulindac. Monitor for increased bleeding during concomitant thearpy.
Telmisartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Terazosin Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Tiaprofenic acid The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Tiaprofenic acid. Monitor for increased bleeding during concomitant thearpy.
Ticlopidine The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Ticlopidine. Monitor for increased bleeding during concomitant thearpy.
Timolol Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Tirofiban The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the antiplatelet agent, Tirofiban. Monitor for increased bleeding during concomitant thearpy.
Tizanidine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Tolazoline Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Tolmetin The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Tolmetin. Monitor for increased bleeding during concomitant thearpy.
Torasemide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Trandolapril The prostacyclin analogue, Treprostinil, may increase the hypotensive effect of Trandolapril.
Triamterene Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Trichlormethiazide Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Urea Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Valsartan Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Verapamil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Warfarin The prostacyclin analogue, Treprostinil, increases the risk of bleeding when combined with the anticoagulant, Warfarin. Monitor for increased bleeding during concomitant thearpy.
Food Interactions Not Available
Targets

1. Prostacyclin receptor

Pharmacological action: yes
Actions: agonist

Receptor for prostacyclin (prostaglandin I2 or PGI2). The activity of this receptor is mediated by G(s) proteins which activate adenylate cyclase

Organism class: human
UniProt ID: P43119 Link_out
Gene: PTGIR Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Falcetti E, Hall SM, Phillips PG, Patel J, Morrell NW, Haworth SG, Clapp LH: Smooth Muscle Proliferation and Role of the Prostacyclin (IP) Receptor in Idiopathic Pulmonary Arterial Hypertension. Am J Respir Crit Care Med. 2010 Jul 9. Pubmed
  2. Sprague RS, Bowles EA, Hanson MS, DuFaux EA, Sridharan M, Adderley S, Ellsworth ML, Stephenson AH: Prostacyclin analogs stimulate receptor-mediated cAMP synthesis and ATP release from rabbit and human erythrocytes. Microcirculation. 2008 Jul;15(5):461-71. Pubmed
  3. Olschewski H, Rose F, Schermuly R, Ghofrani HA, Enke B, Olschewski A, Seeger W: Prostacyclin and its analogues in the treatment of pulmonary hypertension. Pharmacol Ther. 2004 May;102(2):139-53. Pubmed
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Peroxisome proliferator-activated receptor delta

Pharmacological action: yes
Actions: agonist

Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-CoA oxidase and activates its transcription. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Decreases expression of NPC1L1 once activated by a ligand

Organism class: human
UniProt ID: Q03181 Link_out
Gene: PPARD Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Ali FY, Egan K, FitzGerald GA, Desvergne B, Wahli W, Bishop-Bailey D, Warner TD, Mitchell JA: Role of prostacyclin versus peroxisome proliferator-activated receptor beta receptors in prostacyclin sensing by lung fibroblasts. Am J Respir Cell Mol Biol. 2006 Feb;34(2):242-6. Epub 2005 Oct 20. Pubmed

3. P2Y purinoceptor 12

Pharmacological action: yes
Actions: agonist

Receptor for ADP and ATP coupled to G-proteins that inhibit the adenylyl cyclase second messenger system. Not activated by UDP and UTP. Involved in platelets aggregation

Organism class: human
UniProt ID: Q9H244 Link_out
Gene: P2RY12 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
Enzymes

1. Cytochrome P450 2C9

Actions: substrate

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S- warfarin, diclofenac, phenytoin, tolbutamide and losartan

UniProt ID: P11712 Link_out
Gene: CYP2C9
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Gotzkowsky SK, Dingemanse J, Lai A, Mottola D, Laliberte K: Lack of a pharmacokinetic interaction between oral treprostinil and bosentan in healthy adult volunteers. J Clin Pharmacol. 2010 Jul;50(7):829-34. doi: 10.1177/0091270009351173. Epub 2010 Feb 4. Pubmed
Comments
Drug created on June 13, 2005 07:24 / Updated on February 08, 2013 16:19