- Molecular NameTreprostinil
- Synonymtreprostinil
- Weight390.52
- Drugbank_IDDB00374
- ACS_NO289480-64-4
- Show 3D model
- LogP (experiment)N/A
- LogP (predicted, AB/LogP v2.0)5.21
- pkaN/A
- LogD (pH=7, predicted)1.52
- Solubility (experiment)N/A
- LogS (predicted, ACD/Labs)(ph=7)-1.17
- LogSw (predicted, AB/LogsW2.0)0.0
- Sw (mg/ml) (predicted, ACD/Labs)0.06
- No.of HBond Donors3
- No.of HBond Acceptors5
- No.of Rotatable Bonds10
- TPSA86.99
- StatusFDA approved
- AdministrationSubcutaneous or intravenous infusion
- Pharmacologya synthetic analogue of prostacyclin (PGI2).
- Absorption_valueN/A
- Absorption (description)Relatively rapid and complete after subcutaneous infusion, with an absolute bioavailability approximately 100%.
- Caco_2N/A
- BioavailabilityN/A
- Protein binding91.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmSubstantially 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.
- Half life4 h
- ExcretionUrine (79 % of administered dose is excreted in the urine as 4% unchanged drug and 64% as identified metabolites); feces (13%)
- Urinary ExcretionN/A
- CleranceN/A
- ToxicitySymptoms 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.
- LD50 (rat)N/A
- LD50 (mouse)N/A