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Drug intelligence / Profile preview
treprostinil
- Development stage
- Approved
- Lead developer
- United Therapeutics
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
- Administration
- Oral, Inhalation, Intravenous, Subcutaneous
01
Overview
Treprostinil is a synthetic analogue of prostacyclin and acts as a vasodilator and platelet-aggregation inhibitor. It is primarily used for the treatment of pulmonary arterial hypertension (PAH) and pulmonary hypertension associated with interstitial lung disease (PH-ILD). Treprostinil works by relaxing blood vessels in the lungs, improving blood flow, inhibiting platelet aggregation, and reducing smooth muscle proliferation. Its mechanism involves binding to the prostacyclin receptor as well as activating prostaglandin D2 receptor 1 and prostaglandin E2 receptor 2, leading to increased intracellular cAMP levels and subsequent vasodilation. Treprostinil is available in oral (Orenitram), inhaled (Tyvaso), and infusion (Remodulin) formulations[1][2][3][5][6][8].
- Brand names
- RemodulinOrenitramTyvaso
- Other names
- treprostinil
02
Targets
P2Y12 (Purinergic P2Y12 receptor)PPARD (Peroxisome proliferator–activated receptor delta)PTGIR (Prostanoid IP Receptor)PTGDR (Prostanoid DP1 receptor)PTGER2 (Prostaglandin E2 receptor EP2)
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