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

PTGER2 (Prostaglandin E2 receptor EP2)PTGIR (Prostanoid IP Receptor)PPARD (Peroxisome proliferator–activated receptor delta)P2Y12 (Purinergic P2Y12 receptor)PTGDR (Prostanoid DP1 receptor)

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