First Introduction : USA Introduced by : United Therapeutics Trade Name: Remodulln CAS Registry No : 289840-64-4 Molecular Weight: 412.51
Treprostinil sodium has been launched for the treatment of pulmonary hypertension. This synthetically designed tricyclic benzindene analog of the natural potent vasodilator prostacyclin has been developed for subcutaneous infusion. Treprostinil sodium can be prepared in a 15 step stereoselective process. It has been suggested that treprostinil sodium acts via the prostacyclin receptor since the agent could only increase cAMP in human embryonic kidney cells transiently transfected with the human prostacyclin receptor. In a conscious spontaneously hypertensive rat model, treprostinil sodium reduced hypoxia-induced increases in pulmonary arterial pressure and pulmonary vascular resistance in a dose-related manner. At higher doses, the test compound reduced systemic arterial pressure and systemic vascular resistance. In patients with primary pulmonary arterial hypertension, a one year therapy with treprostinil improved hemodynamics parameters: a 22% improvement in cardiac output, a 24% significant decrease in peripheral vascular resistance, a decrease in mean pulmonary arterial pressure (55 vs. 58 mmHg at baseline) and an improvement in NYHA functional class were observed. In addition, 6-min walk distance was significantly improved (463 vs. 399 m at baseline). A larger study conducted in 470 patients with pulmonary arterial hypertension has demonstrated the same type of result. In patients with severe intermittent claudication, infusion of treprostinil was well tolerated and increased the blood flow in most of the peripheral arteries of the lower limb. Treprostinil is eliminated in a biphasic distribution with a terminal half-life of 2-4 h. Approximately 79% of the administrated dose is excreted in the urine. Thus, treprostinil, in contrast to the currently available epoprostenol remains biologically active for a longer time and is not sensitive to light and temperature. Moreover, the subcutaneous administration avoids the epoprostenol systemic side effects due to continuous surgically implanted intravenous infusion. Treprostinil is well tolerated by patients and the main adverse effects currently observed are injection site reaction and injection site pain.
Country of Origin Originator: First Introduction : Introduced by: Trade Name: CAS Registry No
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