MRE-269

MRE-269, also known as Selexipag, is a pharmaceutical compound used in the treatment of pulmonary arterial hypertension (PAH). It is a selective prostacyclin receptor (IP receptor) agonist that helps to dilate blood vessels and reduce blood pressure in the lungs.

Mechanism of Action

MRE-269 acts as an agonist at the prostacyclin receptor, which is a G protein-coupled receptor. Activation of this receptor leads to vasodilation and inhibition of smooth muscle cell proliferation. Prostacyclin is a potent vasodilator and inhibitor of platelet aggregation, and MRE-269 mimics these effects by selectively targeting the IP receptor.

Pharmacokinetics

MRE-269 is administered orally and is metabolized in the liver. It has a half-life of approximately 6-13 hours, allowing for twice-daily dosing. The drug is primarily excreted in the urine.

Clinical Use

MRE-269 is indicated for the treatment of pulmonary arterial hypertension (PAH) to delay disease progression and reduce the risk of hospitalization. It is often used in combination with other PAH therapies, such as endothelin receptor antagonists or phosphodiesterase-5 inhibitors.

Side Effects

Common side effects of MRE-269 include headache, diarrhea, nausea, and jaw pain. These side effects are generally mild to moderate in severity. Patients should be monitored for signs of hypotension and liver function abnormalities.

History

MRE-269 was developed by Nippon Shinyaku and Actelion Pharmaceuticals. It was approved by the U.S. Food and Drug Administration (FDA) in 2015 under the trade name Uptravi.

Research

Ongoing research is exploring the use of MRE-269 in other forms of pulmonary hypertension and its potential benefits in combination therapy.

Also see

• Pulmonary arterial hypertension
• Prostacyclin
• Vasodilation
• G protein-coupled receptor