NS-304

NS-304

NS-304, also known as Selexipag, is a pharmaceutical drug used in the treatment of pulmonary arterial hypertension (PAH). It is a selective prostacyclin receptor agonist that helps to dilate blood vessels and reduce blood pressure in the lungs, thereby improving symptoms and exercise capacity in patients with PAH.

Mechanism of Action

NS-304 acts as an agonist of the prostacyclin receptor (IP receptor). Prostacyclin is a naturally occurring molecule in the body that has vasodilatory and antiproliferative effects on the pulmonary artery smooth muscle cells. By activating the IP receptor, NS-304 mimics the effects of prostacyclin, leading to vasodilation and inhibition of smooth muscle cell proliferation, which are beneficial in managing PAH.

Pharmacokinetics

NS-304 is administered orally and is metabolized in the liver to its active metabolite, ACT-333679. The drug has a half-life of approximately 8 hours, allowing for twice-daily dosing. It is primarily excreted in the urine.

Clinical Use

NS-304 is indicated for the treatment of pulmonary arterial hypertension (PAH) to delay disease progression and improve exercise capacity. 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 NS-304 include headache, diarrhea, nausea, and jaw pain. These side effects are generally mild to moderate in severity. Patients should be monitored for signs of liver dysfunction and other adverse effects.

Clinical Trials

The efficacy and safety of NS-304 were established in the GRIPHON trial, a large, multicenter, randomized, placebo-controlled study. The trial demonstrated that NS-304 significantly reduced the risk of morbidity and mortality in patients with PAH.

Also see

• Pulmonary arterial hypertension
• Prostacyclin
• Endothelin receptor antagonist
• Phosphodiesterase-5 inhibitor

NS-304
Selexipag.svg
INN
Drug class
Routes of administration	Oral
Pregnancy category
Bioavailability
Metabolism	Hepatic
Elimination half-life	8 hours
Excretion	Urine
Legal status
CAS Number	475086-01-2
PubChem	11949646
DrugBank	DB09277
ChemSpider	10128256
KEGG	D08910