PRX-08066 is a drug discovered and developed by Predix (later Epix) Pharmaceuticals

ale S. Dhanoa et al. Patent US 7,030,240 B2 Ale is a style of beer, brewed using a warm fermentation method. In medieval England, the term referred to a drink brewed without hops. As with most beers, ale typically has a bittering agent to balance the malt and act as a preservative. Ale ...

which acts as a potent and selective

antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.serotonin Serotonin (), also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter with a wide range of functions in both the central nervous system (CNS) and also peripheral tissues. It is involved in mood, cognition, reward, learning, ...

5-HT_2B

receptor Receptor may refer to: * Sensory receptor, in physiology, any neurite structure that, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and respond ...

, with a 5-HT_2B binding affinity (K_i) of 3.4nM, and high selectivity over the closely related 5-HT_2A and 5-HT_2C receptors and other receptor targets. PRX-08066 and other selective 5-HT_2B antagonists are being researched for the treatment of

pulmonary arterial hypertension Pulmonary arterial hypertension (PAH) is a syndrome in which the blood pressure in the pulmonary arteries and pulmonary arterioles (the blood vessels located proximal to the capillary bed, the site of oxygen exchange in the lungs) is elevated. T ...

, following the discovery that the potent 5-HT_2B agonist norfenfluramine produces pulmonary arterial hypertension and subsequent heart valve damage. In animal studies, PRX-08066 has been found to reduce several key indicators of pulmonary arterial hypertension and improved cardiac output, with similar efficacy to established drugs for this condition such as

bosentan Bosentan, sold under the brand name Tracleer among others, is a dual endothelin receptor antagonist medication used in the treatment of pulmonary artery hypertension (PAH). Bosentan is available as film-coated tablets (62.5 mg or 125&nb ...

sildenafil Sildenafil, sold under the brand name Viagra among others, is a medication used to treat erectile dysfunction and pulmonary hypertension, pulmonary arterial hypertension. It is also sometimes used off-label for the treatment of certain sym ...

, beraprost and

iloprost Iloprost, sold under the brand name Ventavis among others, is a medication used to treat pulmonary arterial hypertension (PAH), scleroderma, Raynaud's phenomenon, frostbite, and other conditions in which the blood vessels are constricted and b ...

. It is also being researched for potential anti-cancer applications, due to its ability to inhibit

fibroblast A fibroblast is a type of cell (biology), biological cell typically with a spindle shape that synthesizes the extracellular matrix and collagen, produces the structural framework (Stroma (tissue), stroma) for animal Tissue (biology), tissues, and ...

activation.

References

5-HT2B antagonists {{nervous-system-drug-stub