PRX-08066 is a drug discovered and developed by Predix (later Epix) Pharmaceuticals
ale S. Dhanoa et al. Patent US 7,030,240 B2 which acts as a potent and selective
antagonist at the
serotonin 5-HT2B receptor
Receptor may refer to:
* Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse
*Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a ...
, with a 5-HT
2B binding affinity (Ki) of 3.4nM, and high selectivity over the closely related
5-HT2A and
5-HT2C receptors and other receptor targets. PRX-08066 and other selective 5-HT
2B antagonists are being researched for the treatment of
pulmonary arterial hypertension, following the discovery that the potent 5-HT
2B agonist
norfenfluramine
Norfenfluramine, or 3-trifluoromethylamphetamine, is a never-marketed drug of the amphetamine family that behaves as a serotonin and norepinephrine releasing agent and potent 5-HT2A, 5-HT2B, and 5-HT2C agonist. The action of norfenfluramine on ...
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 and Safebo 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 o ...
,
sildenafil,
beraprost and
iloprost
Iloprost is a medication used to treat pulmonary arterial hypertension (PAH), scleroderma, Raynaud's phenomenon and other diseases in which the blood vessels are constricted and blood cannot flow to the tissues. This damages the tissues and cau ...
.
It is also being researched for potential anti-cancer applications, due to its ability to inhibit
fibroblast activation.
References
5-HT2B antagonists
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