PRX-08066 is a drug discovered and developed by Predix (later Epix) Pharmaceuticals [Dale S. Dhanoa et al. Patent US 7,030,240 B2], which acts as a potent and selective
antagonist at the
serotonin5-HT2Breceptor, with a 5-HT2Bbinding 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-HT2B antagonists are being researched for the treatment of
pulmonary arterial hypertension, following the discovery that the potent 5-HT2B 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,
sildenafil,
beraprost and
iloprost.
[1] It is also being researched for potential anti-cancer applications, due to its ability to inhibit
fibroblast activation.[2]
References
^Porvasnik SL, Germain S, Embury J, Gannon KS, Jacques V, Murray J, Byrne BJ, Shacham S, Al-Mousily F (August 2010). "PRX-08066, a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats". The Journal of Pharmacology and Experimental Therapeutics. 334 (2): 364–72.
doi:
10.1124/jpet.109.165001.
PMID20430844.
S2CID206500649.
PRX-08066 is a drug discovered and developed by Predix (later Epix) Pharmaceuticals [Dale S. Dhanoa et al. Patent US 7,030,240 B2], which acts as a potent and selective
antagonist at the
serotonin5-HT2Breceptor, with a 5-HT2Bbinding 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-HT2B antagonists are being researched for the treatment of
pulmonary arterial hypertension, following the discovery that the potent 5-HT2B 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,
sildenafil,
beraprost and
iloprost.
[1] It is also being researched for potential anti-cancer applications, due to its ability to inhibit
fibroblast activation.[2]
References
^Porvasnik SL, Germain S, Embury J, Gannon KS, Jacques V, Murray J, Byrne BJ, Shacham S, Al-Mousily F (August 2010). "PRX-08066, a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats". The Journal of Pharmacology and Experimental Therapeutics. 334 (2): 364–72.
doi:
10.1124/jpet.109.165001.
PMID20430844.
S2CID206500649.