The
purine- and
pyrimidine-sensitive P2Y receptors belong to the large group of
G-protein-coupled receptors that are the target of approximately one-third of the
pharmaceutical drugs used in the clinic today. It is therefore not unexpected that the P2Y receptors could be useful targets for
drug development. This chapter will discuss P2Y receptor-based
therapies currently used, in development and possible future developments. The
platelet inhibitors blocking the
ADP-receptor P2Y(12) reduce
myocardial infarction,
stroke, and mortality in patients with
cardiovascular disease.
Clopidogrel (
Plavix) was for many years the second most selling
drug in the world. The improved P2Y(12) inhibitors
prasugrel,
ticagrelor, and
elinogrel are now entering the clinic with even more pronounced protective effects. The
UTP-activated P2Y(2) receptor stimulates ciliary movement and secretion from epithelial cells.
Cystic fibrosis is a monogenetic disease where reduced
chloride ion secretion results in a severe
lung disease and early death. No specific treatment has been available, but the P2Y(2) agonist Denufosol has been shown to improve lung function and is expected to be introduced as treatment for
cystic fibrosis soon. In preclinical studies, there are indications that P2Y receptors can be important for diabetes,
osteoporosis, cardiovascular, and atherosclerotic disease. In conclusion, P2Y receptors are important for the health of humans for many diseases, and we can expect even more beneficial drugs targeting P2Y receptors in the future.