Timapiprant1 is a highly potent and selective CRTH2 antagonist which is active on both the recombinant and native human receptor.
Preclinical studies have highlighted the following properties of timapiprant:
The Atopix lead compound timapiprant is effective in improving lung function and symptoms in patients with atopic eosinophilic asthma. This group represents 40-50% of all asthmatics and the magnitude of improvement in the responder population is equivalent to high dose inhaled corticosteroids.
Timapiprant has also been shown to reduce both nasal and eye symptoms in allergic subjects exposed to grass pollen. Of particular interest is the ability of timapiprant to reduce the rate of respiratory infections, an effect related to reduction in Th2 immunity which has a damaging effect on host defence. This will be studied by Professor Sebastian Johnston at the National Heart and Lung Institute, Imperial College London, who won a £1.3M Biomedical Catalyst Grant for this innovative research.
Timapiprant has also demonstrated an excellent safety profile in around 800 subjects exposed drug and no safety issues have been highlighted in long term toxicology.