PF-610355

PF-610355 is a long-acting inhaled β2-adrenoreceptor agonist, with an EC50 of 0.26 nM. PF-610355 has the potential for the study of asthma and COPD[1].

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Inflammation/Immunology

PF-610355 is a long-acting (once daily) inhaled β2-adrenoreceptor agonist. PF-610355 has low oral bioavailability due to poor absorption through the gut lumen and high first pass metabolism and warranted further progression. PF-610355 has a short half-life (Clint = 33 (μL/min)/mg) that suggested an unbound intrinsic clearance of >10000 (mL/min)/kg. PF-610355 exhibits an ideal pharmacokinetic profile for an inhaled agent[1].

[1]. Glossop PA, et al. Inhalation by design: novel ultra-long-acting β(2)-adrenoreceptor agonists for inhaled once-daily treatment of asthma and chronic obstructive pulmonary disease that utilize a sulfonamide agonist headgroup. J Med Chem. 2010 Sep 23;53(18):6640-52.

[2]. Fuso L, et al. Long-acting beta-agonists and their association with inhaled corticosteroids in COPD. Curr Med Chem. 2013;20(12):1477-95.