revefenacin

Description: Revefenacin (formerly known as TD-4208; GSK-1160724; trade name: Yupelri) is a long-acting, potent mAChR (muscarinic acetylcholine receptor) antagonist with a high affinity on M3 receptor with a Ki of 0.18 nM. It has the potential to be used for the treatment of respiratory disease. On November 8th 2018, Revefenacin gained FDA approval to treat patients with chronic obstructive pulmonary disease (COPD). Previously, Tiotropium was the only once-daily, long-acting muscarinic antagonist (LAMA) approved in the United States and other countries for the treatment of COPD. Glycopyrronium has shown promise as a LAMA and was recently approved for once-daily maintenance treatment of COPD in the European Union. In conclusion, Revefenacin has the potential to be a long-acting bronchodilator for once-daily treatment of respiratory diseases. Its greater functional selectivity for the lung in preclinical models may translate to an improved tolerability profile compared with marketed muscarinic receptor antagonists.

References: J Pharmacol Exp Ther. 2013 Aug; 346(2):241-50.