Jesse C Nussbaum, Azher Hussain, Peter Butera, Anthony P Ford, Michael M Kitt, Edward A O'Neill, Steven Smith, Gabriel Vargas, Terry O'Reilly, Chris Wynne, S Aubrey Stoch, Marian Iwamoto
Gefapixant (MK-7264, RO4926219, AF-219) is a first-in-class P2X3 antagonists being developed to treat refractory or unexplained chronic cough. The initial single- and multiple-dose safety, tolerability, and pharmacokinetics of gefapixant at doses ranging from 7.5 to 1800 mg were assessed in four clinical trials. Following single-dose administration of 10-450 mg, the pharmacokinetic (PK) profile of gefapixant in plasma and urine demonstrated low inter-subject variability and a dose-proportional exposure. Following administration of multiple doses twice daily, the plasma exposures were dose-proportional at doses ranging from 7...
April 23, 2024: Journal of Clinical Pharmacology