PF-232798

PF‑232798 is a second-generation orally active small molecule CCR5 antagonist developed by Pfizer for the treatment of HIV infection. It was designed to improve upon the pharmacokinetic and resistance profiles of maraviroc (MVC), another CCR5 antagonist. Like MVC, it blocks HIV entry into host cells by binding to the transmembrane region of the chemokine receptor CCR5 but shows additional interactions at the ECL2 hinge region and retains activity against some MVC-resistant HIV strains. Clinical trials demonstrated potent anti-HIV activity and good oral absorption; however, development was discontinued after phase II trials[3][4][6][7].

Other names

849753-15-7UNII-63P7W7886UUNII63P7W7886UUNII 63P7W7886UCHEMBL1649931CHEMBL-1649931CHEMBL 1649931N-(S)-1-(3-Fluorophenyl)-3-(1R,3S,5S)-3-(5-isobutyryl-2-methyl-4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridin-1yl)-8azabicyclo[3.2.1]octan8yl)propyl)acetamide