Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate
Catherine A. Evans(Infinity Pharmaceuticals (United States)), Tao Liu(Infinity Pharmaceuticals (United States)), André Lescarbeau(Infinity Pharmaceuticals (United States)), Somarajan Nair(Infinity Pharmaceuticals (United States)), Louis Grenier(Infinity Pharmaceuticals (United States)), Johan A. Pradeilles(Infinity Pharmaceuticals (United States)), Quentin Glenadel(Infinity Pharmaceuticals (United States)), Thomas T. Tibbitts(Infinity Pharmaceuticals (United States)), Ann Rowley(Infinity Pharmaceuticals (United States)), Jonathan P. DiNitto(Infinity Pharmaceuticals (United States)), Erin Brophy(Infinity Pharmaceuticals (United States)), Erin O’Hearn(Infinity Pharmaceuticals (United States)), Janid A. Ali(Infinity Pharmaceuticals (United States)), David G. Winkler(Infinity Pharmaceuticals (United States)), Stanley I. Goldstein(Infinity Pharmaceuticals (United States)), Patrick J. O’Hearn(Infinity Pharmaceuticals (United States)), Christian M. Martin(Infinity Pharmaceuticals (United States)), Jennifer Hoyt(Infinity Pharmaceuticals (United States)), John R. Soglia(Infinity Pharmaceuticals (United States)), Culver Cheung(Infinity Pharmaceuticals (United States)), Melissa Pink(Infinity Pharmaceuticals (United States)), Jennifer Proctor(Infinity Pharmaceuticals (United States)), Vito J. Palombella(Infinity Pharmaceuticals (United States)), Martin Tremblay(Infinity Pharmaceuticals (United States)), Alfredo Castro(Infinity Pharmaceuticals (United States))
Cited by 150Open Access
Abstract
Optimization of isoquinolinone PI3K inhibitors led to the discovery of a potent inhibitor of PI3K-γ (26 or IPI-549) with >100-fold selectivity over other lipid and protein kinases. IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration in vivo and is currently in Phase 1 clinical evaluation in subjects with advanced solid tumors.
Related Papers
No related papers found
Powered by citation graph analysis