Portal de Periódicos da CAPES

Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate

2016; American Chemical Society; Volume: 7; Issue: 9 Linguagem: Inglês

10.1021/acsmedchemlett.6b00238

1948-5875

Catherine A. Evans, Tao Liu, André Lescarbeau, Somarajan Nair, Louis Grenier, Johan A. Pradeilles, Quentin Glenadel, Thomas T. Tibbitts, Ann Rowley, Jonathan P. DiNitto, Erin Brophy, Erin O’Hearn, Janid A. Ali, David G. Winkler, Stanley I. Goldstein, Patrick J. O’Hearn, Christian M. Martin, Jennifer Hoyt, John R. Soglia, Culver Cheung, Melissa Pink, Jennifer Proctor, Vito J. Palombella, Martin Tremblay, Alfredo Castro,

Multiple Myeloma Research and Treatments

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.