1312684-87-9Relevant articles and documents
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ)
Yue, Eddy W.,Li, Yun-Long,Douty, Brent,He, Chunhong,Mei, Song,Wayland, Brian,Maduskuie, Thomas,Falahatpisheh, Nikoo,Sparks, Richard B.,Polam, Padmaja,Zhu, Wenyu,Glenn, Joseph,Feng, Hao,Zhang, Ke,Li, Yanlong,He, Xin,Katiyar, Kamna,Covington, Maryanne,Feldman, Patricia,Shin, Niu,Wang, Kathy He,Diamond, Sharon,Li, Yu,Koblish, Holly K.,Hall, Leslie,Scherle, Peggy,Yeleswaram, Swamy,Xue, Chu-Biao,Metcalf, Brian,Combs, Andrew P.,Yao, Wenqing
, p. 1554 - 1560 (2019/11/11)
A medicinal chemistry effort focused on identifying a structurally diverse candidate for phosphoinositide 3-kinase delta (PI3Kδ) led to the discovery of clinical candidate INCB050465 (20, parsaclisib). The unique structure of 20 contains a pyrazolopyrimidine hinge-binder in place of a purine motif that is present in other PI3Kδinhibitors, such as idelalisib (1), duvelisib (2), and INCB040093 (3, dezapelisib). Parsaclisib (20) is a potent and highly selective inhibitor of PI3Kδwith drug-like ADME properties that exhibited an excellent in vivo profile as demonstrated through pharmacokinetic studies in rats, dogs, and monkeys and through pharmacodynamic and efficacy studies in a mouse Pfeiffer xenograft model.
