IOA-244 is a Non-ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance

IOA-244 是一种非 ATP 竞争性、高选择性、耐受性好的 PI3K Delta 抑制剂,可靶向实体肿瘤并打破免疫耐受性

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作者:Zoë Johnson #, Chiara Tarantelli #, Elisa Civanelli, Luciano Cascione, Filippo Spriano, Amy Fraser, Pritom Shah, Tyzoon Nomanbhoy, Sara Napoli, Andrea Rinaldi, Karolina Niewola-Staszkowska, Michael Lahn, Dominique Perrin, Mathias Wenes, Denis Migliorini, Francesco Bertoni #, Lars van der Veen, Giusy

Significance

IOA-244 is a first-in-class non-ATP-competitive, PI3Kδ inhibitor with direct antitumor in vitro activity correlated with PI3Kδ expression. The ability to modulate T cells, in vivo antitumor activity in various models with limited toxicity in animal studies provides the rationale for the ongoing trials in patients with solid tumors and hematologic cancers.

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