Sloan-Kettering Institute for Cancer Research

Tri-Institutional Therapeutics Discovery Institute

Amaia Arruabarrena Aristorena

Peter T Meinke

Michael Andrew Foley

Kazuyoshi Aso

Mayako Michino

Maurizio Scaltriti

Daniel Alan Heller

Carles Monterrubio Martinez

Hiroki Takahagi

Jose Manuel Baselga Torres

Yusuke Sasaki

Yosef Shamay

Yasutomi Asano

Makoto Fushimi

The development of a new, targeted drug delivery paradigm coupled to improved PI3K inhibitors (e.g., PI3Kα inhibitors) represents a significant advance in cancer therapy. Provided herein are compounds, such as compounds of Formula (I) and (II), and pharmaceutically acceptable salts, hydrates, solvates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The compounds provided herein are PI3K (e.g., PI3Kα) inhibitors and are therefore useful for the treatment and/or prevention of various diseases (e.g., proliferative diseases such as cancer). Also provided herein are nanoparticles and nanogels (e.g., P-selectin targeting nanoparticles) comprising PI3K inhibitors, such a compound described herein. In certain embodiments, a nanoparticle or nanogel described herein encapsulates a compound described herein for targeting delivery to cancer cells or tumors.

PI3K inhibitors and uses thereof

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New York, NY, United States of America

Amaia Arruabarrena Aristorena