The General Hospital Corporation

Memorial Sloan Kettering Cancer Center

Sloan-kettering Institute for Cancer Research

Tri-institutional Therapeutics Discovery Institute

Maurizio Scaltriti

Jose Baselga

Peter T Meinke

Michael Andrew Foley

Mayako Michino

Pau Castel

Yosef Shamay

Makoto Fushimi

Daniel Alan Heller

Carles Monterrubio Martinez

Amaia Arruabarrena Aristorena

Hiroki Takahagi

Jose Manuel Baselga Torres

Yusuke Sasaki

Yasutomi Asano

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

The present invention relates to methods and compositions for inhibiting growth and proliferation of cancer cells resistant to PI3K inhibition using a combination of PDK1, SGK1 and PI3K inhibitors. The present invention is also directed to methods of treating cancer in a subject exhibiting cancer cells resistant to PI3K inhibition, comprising administering inhibitors of PI3K in combination with inhibitors of PDK1 and/or SGK1 to the subject.

Combination therapy using PDK1 and PI3K inhibitors

The invention provides combinations comprising GDC-0068 or GDC-0941, or a pharmaceutically acceptable salt thereof and ME-HD7945A. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer (e.g., triple negative breast cancer).

Combinations of a PI3K/AKT inhibitor compound with an HER3/EGFR inhibitor compound and use thereof in the treatment of a hyperproliferative disorder

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New York, NY, United States of America

Maurizio Scaltriti