Tolero Pharmaceuticals, Inc.

Sumitomo Pharma Oncology, Inc.

Sumitomo Dainippon Pharma Oncology, Inc.

Clifford J Whatcott

David J Bearss

Steven L Warner

Adam Siddiqui-Jain

Wontak Kim

Peter W Peterson

Lars Mouritsen

Jeyaprakashnarayanan Seenisamy

Jason Marc Foulks

Paul Flynn

Yuka Arikawa

Yuji Fujiwara

Stephen Patrick Anthony

Provided herein is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein values for the variables (e.g., X, X, R, R, R, R, R, R, R, m, n) are as described herein. Compounds of Formula I, pharmaceutically acceptable salts thereof, pharmaceutical compositions of either of the foregoing, and combinations of any of the foregoing can be used to treat tyrosine kinase non-receptor 1 (TNK1)-mediated diseases, disorders and conditions.

Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof

Methods for treating BCL-2 inhibitor-resistant cancer in subjects using an MCL-1 inhibitor as well as compositions associated with the same are disclosed.

Treatment regimen for cancers that are insensitive to BCL-2 inhibitors using the MCL-1 inhibitor alvocidib

Methods for treating a disease in a subject in need thereof by administering an ACVR1 inhibitor having the following formula (I) are disclosed: including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R, R, and Rare as defined herein. Subjects that may benefit from treatment may have mutations in their ACVR1 gene. Various diseases may be treated using the described methods, including cancers (e.g., diffuse intrinsic pontine glioma (DIPG)) and genetic disorders (e.g., fibrodysplasia ossificans progressiva (FOP)).

Methods for treating diseases associated with abnormal ACVR1 expression and ACVR1 inhibitors for use in the same

Combination therapies for treatment of cancer are provided. The disclosed methods comprise administration of a cyclin-dependent kinase inhibitor and a DNA methyltransferase inhibitor to a mammal in need thereof.

Combination therapies for treatment of cancer

The present disclosure is generally directed to profiling peptides, compositions, and kits, as well as methods of use thereof. The profiling peptides comprise an Mcl-1 binding domain, and optionally a cellular uptake moiety. The methods of using such profiling peptides include predicting sensitivity of a cancer, selecting a treatment, treating a cancer, producing a sensitivity profile, and the like.

Profiling peptides and methods for sensitivity profiling

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West Jordan, UT, United States of America

Clifford J Whatcott