Eisai R&d Management Co., Ltd.

Lihua Yu

Silvia Buonamici

Peter G Smith

Ping Zhu

Ermira Pazolli

Michael W Seiler

Sudeep Prajapati

Xiang Liu

James Palacino

Kian Huat Lim

Eunice Sun Park

Dominic J Reynolds

Nathan Elliott Fishkin

Andrew Cook

Thiwanka Samarakoon

Shelby Ellery

Megan Sheehan

Zhenhua Wu

Nicholas Calandra

Yonghong Xiao

John JianShi Wang

Guo Zhu Zheng

Yoshihiko Kotake

Gregg F Keaney

Kazunobu Kira

Parcharee Tivitmahaisoon

Norio Murai

Yoshiharu Mizui

Baudouin Gerard

Satoshi Nagao

Masayuki Miyano

Jacob D Feala

Michael P Thomas

Regina Mikie Kanada Sonobe

Nicholas C Gearhart

Kenzo Arai

Betty Chan

Shouyong Peng

Marco Peter Fekkes

Atsushi Endo

Arani Chanda

Evan Barry

Regina Mikie Kanada Sonabe

Regina Kanada Sonobe

Sundeep Prajapati

Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.

Splicing modulator antibody-drug conjugates and methods of use

This disclosure relates to methods for the treatment of neoplastic disorders by administering Compound 1, or a pharmaceutically acceptably salt thereof, on its own and/or as part of a conjugate or composition, and inducing production of at least one neoantigen.

Methods of using splicing modulators

Splice variants associated with neomorphic SF3B1 mutations are described herein. This application also relates to methods of detecting the described splice variants, and uses for diagnosing cancer, evaluating modulators of SF3B1, and methods of treating cancer associated with mutations in SF3B1.

Splice variants associated with neomorphic SF3B1 mutants

The present disclosure provides a novel solid state form of pladienolide pyridine compounds having Formula I, compositions comprising at least one such solid state form, and methods of preparation and use and the same. The novel solid state form of pladienolide pyridine compounds may be useful in the treatment of cancer, such as, for example, cancers in which agents that target the spliceosome and mutations therein are known to be useful. 

Crystalline form of (2S,3S,6S,7R,10R,E)-7,10-dihydroxy-3,7-dimethyl-12-oxo-2-((R,2E,4E)-6-(piridin-2-yl)hepta-2,4-dien-2-yl)oxacyclododec-4-en-6-yl-4-methylpiperazine-1-carboxylate and methods of use thereof

The present invention provides novel pladienolide pyridine compounds, pharmaceutical compositions containing such compounds, and methods for using the compounds as therapeutic agents. These compounds may be useful in the treatment of cancer, particularly cancers in which agents that target the spliceosome and mutations therein are known to be useful.

Pladienolide pyridine compounds and methods of use

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Acton, MA, United States of America

Lihua Yu