Immunogen, Inc.

Eisai R&d Management Co., Ltd.

Nathan Elliott Fishkin

Michael Louis Miller

Wei Li

Ravi V J Chari

Robert Yongxin Zhao

Ping Zhu

Ermira Pazolli

James Palacino

Thiwanka Samarakoon

Dominic J Reynolds

Andrew Cook

Sudeep Prajapati

Silvia Buonamici

Lihua Yu

Xiang Liu

Shelby Ellery

Megan Sheehan

Yonghong Xiao

Nicholas Calandra

Zhenhua Wu

Rajeeva Singh

Peter G Smith

Michael W Seiler

Shouyong Peng

Daniel J Tavares

Lingyun Rui

Manami Shizuka

Luke B Harris

Juan C Almagro

Ravi Chari

Ravi Vj Chari

Ryan Henry

Peter Smith

Ravi VJ Chari

Michael Miller

SPLICING MODULATOR ANTIBODY-DRUG CONJUGATES AND METHODS OF USE

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

Antibodies, antigen-binding fragments, and conjugates (e.g., antibody-drug conjugates (ADCs) such as those comprising a splicing modulator) that bind to BCMA are disclosed. The disclosure further relates to methods and compositions for use in the treatment of cancer by administering a composition provided herein.

Anti-BCMA antibody-drug conjugates and methods of use

The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

Cytotoxic benzodiazepine derivatives

The invention relates to novel cell-binding agent-cytotoxic agent conjugates, wherein the cell-binding agent (CBA) is covalently linked to the cytotoxic agent through an aldehyde group obtained from oxidation of a 2-hydroxyethylamine moiety on the CBA. The invention also provides methods of preparing the conjugates of the present invention. The invention further provides composition and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the conjugates of the invention.

Conjugates comprising cell-binding agents and cytotoxic agents

The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

Benzodiazepine derivatives

The present invention is directed to methods of preparing a conjugate of a cell-binding agent and a drug (such as a cytotoxic compound). The methods comprise the use of an imine reactive compound to enable efficient conjugations of cytotoxic compounds with cell binding agents.

Methods of preparation of conjugates

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Weymouth, MA, United States of America

Nathan Elliott Fishkin