Immunogen, Inc.

Rajeeva Singh

Ravi V J Chari

Yelena V Kovtun

Robert Yongxin Zhao

Wayne Charles Widdison

Brenda A Kellogg

Daniel J Tavares

Nancy E Dagdigian

Michael Louis Miller

Wei Li

Nathan Elliott Fishkin

Ravi Chari

Lingyun Rui

Peter U Park

Thomas D Chittenden

Julianto Setiady

Sharon D Wilhelm

Ravi VJ Chari

Yelena Kovtun

Michael Miller

This invention describes a method of conjugating a cell binding agent such as an antibody with an effector group (e.g., a cytotoxic agent) or a reporter group (e.g., a radionuclide), whereby the reporter or effector group is first reacted with a bifunctional linker and the mixture is then used without purification for the conjugation reaction with the cell binding agent. The method described in this invention is advantageous for preparation of stably-linked conjugates of cell binding agents, such as antibodies with effector or reporter groups. This conjugation method provides in high yields conjugates of high purity and homogeneity that are without inter-chain cross-linking and inactivated linker residues.

Methods for preparing a purified maytansinoid conjugate in a solution

Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.

Cross-linkers and their uses

Methods for preparing antibody-drug conjugates

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

Conjugation methods

Novel anti-cancer agents, including, but not limited to, antibodies and immunoconjugates, that bind to EGFR are provided. Methods of using the agents, antibodies, or immunoconjugates, such as methods of inhibiting tumor growth are further provided.

Non-antagonistic EGFR-binding molecules and immunoconjugates thereof

Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.

Potent conjugates and hydrophilic linkers

Methods for preparation of antibody-maytansinoid conjugates

Growing community of inventors

Framingham, MA, United States of America

Rajeeva Singh