Potent conjugates and hydrophilic linkers

US9150649B2 · kind B2 · utility

Assignee

• IMMUNOGEN, INC. · US

Inventors

• Rajeeva Singh · Framingham, US
• Yelena Kovtun · Stow, US
• Sharon D. Wilhelm · Arlington, US
• Ravi V. J. Chari · Newton, US

Key dates

• Filing date: Oct 6, 2009
• Grant date: Oct 6, 2015
• Expiry date: Jul 12, 2031

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02A50/30
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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.