Immunoconjugates targeting syndecan-1 expressing cells and use thereof

Abstract

Immunoconjugates comprising a targeting agent selectively targeting cell-surface expressed syndecan-1 and at least one effector molecule as well as in vitro and in vivo methods of using those immunocomjugates are disclosed. The effector molecule may have, in its native form, high non-selective cytotoxicity, but substantially no non-selective cytotoxicity when part of said immunoconjugate. Targeting agents include the antibody B-B4 as well as other agents that bind cell-surface expressed syndecan-1.

Description

BACKGROUND [0001] This invention pertains to immunoconjugates and their use in different indications. In particular, the present invention relates to immunoconjugates, the delivery of their effector molecule(s) to target sites and the site specific release of the effector molecule(s) in, at or near target cells, tissues and organs. More particularly, the present invention relates to immunoconjugates comprising one or more syndecan-1 targeting agent and highly potent effector molecules, which are attached to the targeting agent. The effector molecule is activated by cleavage / dissociation from the targeting agent portion of the immunoconjugate in, at or near the target cells, tissues or organs. [0002] The publications and other materials, including patents, used herein to illustrate the invention and, in particular, to provide additional details respecting the practice are incorporated by reference. For convenience, the publications are referenced in the following text by author and d...

AI Technical Summary

Benefits of technology

[0021] The present invention is also directed to a pharmaceutical composition comprising an effective amount of the immunoconjugate described above and one or more pharmaceutically acceptable excipients.

[0022] The present invention is also directed to a kit comprising, in separate containers, pharmaceutical compositions for use in combination to inhibit, delay and/or prevent the growth of tumors and/or spread of tumor cells, wherein one container comprises an effective amount of above described pharmaceutical composition, and wherein, a separate container comprises a second pharmaceutical composition comprising an effective amount of an agent for the inhibition, delay and/or prevention of the growth of tumors and/or spread of tumor cells, and one or more pharmaceutically acceptable excipients. The agent in said second pharmaceutical composition may be a chemotherapeutic agent or another immunoconjugate.

[0023] In one embodiment, the invention is directed to a method for treating, inhibiting, delaying and/or preventing the growth of tumor cells i

Problems solved by technology

In spite of considerable progress that has been achieved, many of those delivery systems for the treatment of various diseases, for example, the treatment of cancer, are still often ineffective or subject t

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