Akzo N.v.

Akzo Nobel N.v.

Per Immune Holdings, Inc.

Chong-Ho Kim

Reinhard Bredehorst

Nicholas Pomato

Carl-Wilhelm Ernst Vogel

Richard P McCabe

Gregory Alan Hawkins

Gregory A Hawkins

A method for in-vivo targeting a functional moiety in a patient by administering a targeting moiety coupled to an affinity component, wherein the targeting moiety has affinity for binding sites in a target area, and administering a binding partner to the affinity component coupled to a functional moiety to localize the functional moiety in the target area. Preferably the targeting moiety is an antibody and the functional moiety is a radiometal when performing in vivo imaging or therapy. The affinity component may be a novel methotrexate analog. Preferably, the affinity component is thermo-stabilized.

In vivo binding pair pretargeting

A method for in-vivo targeting a functional moiety in a patient by administering a targeting moiety coupled to an affinity component, wherein the targeting moiety has affinity for binding sites in a target area, and administering a binding partner to the affinity component coupled to a functional moiety to localize the functional moiety in the target area. Preferably the targeting moiety is an antibody and the functional moiety is a radiometal when performing in vivo imaging or therapy. The affinity component may be a novel methotrexate analog.

A method for site-specific in-vivo activation of a prodrug in an animal using an activator-targeting moiety conjugate to localize an activator at a predetermined site of use and a prodrug compound that is converted to an active drug in the presence of the activator. In the preferred embodiment, the targeting moiety, the activator, and the prodrug demonstrate little or no immunogenicity in the animal being treated. The targeting moiety is relatively specific for binding to the target tissue than to non-target tissue. The activator is not found or present in only small amounts in circulation or in non-target tissue, does not have a substrate for its activity in circulation or in non-target tissue, can be linked to the targeting moiety, and is capable of converting the prodrug to an active drug. The prodrug is selected for its ability to exert a cytotoxic activity on the target tissue after conversion by the activator.

Site specific in vivo activation of therapeutic drugs

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Rockville, MD, United States of America

Chong-Ho Kim