Cantuzumab mertansine (SB-408075; huC242-DM1) is an antibody-drug conjugate investigated to treat colorectal cancer and other types of cancer.

[1] It is a humanized monoclonal antibody, cantuzumab (huC242) linked to a cytotoxic agent, mertansine (DM1).

After the huC242 mab binds to the external domain of CanAg, the cantuzumab mertansine-CanAg complex is internalized, and the DM1 molecules are released intracellularly by cleavage of the DM1-huC242 disulfide bonds.

[3] Three phase I clinical studies had reported results by 2003.

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