Cantuzumab mertansine explained

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).^[2] It was developed by ImmunoGen.

Mechanism

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]

Clinical trials

Three phase I clinical studies had reported results by 2003.^[4] By 2005, clinical development had been suspended.^[5]

See also

• Cantuzumab ravtansine

Notes and References

1. http://www.ama-assn.org/ama1/pub/upload/mm/365/cantuzumab_mer.doc Statement On A Nonproprietary Name Adopted By The Usan Council - Cantuzumab mertansine
2. Rodon J, Garrison M, Hammond LA, de Bono J, Smith L, Forero L, Hao D, Takimoto C, Lambert JM, Pandite L, Howard M, Xie H, Tolcher AW . 6 . Cantuzumab mertansine in a three-times a week schedule: a phase I and pharmacokinetic study . Cancer Chemotherapy and Pharmacology . 62 . 5 . 911–9 . October 2008 . 18301896 . 10.1007/s00280-007-0672-8 . 5829870 .
3. Helft PR, Schilsky RL, Hoke FJ, Williams D, Kindler HL, Sprague E, DeWitte M, Martino HK, Erickson J, Pandite L, Russo M, Lambert JM, Howard M, Ratain MJ . 6 . A phase I study of cantuzumab mertansine administered as a single intravenous infusion once weekly in patients with advanced solid tumors . Clinical Cancer Research . 10 . 13 . 4363–8 . July 2004 . 15240523 . 10.1158/1078-0432.CCR-04-0088 .
4. Smith SV . Technology evaluation: cantuzumab mertansine, ImmunoGen . Current Opinion in Molecular Therapeutics . 6 . 6 . 666–74 . December 2004 . 15663331 .
5. Web site: Cantuzumab mertansine . Springer Nature Switzerland AG .