Cantuzumab mertansine

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.

Cantuzumab mertansine
Monoclonal antibody
TypeWhole antibody
SourceHumanized (from mouse)
TargetMUC1
Clinical data
ATC code
  • none
Identifiers
CAS Number
ChemSpider
  • none
UNII
 NY (what is this?)  (verify)

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]

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See also

References
  1. Statement On A Nonproprietary Name Adopted By The Usan Council - Cantuzumab mertansine, American Medical Association. Archived 2011-06-04 at the Wayback Machine
  2. Rodon J, Garrison M, Hammond LA, de Bono J, Smith L, Forero L, et al. (October 2008). "Cantuzumab mertansine in a three-times a week schedule: a phase I and pharmacokinetic study". Cancer Chemotherapy and Pharmacology. 62 (5): 911–9. doi:10.1007/s00280-007-0672-8. PMID 18301896.
  3. Helft PR, Schilsky RL, Hoke FJ, Williams D, Kindler HL, Sprague E, et al. (July 2004). "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. doi:10.1158/1078-0432.CCR-04-0088. PMID 15240523.
  4. Smith SV (December 2004). "Technology evaluation: cantuzumab mertansine, ImmunoGen". Current Opinion in Molecular Therapeutics. 6 (6): 666–74. PMID 15663331.
  5. "Cantuzumab mertansine". Springer Nature Switzerland AG.
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