Cantuzumab ravtansine (IMGN242; huC242-DM4), an ADC, is a humanized monoclonal antibody, huC242, covalently linked via a disulfide bond to DM4 (DM4 ). Cantuzumab ravtansine has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts.
Cantuzumab ravtansine (huC242-DM4; 5 days) shows cytotoxic effect in CanAg-positive SNU16 gastric cancer cells[2].
Cantuzumab ravtansine (huC242-DM4; i.v; 3.4 mg/kg; a single dose) causes complete regression of the tumors in SCID mice bearing N87 human gastric tumor xenografts, with significant tumor regression observed at a dose below 2 mg/kg[1]. Cantuzumab ravtansine (huC242-DM4) is also curative in mice bearing human colon tumor xenografts of HT29 and COLO 205 cells, at doses that were non-toxic[1].
References:
[1]. Robert J. Lutz, et al. HuC242-DM4, an antibody-maytansinoid conjugate with superior preclinical activity in human CanAg-positive tumor xenograft models in SCID mice. Cancer Res (2005) 65 (9_Supplement): 334-335. [2]. Olga Ab, et al. Activity of huC242-DM4, an antibody-cytotoxic agent conjugate, used in combination with anti-neoplastic agents against gastric cancer cells in culture. Mol Cancer Ther (2007) 6 (11_Supplement): A127.