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cantuzumab mertansine
- Development stage
- Discontinued
- Lead developer
- ImmunoGen
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Cantuzumab mertansine is an antibody-drug conjugate composed of a humanized monoclonal antibody, cantuzumab (huC242), linked to the cytotoxic agent mertansine (DM1). The antibody targets CanAg, a tumor-associated antigen (a sialylated carbohydrate epitope of MUC1) expressed on various solid tumors, including colorectal cancer. Upon binding to CanAg on tumor cells, the conjugate is internalized and DM1 is released intracellularly by cleavage of disulfide bonds. DM1 acts as a tubulin inhibitor, disrupting microtubule assembly and inducing cell death. Cantuzumab mertansine was developed by ImmunoGen for targeted therapy in cancers expressing CanAg but its clinical development was suspended after early-phase trials due to toxicity concerns and limited efficacy[1][3][4][5][6].
- Other names
- SB-408075SB408075SB 408075huC242-DM1huC-242-DM1huC 242-DM1
02
Targets
CanAg (Cancer-associated antigen)TUBB (Tubulin (alpha and beta subunits))
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