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bivatuzumab mertansine
- Development stage
- Phase 1
- Lead developer
- Boehringer Ingelheim
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Bivatuzumab mertansine is an antibody-drug conjugate composed of bivatuzumab, a humanized monoclonal antibody targeting the CD44 variant 6 (CD44v6) antigen, chemically linked to the cytotoxic agent mertansine (DM1). The drug is designed for targeted treatment of cancers expressing CD44v6, such as squamous cell carcinoma. Upon binding to CD44v6 on tumor cells, the conjugate is internalized and releases mertansine intracellularly by cleavage of disulfide bonds. Mertansine then inhibits tubulin polymerization, disrupting microtubule assembly and leading to mitotic arrest and tumor cell death. Bivatuzumab mertansine was developed primarily for head and neck cancer as well as breast cancer but development was discontinued after phase I trials due to toxicity concerns[1][4][5][6].
- Other names
- bivatuzumab mertansine
02
Targets
CD44v6 (CD44 variant isoform 6)TUBB (Tubulin (alpha and beta subunits))
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