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caxmotabart entudotin
- Development stage
- Phase 3
- Lead developer
- Fosun Pharma
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Caxmotabart entudotin (FS-1502) is a HER2-targeting antibody-drug conjugate (ADC) developed by Shanghai Fosun Pharmaceutical Industrial Development Co. Ltd. in collaboration with LigaChem Biosciences and Iksuda Therapeutics. The molecule consists of a humanized anti-HER2 monoclonal antibody, derived from trastuzumab, conjugated to the potent antimitotic agent monomethyl auristatin F (MMAF) via a cancer-selective, cleavable β-glucuronide linker. This design utilizes site-specific conjugation technology to ensure a stable drug-to-antibody ratio. Upon binding to HER2-expressing tumor cells and subsequent internalization, the linker is cleaved by β-glucuronidase in the lysosomal compartment, releasing MMAF to inhibit tubulin polymerization and induce cell cycle arrest and apoptosis. It is currently being evaluated in clinical trials for the treatment of HER2-positive metastatic breast cancer and other HER2-expressing advanced solid tumors.
- Other names
- caxmotabart entudotin
02
Targets
TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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