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MRG002
- Development stage
- Phase 3
- Lead developer
- Lepu Biopharma
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
MRG002 is a novel antibody-drug conjugate (ADC) targeting HER2. It consists of a humanized anti-HER2 IgG1 monoclonal antibody (a sugar-modified trastuzumab), conjugated to the microtubule-disrupting agent monomethyl auristatin E (MMAE) via a cleavable valine-citrulline linker. The drug is designed to selectively deliver the cytotoxic payload to HER2-expressing tumor cells, leading to cell cycle arrest and apoptosis by inhibiting tubulin polymerization. Developed for various solid tumors with HER2 expression—including breast, gastric, biliary tract, urothelial, and esophageal cancers—MRG002 has shown promising efficacy in both HER2-positive and HER2-low expressing cancers in clinical trials[1][4][6][8].
- Other names
- MRG002MRG-002MRG 002
02
Targets
ERBB2 (Erb-b2 receptor tyrosine kinase 2)TUBB (Tubulin (alpha and beta subunits))
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