Trastuzumab-PEG-MMAE ADC

**Trastuzumab-PEG-MMAE ADC** is an investigational antibody-drug conjugate (ADC) comprising the HER2-targeting monoclonal antibody trastuzumab conjugated to the microtubule-disrupting payload monomethyl auristatin E (MMAE) via a PEG-containing peptide linker. It binds to **HER2** on tumor cells, undergoes receptor-mediated internalization, and releases MMAE intracellularly, which inhibits tubulin polymerization, leading to G2/M cell cycle arrest and apoptosis. Preclinical studies demonstrate approximately 3.4 MMAE payloads per antibody (DAR ~3.4), retained HER2 binding affinity comparable to unconjugated trastuzumab, and enhanced cytotoxicity against HER2-positive breast cancer cells (e.g., MDA-MB-453) versus HER2-negative cells (e.g., HEK-293), with improved antitumor activity and colony formation inhibition over trastuzumab alone.[1]

Other names

MMAE-trastuzumab ADC