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pertuzumab emtansine
- Development stage
- Discontinued
- Lead developer
- Genentech
- Modality
- Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
- Administration
- Intravenous
01
Overview
Pertuzumab emtansine (P-DM1) is an experimental antibody-drug conjugate (ADC) consisting of the HER2-targeted monoclonal antibody pertuzumab covalently linked to the cytotoxic maytansinoid DM1 (mertansine) via a non-cleavable thioether linker (MCC). While pertuzumab binds to subdomain II of the HER2 extracellular domain to inhibit receptor dimerization, the DM1 payload acts as a microtubule-disrupting agent. Upon binding to HER2-expressing cancer cells, the ADC is internalized and degraded in lysosomes, releasing active DM1 metabolites that induce cell cycle arrest and apoptosis. Developed by Genentech, P-DM1 was evaluated in early-phase clinical trials for HER2-positive metastatic breast cancer but development was largely superseded by trastuzumab emtansine (T-DM1).
- Other names
- pertuzumab-DM1pertuzumab-DM-1pertuzumab-DM 1P-DM1P-DM-1P-DM 1pertuzumab emtansine
02
Targets
TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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