Fc Engineered Anti-Human HER2 Therapeutic Antibody, a CDC-Enhanced Biobetter [Lot: CB20-PZ06] (CAT#: Biobet-C006ZP) Datasheet

ERBB2

erb-b2 receptor tyrosine kinase 2

This gene encodes a member of the epidermal growth factor (EGF) receptor family of receptor tyrosine kinases. This protein has no ligand binding domain of its own and therefore cannot bind growth factors. However, it does bind tightly to other ligand-bound EGF receptor family members to form a heterodimer, stabilizing ligand binding and enhancing kinase-mediated activation of downstream signalling pathways, such as those involving mitogen-activated protein kinase and phosphatidylinositol-3 kinase. Allelic variations at amino acid positions 654 and 655 of isoform a (positions 624 and 625 of isoform b) have been reported, with the most common allele, Ile654/Ile655, shown here. Amplification and/or overexpression of this gene has been reported in numerous cancers, including breast and ovarian tumors. Alternative splicing results in several additional transcript variants, some encoding different isoforms and others that have not been fully characterized.

NEU; NGL; HER2; TKR1; CD340; HER-2; MLN 19; HER-2/neu

Protein Based Therapies
Monoclonal antibody (mAb)

Whole Humanized Antibody

Trastuzumab emtansine is an antibody drug conjugate (ADC) consisting of the humanized monoclonal antibody trastuzumab (Herceptin) covalently linked to the cytotoxic agent DM1. The United States Food and Drug Administration (FDA) approved trastuzumab emtansine for female patients with trastuzumab-resistant advanced HER2 positive breast cancer on February 22, 2013.

HER2-positive breast cancer; metastatic breast cancer; Refractory, metastatic Non small cell lung cancer

Ado-trastuzumab
Ado-trastuzumab emtansine
T-DM1
Trastuzumab emtansine
Trastuzumab-DM1
Trastuzumab-MCC-DM1

Trastuzumab Emtansine is a HER2 antibody drug conjugate. The antibody part is humanized anti-HER2 IgG1 trastuzumab, and the drug part is DM1, which is a maytansin derivative that inhibits microtubules. Emtansine is a generic name for 4- [N-maleimidomethyl] cyclohexane-1-carboxylic acid ester (MCC) covalently linking linker and DM1, which is produced through chemical synthesis. Trastuzumab Emtansine binds to subdomain IV of the HER2 receptor and enters the cell through receptor-mediated endocytosis. DM1 binds to tubulin in microtubules and inhibits microtubule function, resulting in cell arrest and apoptosis. Similarly, similar to trastuzumab, in vitro antibody-dependent cytotoxicity and inhibition of HER2 receptor signaling are mediated by the antibody portion of trastuzumab emtansine.

It is suitable for treating early HER2-positive early breast cancer or metastatic breast cancer that substantially overexpresses HER2. Approved for gastric cancer, metastatic gastroesophageal junction adenocarcinoma, and metastatic adenocarcinoma of the gastro-esophageal junction, provided that these cancers overexpress HER2.