This ADC product is comprised of an anti-EGFR monoclonal antibody (cetuximab) conjugated via a EDC/NHS linker to methotrexate. The methotrexate is targeted to certain cancers by immunerecognition and delivered into cancer cells via receptor mediated endocytosis.
The protein encoded by this gene is a transmembrane glycoprotein that is a member of the protein kinase superfamily. This protein is a receptor for members of the epidermal growth factor family. EGFR is a cell surface protein that binds to epidermal growth factor. Binding of the protein to a ligand induces receptor dimerization and tyrosine autophosphorylation and leads to cell proliferation. Mutations in this gene are associated with lung cancer. Multiple alternatively spliced transcript variants that encode different protein isoforms have been found for this gene.
Acid-labile linkers, belonging to chemically cleavable linkers, are designed based on a pH-dependent release mechanism and remain intact during systemic circulation in the blood's neutral pH environment (pH 7.3–7.5) but to undergo hydrolysis and release drug once the ADC is internalized into mildly acidic endosomal (pH 5.0–6.5) and lysosomal (pH 4.5–5.0) compartments of the cell.
ADC payload drug
Name
methotrexate (MTX)
Description
Methotrexate (MTX) and formerly known as amethopterin, is an antimetabolite and antifolate drug.It is used in treatment of cancer, autoimmune diseases, ectopic pregnancy, and for the induction of medical abortions. It acts by inhibiting the metabolism of folic acid.