Cetuximab(Erbitux; ImClone Systems; formerly known as C225) is the most extensively studied and clinically approved chimeric mAb designed to specifically inhibitEGFR[202]. Cetuximab exhibits a 2-log higher affinity for EGFR thanEGFitself, thereby inhibiting EGF binding and receptorautophosphorylationand ...
药效学Cetuximab is an anticancer agent that works by inhibiting the growth and survival of epidermal growth factor receptor (EGFR)-expressing tumour cells with high specificity and higher affinity than epidermal growth factor (EGF) and transforming growth factor-alpha (TGF-α), which are natural lig...
Pharmacological Properties Cetuximab binds to the readily accessible extracellular domain of the EGFR with high affinity (dissociation constant = 0.39 nmol/L), competing with endogenous ligand binding. This competition, resulting in the blockade of receptor-dependent signal transduction pathways, provides ...
As the affinity of cetuximab for EGFR is approximately 5 to 10 fold higher than that of the endogenous ligands, it blocks the binding of these ligands resulting in inhibition of the receptor function. Furthermore, cetuximab induces the internalization of EGFR, which can lead to downregulation of...
bound by covalent and non-covalent bonds. The bond with EGFR is characterized by a higher affinity than either endogenous ligand, as epidermal growth factor (EGF), or transforming growth factor alpha. This binding inhibits activation of the receptor tyrosine kinase and the associated downstream signa...
Cetuximab is a chimeric monoclonal antibody, which binds with high affinity to the extracellular domain of the human EGFR, blocking ligand binding, resulting in inhibition of the receptor function. It also targets cytotoxic immune effector cells towards EGFR-expressing tumor cells (antibody dependent ...
High affinity Fc receptor binding and potent induction of antibody-dependent cellular cytotoxicity (ADCC) in vitro by anti-epidermal growth factor receptor... a functional antagonist by blocking ligand (EGF and TGFa) binding to EGFR and, therefore, inhibits EGFR activation and downstream signaling in...
Panitumumab (Vectibix®) is a fully humanized IgG2 mAb targeting EGFR with a higher affinity than cetuximab, which is authorized for the treatment of adult patients with wild-type KRAS mCRC. Both mAbs avoid the binding of endogenous ligands to EGFR, thus blocking receptor activation and ...
The EGF receptor (EGFR) family consists of four transmembrane receptors: EGFR (HER1/erbB-1), HER2 (erbB-2/neu), HER3 (erbB-3), and HER4 (erbB-4) (2). HER1, HER3, and HER4 comprise three major functional domains: an extracellular ligand-binding domain, a hydrophobic transmembrane ...
Human anti Cetuximab, clone AbD19834_IgG1, is an anti-idiotypic antibody that binds specifically to cetuximab and inhibits the binding of the drug to its target, epidermal growth factor receptor (EGFR). It can be used in bioanalytical assays to measure the levels of cetuximab and biosimilar ...