teplizumab   Click here for help

GtoPdb Ligand ID: 12252

Synonyms: humanized OKT3 | MGA031 | PRV-031 | teplizumab-mzwv | Tzield®
Approved drug Immunopharmacology Ligand
teplizumab is an approved drug (FDA (2022))
Compound class: Antibody
Comment: Teplizumab is a humanized anti-CD3e monoclonal antibody that was originally developed as an immunomodulatory agent. Structurally it is a modified version of the mouse antibody muromonab-CD3 (mOKT3) that has been used to reverse steroid-resistant renal allograft rejection. Alterations in the OKT3 CH2 domain disrupt Fcγ receptor binding, and blocks antibody-mediated effector cells functions and cytokine release [5,7]. It was advanced to extended clinical evaluations for potential to protect pancreatic β-cells in newly diagnosed type 1 diabetes (T1D) patients [4,6], following evidence that it impaired expansion of alloreactive anti-β cell T cells [5], and that a single short course of teplizumab treatment could induce a long-lasting improvement in patients' C-peptide responses and clinical parameters (including preservation of insulin production) in the early stages of T1D [2-3].
Bioactivity Comments
Teplizumab's CD3e binding affinity will be similar to that of its parent antibody muromonab-CD3.
Selectivity at other protein targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
CD3e Hs Antibody Binding - - - 5,7
[5,7]