Epratuzumab-cys-tesirine
<languages /><translate> An antibody-drug conjugate (ADC) composed of a cysteine-engineered version of epratuzumab (hLL2), a humanized anti-CD22 monoclonal antibody.
How is it made?
It is derived from the murine immunoglobulin (Ig) G2a monoclonal antibody LL2 (EPB-2), site-specifically conjugated to the cross-linking cytotoxic agent tesirine (SG3249), a cathepsin B-cleavable valine-alanine pyrrolobenzodiazepine dimer (PBD), with potential antineoplastic activity.
Mechanism of action
- Upon administration of epratuzumab-cys-tesirine, the epratuzumab moiety targets and binds to the B-cell-specific CD22 receptor and is rapidly internalized.
- Upon cleavage, the imine groups of tesirine target and bind to the N2 positions of guanines on opposite strands of DNA.
- This induces interstrand cross-links in the minor groove of DNA and inhibits DNA replication, which inhibits the proliferation of CD22-overexpressing tumor cells.
CD22 cell surface glycoprotein
CD22, a cell surface glycoprotein, is expressed on mature B-cells and on most malignant B cells.
See also
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