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

• Antibody-oligonucleotide conjugate
• Immune stimulating antibody conjugate
• Small molecule drug conjugate

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