Preferred Label : Epratuzumab-cys-tesirine;
NCIt synonyms : Anti-CD22/PBD ADC ADCT-602; Epratuzumab-cys-SG3249; Antibody-drug Conjugate ADCT-602; hLL2-cys-PBD; ADC ADCT-602; hLL2-cys-SG3249;
NCIt definition : An antibody-drug conjugate (ADC) composed of a cysteine-engineered version of epratuzumab
(hLL2), a humanized anti-CD22 monoclonal antibody 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. 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, a cell surface glycoprotein,
is expressed on mature B-cells and on most malignant B-cells.;
UNII : 7X6143A60Y;
Molecule name : ADCT-602;
NCI Metathesaurus CUI : CL556329;
Origin ID : C155794;
UMLS CUI : C4733656;
Semantic type(s)
- concept_is_in_subset
- has_target
