Preferred Label : Laprituximab Emtansine;
NCIt synonyms : Anti-EGFR-SMCC-DM1;
NCIt definition : A targeted antibody payload (TAP)-based immunoconjugate consisting of a human monoclonal
antibody directed against the epidermal growth factor receptor (EGFR) conjugated,
via a nonreducible thioether linker (succinimidyl trans-4-(maleimidylmethyl)cyclohexane-1-carboxylate
or SMCC), to the cytotoxic agent maytansinoid mertansine (DM1), with potential antineoplastic
activity. Upon intravenous administration, the monoclonal antibody moiety of laprituximab
emtansine binds to and inhibits EGFR on tumor cell surfaces. Inhibition of EGFR prevents
EGFR-mediated signaling and may inhibit tumor cell proliferation. After internalization,
the mertansine moiety binds to tubulin and interferes with microtubule assembly/disassembly
dynamics. This inhibits both cell division and the proliferation of cancer cells that
express EGFR. EGFR, overexpressed by a variety of cancers, plays a key role in tumor
cell proliferation and survival. Linkage of the antibody and drug, through a nonreducible
linker, appears to contribute to the improved efficacy and reduced toxicity of this
antibody-drug conjugate (ADC) compared to similar ADCs constructed with reducible
linkers.;
UNII : 7J0LQD86OG;
CAS number : 1622327-37-0;
Molecule name : IMGN289;
NCI Metathesaurus CUI : CL454236;
Origin ID : C111906;
UMLS CUI : C5235369;
Semantic type(s)
- concept_is_in_subset
- has_target
