NCIt definition : An antibody-drug conjugate (ADC) directed against the tumor necrosis factor (TNF)
receptor CD30 with potential antineoplastic activity. Brentuximab vedotin is generated
by conjugating the chimeric anti-CD30 monoclonal antibody SGN-30 to the cytotoxic
agent monomethyl auristatin E (MMAE) via a valine-citrulline peptide linker. Upon
administration and internalization by CD30-positive tumor cells, brentuximab vedotin
undergoes enzymatic cleavage, releasing MMAE into the cytosol; MMAE binds to tubulin
and inhibits tubulin polymerization, which may result in G2/M phase arrest and tumor
cell apoptosis. Transiently activated during lymphocyte activation, CD30 (tumor necrosis
factor receptor superfamily, member 8;TNFRSF8) may be constitutively expressed in
hematologic malignancies including Hodgkin lymphoma and some T-cell non-Hodgkin lymphomas.
The linkage system in brentuximab vedotin is highly stable in plasma, resulting in
cytotoxic specificity for CD30-positive cells.;