Enfortumab Vedotin Drug Description

The antibody-drug conjugates enfortumab vedotin comprises the human anti-nectin-4 antibody conjugated to the highly potent microtubule disrupting agent monomethyl auristatin E (MMAE) via a cleavable maleimidocaproyl-valyl-citrullinyl-p-aminobenzyloxycarbonyl (mc-val-cit-PABC) type linker on an average of 3-4 cysteinyl.

Scientists at Agensys (Santa Monica, CA, 90404) prepared hybridoma (AGS-22M6E) and CHO (ASG-22CE) versions of enfortumab vedotin (also known as ASG-22ME). They were able to bind the the versions of enfortumab vedotin to cell surface expressed nectin-4, a type I transmembrane protein and member of a family of related immunoglobulin-like adhesion molecules and reported high affinity and induced cell death in vitro in a dose-dependent manner. [1]

Using mouse xenograft models of human breast, bladder, pancreatic, and lung cancers, scientists found that treatment with enfortumab vedotin significantly inhibited the growth these tumor types. They also noted tumor regression of breast and bladder xenografts. Overall, these findings validate nectin-4 as an attractive therapeutic target in multiple solid tumors, and support further clinical development, investigation, and application of nectin-4-targeting ADCs.[1]

Clinical trials
Enfortumab vedotin is currently in be investigated in a number of clinical trials.