Telisotuzumab vedotin

Telisotuzumab vedotin is an antibody-drug conjugate. The monoclonal antibody component, telisotuzumab, is targeted against c-Met, a cell surface receptor tyrosine kinase and proto-oncogene. Under normal conditions, c-Met activation initiates a series of intracellular signals that mediate embryogenesis and wound healing. Aberrant activation of c-Met has been implicated in the development and progression of several cancers including cancers of the liver, lung, colon, breast, pancreas, ovaries, prostate, gastrointestinal tract, and nervous system. The small molecule payload of telisotuzumab vedotin, monomethyl auristatin E (MMAE), is a potent microtubule-disrupting agent.

Following binding to c-Met-expressing cells, telisotuzumab vedotin is internalized and cleaved to release MMAE, which disrupts the microtubule network of actively dividing cells leading to cell cycle arrest and apoptotic cell death.