c-KIT EpiTAC

c-KIT EpiTAC is an extracellular targeted protein degrader (eTPD) being developed by Epibiologics for the treatment of gastrointestinal stromal tumors (GIST). It is a bispecific antibody designed with one arm targeting the c-KIT (CD117) receptor tyrosine kinase and the other arm targeting a degrading cell-surface receptor. This dual engagement triggers the internalization and subsequent lysosomal degradation of the c-KIT protein. By eliminating the protein rather than just inhibiting its kinase activity, this approach aims to overcome resistance mutations common with traditional tyrosine kinase inhibitors. Preclinical studies have demonstrated that the EpiTAC selectively targets GIST cells while sparing hematopoietic stem cells, which also express c-KIT, by utilizing a degrading receptor absent from the latter.

Other names

c-KIT degrading bispecific antibodyc-KIT eTPD