NCIt definition : A methylated derivative and structural analog of PRIMA-1 (p53 re-activation and induction
of massive apoptosis), with potential antineoplastic activity. Upon administration,
eprenetapopt covalently modifies the core domain of mutated forms of cellular tumor
antigen p53 (p53) through the alkylation of thiol groups. These modifications restore
both the wild-type conformation and function to mutant p53, which reconstitutes endogenous
p53 activity, leading to cell cycle arrest and apoptosis in tumor cells. This agent
may work synergistically with other antineoplastic agents. p53, a tumor suppressor
and transcription factor normally activated upon DNA damage, is frequently mutated
and overexpressed in cancer cells; it plays a key role in both DNA repair and the
induction of apoptosis.;