eprenetapopt

Eprenetapopt is a small molecule prodrug and structural analog of PRIMA-1, designed to restore the function of mutant and inactivated p53 protein. Upon administration, it is converted to methylene quinuclidinone, which covalently binds to cysteine residues in mutant p53, stabilizing its wild-type conformation and reactivating its tumor suppressor function. This leads to cell cycle arrest and apoptosis in cancer cells with TP53 mutations. Eprenetapopt also induces cell death through p53-independent mechanisms such as glutathione depletion (triggering ferroptosis), inhibition of thioredoxin reductase 1, and inhibition of NFS1 cysteine desulfurase activity. It has been investigated primarily for hematologic malignancies like myelodysplastic syndromes (MDS) and acute myeloid leukemia (AML), as well as various solid tumors including ovarian cancer[1][3][4][5][6][7][8].

Brand names

APR-246APR246APR 246

Other names

eprenetapoptPRIMA-1-METPRIMA1-METPRIMA 1-MET