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PRIMA-1

Development stage
Preclinical
Lead developer
Aprea Therapeutics
Modality
Small Molecules
Administration
Intravenous, Intratumoral
01

Overview

PRIMA-1 is a small-molecule experimental anticancer agent that was originally identified in a cell-based screen for compounds capable of restoring wild-type function to mutant p53, a frequently altered tumor suppressor in human cancers. It is a low–molecular weight bicyclic compound (2,2-bis(hydroxymethyl)-1-azabicyclo[2.2.2]octan-3-one) that reactivates the transcriptional and pro-apoptotic functions of mutant p53, thereby inducing cell cycle arrest and apoptosis in a range of tumor cell lines and reducing tumor growth in xenograft models.[1][9] PRIMA-1 is considered a lead compound for the development of p53-targeted anticancer drugs, and its methylated derivative PRIMA-1MET (APR-246) has advanced into clinical trials, while PRIMA-1 itself is currently used primarily as a research tool compound rather than a therapeutic product.[1][3][4][9]

Other names
2,2-bis(hydroxymethyl)-1-azabicyclo[2.2.2]octan-3-onep53 reactivation and induction of massive apoptosisp-53 reactivation and induction of massive apoptosisp 53 reactivation and induction of massive apoptosis
02

Targets

TP53 (Cellular Tumor Antigen p53 R175H)

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