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PT-202 is a preclinical-stage small molecule xanthine derivative being developed by p53-Therapeutics for the treatment of cancers harboring mutated p53. As an analog of the p53-pathway restoring compound CB002, PT-202 bypasses defective p53 signaling by inducing the integrated stress response (ISR) and upregulating the transcription factors ATF3 and ATF4. This non-canonical pathway activation leads to the transcriptional upregulation of pro-apoptotic p53 target genes, such as NOXA (PMAIP1) and DR5 (TNFRSF10B), thereby promoting apoptotic cell death and cell cycle arrest at the S-phase checkpoint in tumor cells without affecting normal cells.
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