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1791P A Phase I Pharmacology Study of the Dual MDMX/MDM2 Inhibitor, ALRN 6924, in Healthy Volunteers

Annals of oncology(2021)

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摘要
ALRN-6924 is a cell-permeating, stabilized alpha-helical peptide that binds with high affinity to endogenous p53 inhibitors MDM2 and MDMX. ALRN-6924 activates p53 in cells with wild-type, functional p53. Therefore, for patients with tumors harboring mutated p53, pre-treatment with ALRN-6924 may transiently induce cell cycle arrest in normal cells, allowing chemotherapy to selectively target cancer cells that are actively cycling.
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