Drug intelligence / Profile preview

potrasertib

Development stage
Phase 1
Lead developer
IMPACT Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

Potrasertib is an oral, small-molecule, selective inhibitor of the serine/threonine-protein kinase WEE1, being developed by IMPACT Therapeutics for the treatment of advanced solid tumors, including small cell lung cancer, ovarian, colorectal, and other solid malignancies.[1][3][9][11] By blocking WEE1, a key regulator of the G2/M cell cycle checkpoint that normally phosphorylates and inhibits CDK1 and CDK2, potrasertib prevents DNA-damaged cancer cells from arresting and repairing DNA before mitosis, thereby forcing premature, error-prone mitotic entry and promoting cell death, particularly in tumors with TP53 defects and high replication stress.[1][7][11][13] Early clinical data indicate antitumor activity and acceptable tolerability as monotherapy and in combination with chemotherapy or radiotherapy, and the agent remains in phase 1 clinical development without regulatory approvals to date.[1][3][7][9][11]

Other names
IMP7068IMP-7068IMP 7068
02

Targets

WEE1 (WEE1 G2 checkpoint kinase)

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