Drug intelligence / Profile preview

adavosertib

Development stage
Phase 2
Lead developer
AstraZeneca
Modality
Small Molecules
01

Overview

Adavosertib is a first-in-class, selective, small-molecule inhibitor of the tyrosine kinase WEE1. By inhibiting WEE1, adavosertib disrupts the G2 DNA damage checkpoint in cancer cells, particularly those with p53 deficiencies. This abrogation leads to premature mitosis and cell death in tumor cells that rely on this checkpoint for survival after DNA damage. Adavosertib has demonstrated antitumor activity as monotherapy and in combination with other agents across various solid tumors, including ovarian cancer (notably *CCNE1*-amplified), triple-negative breast cancer, small-cell lung cancer, and other refractory solid tumors. The drug was originally developed by Merck & Co and further developed by AstraZeneca and several academic collaborators[3][6][8].

Brand names
adavosertib
Other names
adavosertibum
02

Targets

WEE2 (Wee1-like protein kinase 2)WEE1 (WEE1 G2 checkpoint kinase)

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