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adavosertib

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Associated Genetic Biomarkers

Overview

Generic Name(s):
955365-80-7, 2-allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-6-((4-(4-methylpiperazin-1-yl)phenyl)amino)-1h-pyrazolo[3,4-d]pyrimidin-3(2h)-one, and mk 1775
NCI Definition [1]:
A small molecule inhibitor of the tyrosine kinase WEE1 with potential antineoplastic sensitizing activity. Adavosertib selectively targets and inhibits WEE1, a tyrosine kinase that phosphorylates cyclin-dependent kinase 1 (CDK1, CDC2) to inactivate the CDC2/cyclin B complex. Inhibition of WEE1 activity prevents the phosphorylation of CDC2 and impairs the G2 DNA damage checkpoint. This may lead to apoptosis upon treatment with DNA damaging chemotherapeutic agents. Unlike normal cells, most p53 deficient or mutated human cancers lack the G1 checkpoint as p53 is the key regulator of the G1 checkpoint and these cells rely on the G2 checkpoint for DNA repair to damaged cells. Annulment of the G2 checkpoint may therefore make p53 deficient tumor cells more vulnerable to antineoplastic agents and enhance their cytotoxic effect.

Clinical Trials

View Clinical Trials for adavosertib

Adavosertib has been investigated in 27 clinical trials, of which 19 are open and 8 are closed. Of the trials investigating adavosertib, 1 is early phase 1 (1 open), 12 are phase 1 (7 open), 1 is phase 1/phase 2 (1 open), and 13 are phase 2 (10 open).

TP53 Loss, TP53 Mutation, and ER Negative are the most frequent biomarker inclusion criteria for adavosertib clinical trials.

Malignant solid tumor, fallopian tube carcinoma, and ovarian carcinoma are the most common diseases being investigated in adavosertib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Adavosertib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Adavosertib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating adavosertib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
mk1775, azd1775, mk-1775, azd-1775, 955365-80-7, mk 1775, 2-allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-6-((4-(4-methylpiperazin-1-yl)phenyl)amino)-1h-pyrazolo[3,4-d]pyrimidin-3(2h)-one, 2-allyl-1-(6-(2-hydroxypropan-2-yl)pyridin-2-yl)-6-((4-(4-methylpiperazin-1-yl)phenyl)amino)-1h-pyrazolo[3,4-d]pyrimidin-3(2h)-one
Drug Categories [2]:
Tyrosine kinase inhibitors
Drug Target(s) [2]:
WEE1
NCIT ID [1]:
C91725

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.