Drug intelligence / Profile preview

azd5438

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

Overview

AZD5438 is a potent, orally bioavailable small molecule inhibitor of cyclin-dependent kinases (CDKs), specifically targeting CDK1, CDK2, and CDK9 with low nanomolar IC50 values. It also inhibits CDK5, CDK4, and CDK7 at higher concentrations. Developed by AstraZeneca for oncology indications, particularly solid tumors, AZD5438 exerts antiproliferative effects in vitro and in vivo by blocking cell cycle progression at G1/S/G2-M phases through inhibition of phosphorylation of key substrates such as pRb and nucleolin. The drug demonstrated tumor growth inhibition in xenograft models and was evaluated in phase I clinical trials for advanced solid malignancies[1][2][3][5][6][7].

Other names
4-(1-isopropyl-2-methylimidazol-5-yl)-2-(4-methylsulphonylanilino)pyrimidine
02

Targets

CDK7CDK1 (Cyclin-dependent kinase 1)CDK4 (Cyclin-dependent kinase 4)CDK2 (Cyclin-dependent kinase 2)CDK9 (Cyclin-dependent kinase 9)CDK5 (Cyclin-dependent kinase 5)

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