Drug intelligence / Profile preview

AZD-7762

Development stage
Discontinued
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Intravenous
01

Overview

AZD7762 is a synthetic small molecule inhibitor of checkpoint kinases, specifically Chk1 and Chk2. It acts as an ATP-binding competitive inhibitor, preventing cell cycle arrest and subsequent nucleotide excision repair in DNA-damaged tumor cells, which can result in tumor cell apoptosis. The drug was developed primarily for the treatment of solid tumors and has been shown to sensitize cancer cells to DNA-damaging agents such as gemcitabine, topotecan, doxorubicin, cisplatin, and radiation therapy by abrogating the G2/M checkpoint. In preclinical studies and early clinical trials, AZD7762 demonstrated inhibition of tumor cell proliferation and enhanced the effects of chemotherapy and radiotherapy. However, clinical development was terminated due to safety concerns[1][4][6][7].

Other names
(S)-5-(3-Fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide3-(Carbamoylamino)-5-(3-Fluorophenyl)-N-[(3s)-Piperidin-3-Yl]thiophene-2-Carboxamide860352-01-8CHEMBL2041933CHEMBL-2041933CHEMBL 2041933UNII-5D822Y3L1HUNII5D822Y3L1HUNII 5D822Y3L1H
02

Targets

CHEK2 (Checkpoint kinase 2)CHEK1 (Checkpoint kinase 1)

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