Drug intelligence / Profile preview

azm475271

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

AZM475271 is an **orally active small molecule inhibitor** that selectively targets **Src family tyrosine kinases**, particularly **Src** and **Yes**, with potent inhibitory activity (IC50 values in the low nanomolar range)[1][3][7][8]. It inhibits phosphorylation of c-Src kinase, Lck, c-Yes, and VEGFR2[1], and its mechanism disrupts signaling pathways associated with cell proliferation, migration, angiogenesis, and metastasis[4][9]. Developed originally by **AstraZeneca**, AZM475271 showed antitumor and antimetastatic activities in preclinical models, including inhibition of tumor growth, vascularization, and progression in lung adenocarcinoma and pancreatic carcinoma models[2][4][9]. Clinical development advanced to early phase trials in oncology, including hematologic neoplasms and solid tumors, but was **discontinued** before approval[5].

Other names
AZM475271AZM-475271AZM 475271M475271M-475271M 475271
02

Targets

YES1 (YES proto-oncogene 1 tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)LCK (Proto-oncogene tyrosine-protein kinase Lck)

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