Drug intelligence / Profile preview

anastrozole + saracatinib

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

Overview

Anastrozole + saracatinib is a combination of two small molecule drugs investigated primarily for the treatment of hormone receptor-positive breast cancer in postmenopausal women. Anastrozole is a non-steroidal aromatase inhibitor that reduces estrogen production by inhibiting the aromatase enzyme, thereby limiting estrogen-driven tumor growth. Saracatinib (AZD0530) is a potent and selective oral inhibitor of Src family kinases (including c-Src and c-Yes) and Abl tyrosine kinase. It acts by competitively binding to the ATP-binding site of these kinases, blocking their activity and interfering with signaling pathways involved in cell proliferation, survival, invasion, metastasis, and resistance to endocrine therapy. The rationale for combining these agents is based on preclinical evidence that Src inhibition can enhance the anti-proliferative effects of endocrine therapy and potentially overcome or delay resistance to aromatase inhibitors in hormone-sensitive breast cancer[1][4][5]. This combination has been evaluated in phase I/II clinical trials for safety, tolerability, pharmacokinetics, and preliminary efficacy as neoadjuvant or metastatic therapy[1][3][4].

Other names
anastrozole plus saracatinibanastrozole + AZD0530
02

Targets

ESR1 (ERα)YES1 (YES proto-oncogene 1 tyrosine kinase)CYP19A1 (Aromatase)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)ABL2 (ABL proto-oncogene 2, non-receptor tyrosine kinase)LCK (Proto-oncogene tyrosine-protein kinase Lck)

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