exemestane + saracatinib

Exemestane + saracatinib is an investigational combination therapy studied primarily for hormone receptor-positive metastatic breast cancer in postmenopausal women. Exemestane is a steroidal aromatase inhibitor that irreversibly inhibits the aromatase enzyme, leading to decreased estrogen production and thus suppressing the growth of estrogen-dependent breast cancer cells. Saracatinib (AZD0530) is an orally available, potent, and selective dual kinase inhibitor targeting Src family kinases and Abl tyrosine kinase. Saracatinib has been shown in preclinical models to prevent or delay the development of resistance to endocrine therapies by inhibiting Src-mediated signaling pathways involved in cell proliferation, migration, metastasis, and osteoclast activity. The combination was evaluated in a phase II randomized trial for its ability to improve progression-free survival compared with exemestane alone[1][4]. Both drugs are small molecules; exemestane was developed by Pharmacia & Upjohn (now Pfizer), while saracatinib was developed by AstraZeneca.