Cancer
Cell culture and mouse studies identified a benzopyran-based dual ESR1/ESR2 inhibitor and selective estrogen receptor down-regulator (SERD) that could help treat hormone therapy-resistant breast cancer. Chemical synthesis and testing in cell-based assays of benzopyran analogs yielded a compound that inhibited the activity of ESR1 and ESR2 with IC50 values of 1.6 and 3.2 nM, respectively, and decreased ESR1 levels compared with vehicle. In a xenograft mouse model of hormone therapy-resistant breast cancer, oral administration of the compound decreased tumor growth compared with subcutaneous Faslodex fulvestrant or oral tamoxifen. Next steps by Olema Pharmaceuticals Inc. could include optimizing and testing the compound in additional models of breast cancer.
AstraZeneca plc markets Faslodex, a selective estrogen receptor down-regulator (SERD), for breast cancer...