Cancer

Cell culture studies identified a selective degrader of ESR1 that could help treat estrogen receptor-positive breast cancer. Chemical synthesis and testing in human estrogen receptor-positive breast cancer lines of analogs of the generic selective estrogen receptor modulator (SERM) raloxifene linked to a vHL ligand yielded a compound that degraded ESR1 by 50% at a concentration of 0.43 nM and inhibited proliferation with an IC₅₀ of 0.77 nM. In one of the cell lines, the compound decreased growth compared with raloxifene or Faslodex fulvestrant. Next steps could include testing the compound in animal models of estrogen receptor-positive breast cancer.

Raloxifene is marketed for breast cancer and osteoporosis...