lsz102

Description: LSZ-102 is a potent, orally bioactive and selective ERalpha antagonist and SERD (estrogen receptor degrader) with an IC50 of 0.2 nM has the potential for the treatment of Estrogen Receptor Positive Breast Cancer. In breast cancer, estrogen receptor alpha (ERalpha) positive cancer accounts for approximately 74% of all diagnoses, and in these settings, it is a primary driver of cell proliferation. Treatment of ERalpha positive breast cancer has long relied on endocrine therapies such as selective estrogen receptor modulators, aromatase inhibitors, and SERDs. LSZ102 is a compound currently in clinical development for the treatment of ERalpha positive breast cancer.

References: J Med Chem. 2018 Apr 12; 61(7):2837-2864.