Description
LSZ102 is a potent, orally bioavailable, selective estrogen receptor degrader (SERD) with ERalpha transcription IC50 of 6nM and ERalpha degradation IC50 of 0.2nM; robustly causes inhibition of cell proliferation in MCF-7 cells with IC50 of 1.7nM, inhibits the mRNA level of canonical endogenous ER target gene GREB1 with IC50 of 8.9nM; demonstrates anti-tumor efficacy in the ER+ human breast cancer MCF-7 xenograft model (10mg/kg). Breast Cancer Phase 1 Clinical