SAR439859 (Amcenestrant) is a potent, orally available, selective estrogen receptor degrader (SERD) with IC50 of 0.2 nM (ERα degradation).
SAR439859 showed an outstanding overall profile with high degradation efficacy (98%) comparable to the in vitro activity of fulvestrant combined with a remarkable metabolic stability.
SAR439859 displayed no off-target activity in a large Cerep panel for in vitro selectivity.
SAR439859 exhibited substantial tumor-growth inhibition, at a dose of 25 mg/kg/BID, SAR439859 displayed tumor regression in MCF-7 tamoxifen-sensitive xenograft, with no weight loss.
