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Description: GLL398 (GLL-398) is a novel, potent, orally bioavailable, and selective estrogen receptor downregulator. GLL-398 strongly binds to ERalpha in a fluorescence resonance energy transfer binding assay (IC50 =1.14 nM) and potently degrades ERalpha in MCF-7 breast cancer cells (IC50 = 0.21 uM). Most importantly, the introduction of the boronic acid group confers superior oral bioavailability of GLL398 (AUC = 36.9 ug·h/mL) in rats as compared to GW7604 (AUC = 3.35 ug·h/mL). The strikingly favorable pharmacokinetic property of GLL398 makes it a promising oral SERD suitable for clinical evaluation.
References: ACS Med Chem Lett. 2016 Nov 29; 8(1):102-106.
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