Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD)

WuXi AppTec scientists contributed to a study which identified a novel, indole-based, selective estrogen receptor degrader (SERD), designated LX-039. The authors show that LX-039 exhibits potent activity in ER degradation and proliferation assays.

With favorable ADME/PK properties, LX-039 also exhibits higher efficacy in a tamoxifen-resistant MCF7 CDX model compared to fulvestrant, with up to 90% inhibition of tumor growth.

View the abstract here

Check out our extensive platform of ADME/DMPK and Discovery Chemistry services