In vitro activity: GDC-0927 (formerly known as SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective ER (estrogen receptor) antagonist/ER degrader (SERD) that induces tumor regression in ER+ BC patient-derived xenograft models. GDC-0927 appears well-tolerated to date with PK exposure supporting QD dosing, evidence of robust PD target engagement, and encouraging anti-tumor activity in heavily pretreated pts with advanced or metastatic ER+ BC, including pts with ESR1 mutations. GDC-0927 is a next-generation orally active SERD which appears to have greater potential than GDC-0810 to be a best-in-class SERD molecule. GDC-0927 targets estrogen receptor alpha (ERα), a receptor expressed in more than 70% of breast cancers, making it a popular target for the disease.

Kinase Assay: GDC-0927 (formerly known as SRN-927) is a novel, potent, non-steroidal, orally bioavailable, selective ER (estrogen receptor) antagonist/ER degrader (SERD). GDC-0927 targets estrogen receptor alpha (ERα), a receptor expressed in more than 70% of breast cancers, making it a popular target for the disease.

Cell Assay: