GLL398, an oral selective estrogen receptor degrader (SERD), blocks tumor growth in xenograft breast cancer models.

ABSTRACT:

Purpose

Selective estrogen receptor degrader (SERD) has proven clinically effective in treating advanced or metastatic breast cancer since the approval of fulvestrant by FDA in 2002. Recent expansion of indications as a first line monotherapy and as combination therapy with CDK4/6 inhibitors further extends its clinical utility as an efficacious breast cancer endocrine regimen. However, the poor pharmacokinetic properties of fulvestrant and its injection-only administration route has driven continued efforts to develop orally bioavailability SERD that could potentially improve clinical response to SERD treatment. GLL398, a boron-modified GW5638 analog, showed superior oral bioavailability, while retaining both antiestrogenic activity and ER degrading efficacy at a potency level com

SUBMITTER: Guo S 

PROVIDER: S-EPMC7069796 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature