Drug intelligence / Profile preview

fulvestrant + dalpiciclib isethionate

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

A combination therapy consisting of fulvestrant, a selective estrogen receptor degrader (SERD), and dalpiciclib isethionate (SHR6390), an oral small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). Developed by Jiangsu Hengrui Pharmaceuticals and its subsidiary Shandong Suncadia Medicine, this regimen is indicated for patients with hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) locally advanced or metastatic breast cancer. Dalpiciclib functions by selectively inhibiting CDK4/6, thereby preventing the phosphorylation of the retinoblastoma (Rb) protein and blocking cell cycle progression from the G1 to the S phase. Fulvestrant competitively binds to estrogen receptors and induces their down-regulation and degradation. The combination has demonstrated clinical efficacy in the DAWNA-1 trial, significantly extending progression-free survival compared to fulvestrant alone in patients who progressed on prior endocrine therapy.

Brand names
FaslodexAiRuikang
Other names
dalpiciclib + fulvestrantSHR6390 + fulvestrant
02

Targets

CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)ER (Estrogen receptor)

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