Drug intelligence / Profile preview

dalpiciclib + exemestane + fulvestrant

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Recombinant Proteins and Enzymes, Small Molecules
Administration
Oral, Intramuscular
01

Overview

Dalpiciclib + exemestane + fulvestrant is a combination therapy under investigation for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative breast cancer. Dalpiciclib is a novel, orally administered small molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which are key regulators of cell cycle progression. Exemestane is an aromatase inhibitor that suppresses estrogen synthesis, while fulvestrant is a selective estrogen receptor degrader (SERD) that binds to and accelerates degradation of the estrogen receptor. The combination aims to enhance antitumor efficacy by simultaneously inhibiting cell cycle progression and blocking estrogen signaling pathways critical for HR-positive breast cancer cell survival and proliferation[1][5][6]. This regimen has been studied in clinical trials as neoadjuvant or advanced therapy in various settings for HR-positive/HER2-negative breast cancer.

02

Targets

ESR1 (ERα)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)CYP19A1 (Aromatase)

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