Drug intelligence / Profile preview

dalpiciclib + fulvestrant + compound gossypol acetate

Development stage
Phase 2
Lead developer
Hengrui Therapeutics
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Dalpiciclib + fulvestrant + compound gossypol acetate is an investigational triple-drug combination therapy currently under clinical evaluation for the treatment of advanced breast cancer. The regimen consists of **dalpiciclib** (SHR6390), a selective small-molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6); **fulvestrant**, a selective estrogen receptor degrader (SERD); and **compound gossypol acetate**, a natural polyphenolic compound that acts as a BH3 mimetic and inhibitor of anti-apoptotic Bcl-2 family proteins. This combination is designed to simultaneously target the CDK4/6-Rb cell cycle pathway, estrogen receptor signaling, and apoptotic escape mechanisms. It is primarily being studied in patients with hormone receptor-positive (HR+), HER2-negative metastatic breast cancer who have previously progressed on or failed treatment with other CDK4/6 inhibitors, aiming to overcome endocrine and cell-cycle-related resistance.

Brand names
Darcilie
Other names
dalpiciclib + fluvestrant + compound gossypol acetatedalpiciclib + fulvestrant + gossypol acetate
02

Targets

BCL2L1 (B-cell lymphoma-extra large protein)CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)ESR1 (ERα)ESR2 (ERβ)MCL1 (Myeloid cell leukemia sequence 1)

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