Drug intelligence / Profile preview

dalpiciclib + exemestane

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

Overview

Dalpiciclib + exemestane is a combination therapy under investigation primarily for hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer. Dalpiciclib is an oral small-molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which blocks cell cycle progression in cancer cells by inhibiting phosphorylation of retinoblastoma protein. Exemestane is a steroidal aromatase inhibitor that suppresses estrogen synthesis, thereby reducing tumor growth in estrogen-dependent cancers. The combination leverages dual mechanisms—cell cycle arrest and endocrine suppression—to enhance antitumor efficacy. This regimen has been studied as neoadjuvant therapy and in other settings for HR+/HER2- breast cancer, showing promising objective response rates and manageable safety profiles[1][6][10].

02

Targets

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

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