Drug intelligence / Profile preview

dalpiciclib + pyrotinib + aromatase inhibitor

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

Overview

This combination regimen consists of dalpiciclib, pyrotinib, and an aromatase inhibitor (AI), such as letrozole, anastrozole, or exemestane. Dalpiciclib is a selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which are key regulators of the cell cycle. Pyrotinib is an orally active, irreversible pan-ErbB receptor tyrosine kinase inhibitor that targets HER1 (EGFR), HER2, and HER4. The aromatase inhibitor component functions by blocking the synthesis of estrogen. This triplet therapy is being evaluated by the Second Affiliated Hospital of Soochow University in a Phase 2 clinical trial as a first-line, chemotherapy-free treatment option for elderly patients with advanced triple-positive breast cancer (ER-positive, PR-positive, and HER2-positive), aiming to provide high efficacy with lower toxicity compared to traditional chemotherapy.

Brand names
DawnaAiRuiNi
Other names
DarcilideDarsiliDalsilyPyrrotinibLetrozoleAnastrozoleExemestane
02

Targets

EGFR (Epidermal growth factor receptor)ERBB4 (Erb-b2 receptor tyrosine kinase 4)CDK6 (Cyclin-dependent kinase 6)CYP19A1 (Aromatase)ERBB2 (Erb-b2 receptor tyrosine kinase 2)CDK4 (Cyclin-dependent kinase 4)

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