Drug intelligence / Profile preview

pyrotinib maleate + dalpiciclib isethionate + standard endocrine therapy

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

Overview

This combination therapy consists of pyrotinib maleate, dalpiciclib isethionate, and standard endocrine therapy. Pyrotinib is an irreversible pan-ErbB receptor tyrosine kinase inhibitor (TKI) that targets the intracellular kinase domains of EGFR (HER1), HER2, and HER4. Dalpiciclib (also known as darcilib or SHR6390) is a potent and selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), which are key regulators of the cell cycle. Standard endocrine therapy typically involves aromatase inhibitors or estrogen receptor antagonists. This triplet regimen is being evaluated as a neoadjuvant treatment for patients with hormone receptor-positive (HR+) and HER2-low expression breast cancer to improve pathological complete response rates. The development is primarily associated with Jiangsu Hengrui Pharmaceuticals (the drug manufacturer) and clinical investigation by The First Affiliated Hospital of Xiamen University.

Brand names
AiRuiNiAiRuikang
Other names
pyrotinib + dalpiciclib + endocrine therapypyrotinib + darcilib + endocrine therapy
02

Targets

ERBB4 (Erb-b2 receptor tyrosine kinase 4)ERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)CDK6 (Cyclin-dependent kinase 6)CYP19A1 (Aromatase)CDK4 (Cyclin-dependent kinase 4)ESR1 (ERα)

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