Drug intelligence / Profile preview

dalpiciclib + pyrotinib

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

Overview

Dalpiciclib + pyrotinib is an investigational oral combination therapy for HER2-positive advanced or metastatic breast cancer. Dalpiciclib is a selective cyclin-dependent kinase 4/6 (CDK4/6) inhibitor that blocks cell cycle progression by inhibiting phosphorylation of the retinoblastoma protein, leading to G1 phase arrest. Pyrotinib is an irreversible pan-ErbB receptor tyrosine kinase inhibitor targeting HER1 (EGFR), HER2, and HER4 receptors; it inhibits tumor cell proliferation by blocking downstream signaling pathways critical for cancer growth. The combination has demonstrated promising efficacy and manageable toxicity in clinical trials as a chemotherapy-free regimen for patients with HER2-positive advanced breast cancer—including those with hormone receptor–positive or –negative disease and brain metastases[2][3][4]. It is being studied both as a dual regimen and in triplet combinations with endocrine therapies such as letrozole[1][3][7].

Brand names
DawuAiRuiNi
Other names
Dalpiciclib and PyrotinibSHR6390 and PyrotinibSHR-6390 and PyrotinibSHR 6390 and PyrotinibSHR6390 + Pyrotinib
02

Targets

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

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