Drug intelligence / Profile preview

trastuzumab + pyrotinib + dalpiciclib

Development stage
Unknown
Lead developer
Hengrui Pharmaceutical
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of three agents used in the treatment of HER2-positive breast cancer, particularly in advanced or metastatic settings. - Trastuzumab is a monoclonal antibody that targets the human epidermal growth factor receptor 2 (HER2/ERBB2), inhibiting its signaling and mediating antibody-dependent cellular cytotoxicity. - Pyrotinib is an oral, irreversible small molecule tyrosine kinase inhibitor that targets multiple members of the ErbB family (HER1/EGFR, HER2/ERBB2, and HER4), blocking downstream signaling pathways such as RAS/RAF/MEK/MAPK and PI3K/AKT to inhibit tumor cell proliferation[3][4][5]. - Dalpiciclib is a selective cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor that blocks cell cycle progression from G1 to S phase by inhibiting phosphorylation of retinoblastoma protein. This triple combination aims to provide comprehensive blockade of HER2-driven signaling and cell cycle progression for improved antitumor efficacy in patients with HER2-positive breast cancer who may have progressed on prior therapies.

Other names
trastuzumab + pyrotinib + dalpiciclib
02

Targets

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

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