Drug intelligence / Profile preview

pyrotinib + trastuzumab + vinorelbine

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

Overview

Pyrotinib + trastuzumab + vinorelbine is a combination regimen used in the treatment of HER2-positive breast cancer, particularly in patients who have developed resistance to prior anti-HER2 therapies such as trastuzumab and pertuzumab. Pyrotinib is an oral, irreversible pan-ErbB receptor tyrosine kinase inhibitor targeting HER1 (EGFR), HER2, and HER4. Trastuzumab is a monoclonal antibody that binds to the extracellular domain of the HER2 receptor, inhibiting downstream signaling and mediating antibody-dependent cellular cytotoxicity. Vinorelbine is a semi-synthetic vinca alkaloid chemotherapy agent that disrupts microtubule assembly by binding tubulin, thereby inhibiting mitosis. This combination aims to overcome resistance mechanisms by simultaneously blocking multiple pathways involved in tumor growth and survival. The regimen has shown promising efficacy as neoadjuvant or second-line therapy for locally advanced or metastatic HER2-positive breast cancer[6][1].

02

Targets

ERBB4 (Erb-b2 receptor tyrosine kinase 4)EGFR T790M (Epidermal growth factor receptor T790M mutant)TUBB (Tubulin (alpha and beta subunits))ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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