Drug intelligence / Profile preview

pyrotinib + trastuzumab + dalpiciclib + letrozole

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

Overview

This is a four-drug combination regimen consisting of pyrotinib, trastuzumab, dalpiciclib, and letrozole. Pyrotinib is an oral irreversible tyrosine kinase inhibitor targeting HER2 and EGFR; trastuzumab is a monoclonal antibody against the HER2 receptor; dalpiciclib is an oral cyclin-dependent kinase 4/6 (CDK4/6) inhibitor; and letrozole is a nonsteroidal aromatase inhibitor that suppresses estrogen synthesis. This combination has been investigated as neoadjuvant therapy for triple-positive breast cancer (TPBC), which expresses hormone receptors (HR) and overexpresses HER2. The regimen aims to provide chemotherapy-sparing treatment by simultaneously inhibiting HER2 signaling, cell cycle progression, and estrogen-driven tumor growth. Clinical trials have shown promising pathological response rates with acceptable safety profiles in patients with TPBC[1][2][3].

02

Targets

ERBB4 (Erb-b2 receptor tyrosine kinase 4)ER (Estrogen receptor)CDK6 (Cyclin-dependent kinase 6)CYP19A1 (Aromatase)CYP3A4 (Cytochrome P450 3A4)ERBB2 (Erb-b2 receptor tyrosine kinase 2)CDK4 (Cyclin-dependent kinase 4)CYP2A6 (Cytochrome P450 2A6)EGFR T790M (Epidermal growth factor receptor T790M mutant)CYP1A1 (Cytochrome P450 1A1)

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