Drug intelligence / Profile preview

pyrotinib + trastuzumab + dalpiciclib

Development stage
Phase 3
Lead developer
Hengrui Therapeutics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Subcutaneous
01

Overview

Pyrotinib + trastuzumab + dalpiciclib is an investigational, chemotherapy-free combination regimen being studied for the treatment of advanced HER2-positive breast cancer. This triplet therapy consists of **pyrotinib**, an irreversible pan-HER (HER1, HER2, and HER4) tyrosine kinase inhibitor; **trastuzumab**, a HER2-targeting monoclonal antibody; and **dalpiciclib**, a selective cyclin-dependent kinase 4/6 (CDK4/6) inhibitor. The combination is designed to exploit synergistic anti-tumor activity by simultaneously blocking HER2 signaling at both the extracellular and intracellular levels while inhibiting cell cycle progression. It is currently being evaluated in the Phase III DIAMOND trial (DIAMOND-01) as a potentially less toxic and more convenient alternative to standard taxane-based chemotherapy regimens in patients with HER2-positive metastatic breast cancer who have received limited prior systemic therapy.

Other names
pyrotinib plus trastuzumab plus dalpiciclibpyrotinib + subcutaneous trastuzumab + dalpiciclib
02

Targets

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

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