Drug intelligence / Profile preview

tucatinib + trastuzumab

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

Overview

Tucatinib + trastuzumab is a combination therapy used primarily for the treatment of HER2-positive cancers. Tucatinib is an oral small molecule tyrosine kinase inhibitor that selectively targets the human epidermal growth factor receptor 2 (HER2), blocking its activity and thereby inhibiting cancer cell proliferation and survival. Trastuzumab is a monoclonal antibody that binds to the extracellular domain of HER2, preventing receptor activation and downstream signaling. This combination is approved for use in adults with unresectable or metastatic HER2-positive breast cancer who have received prior anti-HER2 therapies, as well as for RAS wild-type, HER2-positive metastatic colorectal cancer after previous chemotherapy regimens[1][4][8]. The combination exploits dual blockade of the HER2 pathway to improve outcomes in patients with advanced disease.

02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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