Drug intelligence / Profile preview

patritumab deruxtecan + trastuzumab + tucatinib

Development stage
Unknown
Lead developer
Daiichi Sankyo
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous, Oral
01

Overview

This is an **investigational combination therapy** comprising patritumab deruxtecan (an antibody-drug conjugate targeting HER3), trastuzumab (a monoclonal antibody targeting HER2), and tucatinib (a small molecule HER2 kinase inhibitor). Patritumab deruxtecan binds HER3 and delivers a cytotoxic payload into HER3-expressing cancer cells[1]. Trastuzumab binds to HER2, inhibiting downstream signaling and mediating antibody-dependent cellular cytotoxicity. Tucatinib selectively inhibits the kinase activity of HER2. This combination is being studied in HER2-positive breast cancer, primarily for advanced or metastatic disease, as a targeted therapy approach for patients who have progressed on previous HER2-directed therapies[1].

02

Targets

TOP1 (DNA Topoisomerase I)ERBB3 (Erb-b2 receptor tyrosine kinase 3)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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