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fam-trastuzumab-deruxtecan + osimertinib

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

Overview

This is a combination therapy consisting of fam-trastuzumab-deruxtecan (an antibody-drug conjugate targeting HER2) and osimertinib (a third-generation EGFR tyrosine kinase inhibitor). The combination is being investigated for the treatment of non-small cell lung cancer (NSCLC) with acquired resistance to EGFR-targeted therapies, particularly in cases where HER2 mutations or amplifications are identified as mechanisms of resistance. Fam-trastuzumab-deruxtecan delivers a cytotoxic payload specifically to HER2-expressing tumor cells, while osimertinib inhibits mutant EGFR signaling. The combination aims to overcome resistance by dual blockade of both pathways[1][3].

Brand names
EnhertuTagrisso
Other names
fam-trastuzumab deruxtecan-nxki + osimertinibtrastuzumab deruxtecan + osimertinib
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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