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Tagrisso + Imfinzi + Enhertu + Imjudo

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

Overview

**Tagrisso + Imfinzi + Enhertu + Imjudo** is an experimental four-drug combination therapy primarily investigated for advanced non-small cell lung cancer (NSCLC), particularly in patients with EGFR-mutated tumors progressing after prior EGFR tyrosine kinase inhibitor (TKI) therapy. It combines **Tagrisso (osimertinib)**, a third-generation irreversible small-molecule EGFR TKI that selectively inhibits EGFR-mutant kinases including T790M; **Imfinzi (durvalumab)**, a human IgG1 monoclonal antibody blocking PD-L1 to restore anti-tumor T-cell activity; **Enhertu (trastuzumab deruxtecan)**, an antibody-drug conjugate (ADC) comprising a HER2-directed antibody linked to a topoisomerase I inhibitor payload for targeted delivery; and **Imjudo (tremelimumab)**, a human IgG2 monoclonal antibody targeting CTLA-4 to enhance T-cell priming and activation. Developed by AstraZeneca (Tagrisso, Imfinzi, Imjudo) and Daiichi Sankyo/AstraZeneca (Enhertu), this regimen aims to address multiple resistance mechanisms in EGFR-mutant NSCLC through synergistic EGFR inhibition, HER2 targeting, and dual immune checkpoint blockade.

02

Targets

TOP1 (DNA Topoisomerase I)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)ERBB2 (Erb-b2 receptor tyrosine kinase 2)CD274 (Programmed cell death protein 1 ligand 1)EGFR T790M (Epidermal growth factor receptor T790M mutant)

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