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Epidermal growth factor receptor (EGFR) and B7 homolog 3 (B7-H3) (EGFR/B7-H3)

Target
EGFR/B7-H3
Molecular classification
Receptor tyrosine kinase, Immune checkpoint molecule, Cell surface antigen
01

Overview

The targets of interest are the Epidermal Growth Factor Receptor (EGFR) and B7-H3 (also known as CD276). EGFR is a transmembrane receptor tyrosine kinase that regulates essential cellular processes such as growth, survival, and migration; its dysregulation is a major driver in various cancers, particularly non-small cell lung cancer. B7-H3 is an immune checkpoint protein from the B7 family that is overexpressed in many solid tumors and is associated with tumor progression, metastasis, and immune evasion. The simultaneous targeting of these two antigens is a therapeutic strategy aimed at increasing tumor specificity and overcoming resistance to single-target therapies. FH-006 is a bispecific antibody-drug conjugate (ADC) designed to bind both EGFR and B7-H3 on the surface of tumor cells. Upon binding and internalization, the drug releases a potent topoisomerase I inhibitor payload, which induces DNA damage and apoptosis in the target cells. This dual-targeting approach is currently being investigated in clinical trials for the treatment of advanced solid tumors, including lung squamous cell carcinoma.

Other names
CD276B7-H3ErbB-1HER1Epidermal growth factor receptorB7 homolog 3CD276 MoleculeCostimulatory Molecule
02

Mechanism of action

Bispecific antibody-drug conjugate (ADC) targeting EGFR and B7-H3, delivering a topoisomerase I inhibitor payload to induce DNA damage and cell death.

03

Biological functions

Cell proliferationSignal transductionImmune regulationApoptosis inhibitionCell survivalAngiogenesis
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Disease associations

Non-small cell lung cancerSolid tumorsLung squamous cell carcinomaCancer
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Safety considerations

Hematological toxicityGastrointestinal toxicityInfusion-related reactionsPotential for interstitial lung disease
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Interacting drugs

FH-006
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Biomarkers

EGFR expressionB7-H3 (CD276) expression

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