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Drug Target Encyclopedia Series (11) — HER2
Release Time：
2025-12-05 13:35
HER2 is a transmembrane receptor tyrosine kinase belonging to the ErbB family, playing a key role in regulating cell growth, survival, and differentiation. Overexpression or amplification of HER2 drives oncogenesis in multiple tumor types, leading to aggressive disease progression.
HER2 is overexpressed in:
• Breast cancer (~15–20% of cases)
• Gastric and gastroesophageal junction (GEJ) cancer
• Colorectal cancer (subset)
• Lung adenocarcinoma (subset)
Targeting HER2 in oncology:
- Monoclonal antibodies – Trastuzumab (FDA-approved) revolutionized HER2+ breast cancer therapy by blocking receptor signaling and mediating ADCC.
- Antibody-drug conjugates (ADCs) – Trastuzumab deruxtecan (T-DXd) delivers potent cytotoxic payloads directly to HER2+ tumor cells, with remarkable efficacy even in HER2-low cancers.
- Bispecific antibodies – Emerging HER2/CD3 bispecifics redirect T cells to HER2-expressing tumors.
- CAR-T cell therapy – HER2-CAR-T is under investigation for solid tumors, showing potential but requiring safety optimization to avoid on-target/off-tumor toxicity.
- Small molecule TKIs – Lapatinib, neratinib, and tucatinib inhibit HER2 signaling in advanced or resistant disease.
Challenges include primary and acquired resistance to HER2-targeted agents, tumor heterogeneity, and toxicity in normal HER2-expressing tissues.
Current research is exploring HER2-targeted therapies for HER2-low/ultra-low tumors, novel ADC payloads, CAR-NK strategies, and combination regimens with checkpoint inhibitors to overcome resistance.
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