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ELVN-002 + fam-trastuzumab deruxtecan-nxki
- Development stage
- Unknown
- Lead developer
- Enliven Therapeutics
- Modality
- Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
- Administration
- Oral, Intravenous
01
Overview
This is a **combination therapy** consisting of two investigational drugs: ELVN-002, a potent, highly selective, central nervous system-penetrant, irreversible HER2 inhibitor (small molecule tyrosine kinase inhibitor), and fam-trastuzumab deruxtecan-nxki, a HER2-targeted antibody-drug conjugate. ELVN-002 is designed to inhibit wild-type and mutant HER2 while sparing EGFR, offering potential utility in HER2-driven malignancies, including those with brain metastases. Fam-trastuzumab deruxtecan-nxki (Enhertu/T-DXd) is an antibody-drug conjugate composed of a humanized anti-HER2 monoclonal antibody linked to a cytotoxic topoisomerase I inhibitor, used primarily in HER2-positive cancers. The combination is being studied in early-phase trials for enhanced anti-tumor activity in HER2-positive and HER2-mutated solid tumors, notably breast cancer and non-small cell lung cancer.
- Brand names
- Enhertu (for fam-trastuzumab deruxtecan-nxki)
- Other names
- DS-8201a (for fam-trastuzumab deruxtecan-nxki)
02
Targets
TOP1 (DNA Topoisomerase I)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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