neratinib + fam-trastuzumab deruxtecan

**Neratinib + fam-trastuzumab deruxtecan** is an investigational combination therapy being evaluated in clinical trials for patients with advanced or metastatic solid tumors harboring HER2 alterations. **Neratinib** is a small molecule irreversible tyrosine kinase inhibitor (TKI) that targets the HER2 receptor (ERBB2) and other members of the ErbB family, blocking intracellular signaling that promotes tumor growth. **Fam-trastuzumab deruxtecan** is an antibody-drug conjugate (ADC) composed of a humanized anti-HER2 monoclonal antibody (trastuzumab) linked to a topoisomerase I inhibitor payload (deruxtecan) via a cleavable linker. The antibody component targets HER2-expressing cells, delivering the cytotoxic payload selectively. The combination is designed for enhanced blockade of HER2-mediated signaling and HER2-driven tumor cell death. Neratinib acts intracellularly, while fam-trastuzumab deruxtecan delivers targeted cytotoxicity. This dual approach intends to optimize HER2 pathway inhibition and overcome limitations of single-agent therapies. This combination is being developed and tested primarily for HER2-altered solid tumors, especially HER2-positive breast cancer, with clinical trials currently in **Phase I**[1][2].

Brand names

NerlynxEnhertu

Other names

neratinib + trastuzumab deruxtecanneratinib + DS-8201a