targetsTarget

HER4 (ERBB4)

The fourth member of the HER family, hit by the irreversible pan-HER inhibitors afatinib, dacomitinib and neratinib along with EGFR and HER2. It has no approved drug of its own, and its role in cancer is less clear than that of its siblings.

ERBB4 (HER4) is a receptor tyrosine kinase activated by neuregulins that pairs with HER2 and other family members. Unlike EGFR and HER2 it is not an established oncogenic driver, and some studies link its expression to better outcomes in breast cancer. The irreversible pan-HER inhibitors afatinib and dacomitinib, approved for EGFR-mutant lung cancer, and neratinib, approved for HER2-positive breast cancer, inhibit ERBB4 as part of covering the whole family and preventing escape through HER2 or HER3 dimers. Rare ERBB4 mutations occur in melanoma and lung cancer but have no approved matched therapy.

HER4 (ERBB4): what it is and how drugs act on it · animated generic schematic, not to scale

Target · the protein and the cell it sits on
Drug · antibody, small molecule, cell or radioligand
Effect · signal, damage or kill

In plain words · The fourth member of the HER family, hit by the irreversible pan-HER inhibitors afatinib, dacomitinib and neratinib along with EGFR and HER2. It has no approved drug of its own, and its role in cancer is less clear than that of its siblings.

1 · What it is
The fourth member of the HER family, hit by the irreversible pan-HER inhibitors afatinib, dacomitinib and neratinib along with EGFR and HER2. It has no approved drug of its own, and its role in cancer is less clear than that of its siblings.
2 · What goes wrong in cancer
Neuregulin receptor of the HER family; inhibited by pan-HER covalent inhibitors rather than by a dedicated drug.
3 · How drugs use it
No product in this corpus aims at HER4 (ERBB4) yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.