Neratinib/neratinib: significant efficacy and comprehensive effects, but you need to be wary of side effects

Neratinib/ Neratinib, an oral small molecule pan-human TKI, has made a splash in the anti-cancer field since it was approved by the U.S. Food and Drug Administration (FDA) in 2017. It irreversibly binds to HER1, HER2 and HER4 in the epidermal growth factor receptor (EGFR), effectively blocking the signal transduction of these receptors, thereby exerting powerful anti-cancer effects.

For patients with drug-resistant breast cancer (BC) who have previously receivedHER2 monoclonal antibodies or targeted therapy, neratinib has shown a unique efficacy in reversing drug resistance, providing new treatment hope for these patients. Neratinib has demonstrated excellent efficacy in multiple clinical trials, either as monotherapy or in combination with other therapies.

In theI-SPY2 neoadjuvant trial, the combined use of neratinib and trastuzumab significantly improved the pathological complete response (pCR) rate in patients with HER2-positive, hormone receptor (HR)-negative breast cancer. This result undoubtedly opens up a new path for the treatment of breast cancer. In the ExteNET trial, neratinib also showed significant effects in extended adjuvant therapy after trastuzumab treatment, further confirming its important role in the treatment of breast cancer.

However, despite the excellent efficacy of neratinib, its side effects cannot be ignored. The most common adverse reaction is diarrhea, which may cause considerable distress to patients. To reduce the incidence, severity, and duration of diarrhea, doctors often recommend loperamide for prevention and treatment. Neratinib also has the potential to prevent and control brain metastases in patients with advanced breast cancer. This discovery provides a new strategy for the treatment ofHER2-positive breast cancer, making neratinib's position in the treatment of breast cancer more stable.