pyrotinib + loperamide

**Pyrotinib + loperamide** is a combination of pyrotinib, an oral, irreversible pan-HER tyrosine kinase inhibitor targeting EGFR (HER1), HER2, and HER4, and loperamide, a peripheral µ-opioid receptor agonist used as an anti-diarrheal agent. Pyrotinib is primarily developed as an anti-cancer drug for HER2-positive breast cancer, showing significant benefit in progression-free survival in multiple phase III trials. Diarrhea is a frequent and sometimes severe adverse event associated with pyrotinib therapy, with an incidence exceeding 95%. Loperamide is recommended for the management and prevention of pyrotinib-induced diarrhea; its use can increase pyrotinib exposure while being effective in reducing the incidence of high-grade diarrhea[1][2][3]. The prophylactic co-administration of loperamide does not significantly change the overall and high-grade diarrhea rates between 21-day and 42-day regimens, but is considered clinically pragmatic for early cycles of pyrotinib administration[2][3].

Other names

pyrotinibloperamide