The difference between neratinib/neratinib and pyrotinib

Neratinib/Neratinib and Pyrotinib are two drugs for the treatment of breast cancer. They have certain similarities in structure and mechanism of action, but there are significant differences in clinical application, indications and side effects.

Neratinib, branded as Nerlynx, is an irreversible TKI for HER1, HER2, and HER4. It has been approved by the U.S. Food and Drug Administration (FDA) as an extended adjuvant treatment for patients with early-stage HER2 overexpression/amplification breast cancer after surgery and trastuzumab-based adjuvant therapy. Neratinib inhibits the phosphorylation of the ErbB family and downstream pathways including ERK and Akt by covalently binding to cysteine u200bu200bresidues Cys-773 and Cys-805 of the ATP-binding domains of HER1, HER2, and HER4. Neratinib inhibits the activity of the HER2 receptor family and prevents the activation of signaling pathways, thereby reducing the growth and spread of breast cancer cells. And one study found that neratinib can inhibit the ATP-binding cassette transporter and subsequently reverse the multidrug resistance of cancer cells.

Pyrotinib, trade nameIrene, is a new generation of anti- HER2 targeted drug developed by relevant Chinese pharmaceutical companies. It has been conditionally approved by the National Medical Products Administration for the first time and can be combined with capecitabine to treat patients with HER2-positive advanced or metastatic breast cancer and patients who have previously received anthracycline or taxane chemotherapy. It is a small molecule irreversible bi-pan-ErbB TKI active on HER1, HER2 and HER4. By covalently binding to the ATP-binding site of the intracellular kinase region, the drug inhibits the formation and autophosphorylation of HER family homo/heterodimers. Its mechanism of action is similar to neratinib, thereby blocking the activation of HER family signaling pathways and tumor cell cycles and limiting tumor development.

Diarrhea is the most common side effect of these twoTKI drugs, mostly grade 1 and 2. The mechanism by which TKIs cause diarrhea remains unclear, which is different from the intestinal epithelial damage caused by chemotherapy. Currently, management of TKI-induced diarrhea is similar to chemotherapy-induced diarrhea within the scope of effective assessment, including patient education, dietary control, and pharmacological management. Neratinib may also cause headache and dizziness, and pylotinib may cause a decrease in white blood cells.

In general, although neratinib and pyrotinib are both targeted therapeutic drugs, there are significant differences in clinical application, mechanism of action, and side effects. When choosing which drug to use, the decision should be based on the patient's specific condition, physical condition, and doctor's recommendations. At the same time, patients also need to pay close attention to their physical condition when taking these drugs. If they have any discomfort, they should seek medical treatment in time.