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capecitabine + pyrotinib
- Development stage
- Unknown
- Lead developer
- Hengrui Pharmaceutical
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Capecitabine + pyrotinib is an oral combination therapy used primarily for the treatment of HER2-positive advanced or metastatic breast cancer. Capecitabine is a prodrug of 5-fluorouracil (5-FU), functioning as an antimetabolite that inhibits DNA synthesis in rapidly dividing tumor cells. Pyrotinib is a small-molecule, irreversible pan-ErbB receptor tyrosine kinase inhibitor targeting epidermal growth factor receptor (EGFR/HER1), HER2, and HER4. The combination has demonstrated significant efficacy in patients previously treated with taxanes, anthracyclines, and/or trastuzumab, improving progression-free survival and overall response rates compared to other regimens such as lapatinib plus capecitabine. It has been conditionally approved in China for this indication and recommended as a second-line treatment by the Chinese Society of Clinical Oncology[1][2][6][7][10].
- Brand names
- AiRuiNiXeloda
- Other names
- SHR-1258SHR1258SHR 1258capecitabinepyrotinib-Henan Cancer Hospital-breast cancer (HER2-positive metastatic)
02
Targets
ERBB4 (Erb-b2 receptor tyrosine kinase 4)TS (Thymidylate synthase)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB2 (Erb-b2 receptor tyrosine kinase 2)
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