# Pyrotinib

Source: https://onco.cc/drugs/pyrotinib/  
OnCo record `pyrotinib` (Treatment). Data CC BY-NC 4.0, attribute "Data from OnCo (onco.cc)"; commercial use needs a licence.

## TL;DR

Pyrotinib is an irreversible pan-ErbB kinase inhibitor pill (EGFR, HER2, HER4) from Jiangsu Hengrui, approved in China since 2018 but not in the US or EU. It is the standard HER2 pill there, given with capecitabine after trastuzumab, and the comparator that new Chinese HER2 ADCs are beating; diarrhoea affects nearly every patient.

## Summary

Pyrotinib is an irreversible pan-ErbB tyrosine kinase inhibitor covering EGFR, HER2 and HER4, developed by Jiangsu Hengrui. It is China's HER2 pill, widely used there with capecitabine for HER2-positive advanced breast cancer and in the first line with trastuzumab and chemotherapy. PHOEBE (versus lapatinib plus capecitabine) showed PFS of 12.5 versus 6.8 months, and PHILA (first line with trastuzumab plus docetaxel) showed PFS of 24.3 versus 10.4 months. It is approved in China (2018, with 2020s expansions) but not in the US or EU, and diarrhoea is near universal (95% any grade, 31% grade 3 or higher) and drives dose management. It is the control arm of HORIZON-Breast01, where the ADC trastuzumab rezetecan beat pyrotinib plus capecitabine (PFS 30.6 versus 8.3 months). For a newcomer, pyrotinib is the standard HER2 pill in China and the benchmark for the new Chinese HER2 ADCs.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-07
- Brand: Airuini
- Modality: Small-molecule irreversible pan-HER kinase inhibitor
- Mechanism: Irreversible pan-ErbB TKI (EGFR, HER2, HER4).
- Approvals: China 2018: HER2+ advanced breast cancer with capecitabine
- Dosing: Oral; 400 mg once daily with capecitabine
- Toxicity (grade 3+): Diarrhoea 31%

## Sources

- FDA label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Pyrotinib

## Connected records

- cancers: [HER2-positive breast cancer](https://onco.cc/cancers/breast-her2-positive/), [HER2-positive breast cancer with brain metastases](https://onco.cc/cancers/her2-positive-breast-brain-metastases/)
- technologies: [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/)
- targets: [EGFR](https://onco.cc/targets/egfr/), [HER2](https://onco.cc/targets/her2/)
- companies: [Jiangsu Hengrui Pharmaceuticals](https://onco.cc/companies/hengrui/)
- trials: [A Clinical Study of JS105 in Combination With Other Anti-tumor Therapies in Patients With Solid Tumors](https://onco.cc/trials/nct06208410/), [A Study of Evaluating The Effects Of Pyrotinib After Adjuvant Trastuzumab In Women With Early Stage Breast Cancer](https://onco.cc/trials/nct03980054/), [A Study of RC48-ADC Combined With Pyrotinib For Treatment of Local Advanced or Metastasis NSCLC With HER2 Mutation](https://onco.cc/trials/nct05745740/), [A Trial of Injectable SHR-A1811 in Combination With Pyrotinib or SHR-1316 in Subjects With Advanced Non-small Cell Lung Cancer](https://onco.cc/trials/nct05482568/), [A Trial of SHR-A1811 Combined With Other Antitumor Therapies in Advanced Solid Tumors.](https://onco.cc/trials/nct06015048/), [HORIZON-Breast01](https://onco.cc/trials/horizon-breast01/), [Inetetamab Plus Rapamycin and Chemotherapy for HER2+ Metastatic Breast Cancer With Abnormal Activation of PAM Pathway](https://onco.cc/trials/nct04736589/), [Pyrotinib and Vinorelbine Tartrate Capsules With or Without Inetetamab for First Line Treatment in Patients With Trastuzumab-resistant HER2-positive Advanced Breast Cancer](https://onco.cc/trials/nct04963595/)
- people: [Binghe Xu](https://onco.cc/people/xu-binghe/), [Fei Ma](https://onco.cc/people/ma-fei/), [Piaoyang Sun](https://onco.cc/people/sun-piaoyang/)
- drugs: [Poziotinib](https://onco.cc/drugs/poziotinib/)

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