# Lapatinib

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

## TL;DR

Lapatinib was the first HER2-blocking pill (2007) and is now mostly a comparator arm and a late-line option, displaced by tucatinib and ADCs.

## Summary

Lapatinib is a reversible, ATP-competitive dual inhibitor of the EGFR and HER2 kinases, and was the first HER2-blocking pill (2007). It is approved with capecitabine for HER2-positive advanced breast cancer after trastuzumab (EGF100151: time to progression 8.4 versus 4.4 months) and with letrozole in hormone receptor-positive, HER2-positive disease. The adjuvant ALTTO trial was negative and neoadjuvant NeoALTTO raised pathological complete response but not survival, so it never established a role in early disease. Diarrhoea and rash are the main toxicities, with a hepatotoxicity warning. It has been displaced by tucatinib and by antibody-drug conjugates and now serves mainly as the control arm in ACE-Breast-02 and other Chinese ADC trials. For a newcomer, lapatinib is the original HER2 pill, now mostly a comparator and a late-line option.

## Fields

- Kind: Treatment
- Status: approved
- Last checked: 2026-09-07
- Brand: Tykerb
- Modality: Small-molecule reversible HER2/EGFR kinase inhibitor
- Mechanism: Reversible dual EGFR/HER2 ATP-competitive inhibitor.
- Approvals: US 2007: HER2+ advanced breast cancer with capecitabine after trastuzumab; US 2010: HR+/HER2+ metastatic breast cancer with letrozole
- Dosing: Oral; 1250 mg once daily with capecitabine; 1500 mg with letrozole
- Toxicity (grade 3+): Diarrhoea 13%

## Sources

- Wikipedia: https://en.wikipedia.org/wiki/Lapatinib
- FDA label (DailyMed): https://dailymed.nlm.nih.gov/dailymed/search.cfm?query=Lapatinib

## Connected records

- cancers: [Colorectal cancer](https://onco.cc/cancers/colorectal/), [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: [HER2 tyrosine kinase inhibitors](https://onco.cc/technologies/her2-tyrosine-kinase-inhibitors/), [Small-molecule kinase inhibitors](https://onco.cc/technologies/kinase-inhibitors/)
- targets: [EGFR](https://onco.cc/targets/egfr/), [HER2](https://onco.cc/targets/her2/)
- companies: [Novartis](https://onco.cc/companies/novartis/)
- trials: [A Phase Ⅲ Study of Hemay022 in Combination With AI In Advanced Breast Cancer](https://onco.cc/trials/nct06313983/), [ACE-Breast-02](https://onco.cc/trials/ace-breast-02/), [GeparSixto](https://onco.cc/trials/geparsixto/), [HERACLES](https://onco.cc/trials/heracles/), [Molecular Profiling of Advanced Soft-tissue Sarcomas](https://onco.cc/trials/nct03784014/), [NALA](https://onco.cc/trials/nala/), [SYD985 vs. Physician's Choice in Participants With HER2-positive Locally Advanced or Metastatic Breast Cancer](https://onco.cc/trials/nct03262935/)
- key papers: [A molecularly annotated platform of patient-derived xenografts identifies HER2 as an effective therapeutic target in cetuximab-resistant colorectal cancer](https://onco.cc/key-papers/paper-bertotti-xenopatients-her2-cetuximab-resistant-colorectal-cancer-discov-2011/), [Dual-targeted therapy with trastuzumab and lapatinib in treatment-refractory, KRAS codon 12/13 wild-type, HER2-positive metastatic colorectal cancer (HERACLES)](https://onco.cc/key-papers/paper-sartore-bianchi-heracles-trastuzumab-lapatinib-lancet-oncol-2016/)
- people: [Thomas Bachelot](https://onco.cc/people/thomas-bachelot/)
- pathways: [Breast cancer (KEGG map)](https://onco.cc/pathways/breast-cancer-signalling/)

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JSON: https://onco.cc/api/v1/entities/lapatinib.json