Tykerb
An oral targeted therapy used in combination to treat HER2-positive breast cancer.
Where Lapatinib is approved
All regulators →Of the three regulators tracked here, the first to approve Lapatinib was the EU, on 10 Jun 2008.
From the regulators' own registers: FDA Drugs@FDA, the EMA medicines list and Health Canada's Notice of Compliance database. Dates are the first listed approval of a product containing only this substance; combination products and nationally authorised EU medicines are not counted.
How Lapatinib works
All drug targets →- Receptor protein-tyrosine kinase erbB-2 inhibitor InhibitorTarget: ERBB2 erb-b2 receptor tyrosine kinase 2✓ In ChEMBL and the Guide to Pharmacology
- Epidermal growth factor receptor erbB1 inhibitor InhibitorTarget: EGFR epidermal growth factor receptor✓ In ChEMBL and the Guide to Pharmacology
- Esophageal adenocarcinomaPhase 3
- Gastric adenocarcinomaPhase 3
- Gastric cancerPhase 3
- Gastroesophageal junction adenocarcinomaPhase 3
- Head and neck squamous cell carcinomaPhase 3
- Soft tissue sarcomaPhase 3
- Triple-negative breast carcinomaPhase 3
- Breast adenocarcinomaPhase 2/3
- NF2-related schwannomatosisPhase 2
- Adenoid cystic carcinomaPhase 2
Mechanisms and diseases from ChEMBL via the Open Targets Platform (release 26.09), ChEMBL record CHEMBL554, CC BY-SA 3.0. Targets checked against the IUPHAR/BPS Guide to PHARMACOLOGY (2026.3), ligand 5692, CC BY-SA 4.0. Trial phases are not approvals: approved uses are shown from the regulators' own records where we hold them.
NICE appraisals of Lapatinib
All NICE appraisals →NICE, which decides whether the NHS in England should fund new medicines, has published 1 technology appraisal of Lapatinib. 1 is current.
| Appraisal | NICE recommendation | Published | Status |
|---|---|---|---|
| Lapatinib or trastuzumab in combination with an aromatase inhibitor for the first-line treatment of metastatic hormone receptor-positive breast cancer that overexpresses HER2 NICE TA257 | Not recommended | 27 Jun 2012 | Current |
NICE decisions apply to the NHS in England. In Ireland the HSE decides on reimbursement, advised by the National Centre for Pharmacoeconomics. Titles, categories and dates link to the guidance on nice.org.uk. © NICE 2026 technology appraisal guidance. Available from www.nice.org.uk/guidance. All rights reserved. Subject to Notice of rights. NICE guidance is prepared for the National Health Service in England. All NICE guidance is subject to regular review and may be updated or withdrawn. NICE accepts no responsibility for the use of its content in this product/publication.
Patient leaflets for Lapatinib
The package leaflet is the official guide for patients that comes with every medicine. These links go to the regulators that publish it.
- EUEuropean Union: TyverbEMA product information: package leaflet and summary of product characteristics in every EU language.
- UKUnited Kingdom: Search MHRA ProductsPatient information leaflets and SmPCs for UK-licensed products.
- USUnited States: Search DailyMedFDA-approved labels, including patient and medication guides.
Leaflets differ between brands and countries; always read the one that comes with your own medicine. This is regulatory information, not medical advice.
Reference identifiers for Lapatinib
- ATC code
- L01XE07
- ChEMBL
- CHEMBL554
- DrugBank
- DB01259
- PubChem CID
- 208908
- CAS number
- 231277-92-2
- FDA UNII
- 0VUA21238F
- Wikidata
- Q420323
- Wikipedia
- Lapatinib
Codes that identify this medicine in other databases, from Wikidata (CC0), matched by its ChEMBL ID. The ATC code is the WHO classification of what the medicine is used for.
What Tykerb is used for
TYKERB ® is indicated in combination with: capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress human epidermal growth factor receptor 2 (HER2) and who have received prior therapy, including an anthracycline, a taxane, and trastuzumab. Limitations of Use : Patients should have disease progression on trastuzumab prior to initiation of treatment with TYKERB in combination with capecitabine. letrozole for the treatment of postmenopausal women with hormone receptor-positive metastatic breast cancer that overexpresses the HER2 receptor for whom hormonal therapy is indicated. TYKERB in combination with an aromatase inhibitor has not been compared to a trastuzumab-containing chemotherapy regimen for the treatment of metastatic breast cancer. TYKERB is a kinase inhibitor indicated in combination with: ( 1 ) capecitabine for the treatment …
How it works
12.1 Mechanism of Action Lapatinib is a 4-anilinoquinazoline kinase inhibitor of the intracellular tyrosine kinase domains of both Epidermal Growth Factor Receptor (EGFR [ErbB1]) and of Human Epidermal Receptor Type 2 (HER2 [ErbB2]) receptors (estimated K i app values of 3nM and 13nM, respectively) with a dissociation half-life of greater than or equal to 300 minutes. Lapatinib inhibits ErbB-driven tumor cell growth in vitro and in various animal models. An additive effect was demonstrated in an in vitro study when lapatinib and 5-FU (the active metabolite of capecitabine) were used in combination in the 4-tumor cell lines tested. The growth inhibitory effects of lapatinib were evaluated in…
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How this page is built
The facts on this page are pulled directly from official U.S. FDA datasets — they are not written from memory. Each field below names the dataset it came from, so you can check it yourself.
- FDA Drug Label (openFDA) ↗ Indications, mechanism of action and pharmacologic class
- Drugs@FDA ↗ First FDA approval date and the company holding the application
- FDA Drug Shortage Database ↗ Current US supply / shortage status
Plain-English summaries and drug-class explainers are written and reviewed by Sreepriya Prasannan (MSc Digital Transformation of Life Sciences (Innopharma Education / Griffith College); MSc & BSc Botany). Data is retrieved automatically from the sources above and cross-checked with AI-assisted verification (Anthropic's Claude) — brand and generic names are matched against the exact FDA product record so that a combination product or a different formulation cannot be mistaken for the drug on this page. An editor reviews the result before publication. We describe this in full in our editorial standards and corrections policy. The FDA data on this page was last retrieved on 6 Oct 2026. How every register is built: methodology · fixes we have made: corrections log.