Drug glossary Targeted therapy

Lapatinib Tykerb

Used in colorectal cancer outside its approved indication. It appears in 8 clinical trials.

Oral EGFR HER2

United States Off-label

European Union EMA approved Since 2007

Spain Hospital use Used off-label in colorectal cancer

What it is

Lapatinib is an oral tyrosine kinase inhibitor that blocks both EGFR and HER2 receptors. In colorectal cancer, it has been evaluated primarily in patients with refractory disease who have progressed on standard chemotherapy regimens including 5-fluorouracil, irinotecan, and oxaliplatin. The drug is typically used in combination with chemotherapy agents such as capecitabine and oxaliplatin for patients with advanced colorectal adenocarcinoma. Lapatinib may be particularly relevant for colorectal tumors with HER2 amplification or overexpression.

How it works

Lapatinib works by reversibly binding to the ATP-binding site of both epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2) tyrosine kinases. This dual inhibition blocks downstream signaling pathways including PI3K/AKT and RAS/RAF/MEK/ERK cascades that promote tumor cell proliferation, survival, and metastasis.

Molecular targets

EGFR HER2

Common side effects

DiarrheaSkin rashNauseaFatigueHand-foot syndromeDecreased left ventricular ejection fractionHepatotoxicityQT prolongation

Not all are listed, and everyone experiences them differently. If you notice any, tell your care team.

Trials with this drug

1 recruiting

Adapting Treatment to the Tumor Molecular Alterations for Patients With Advanced Solid Tumors: MyOwnSpecificTreatment NCT02029001 Recruiting Phase 2 France Study of Trastuzumab-emtansine in Patients With HER2-positive Metastatic Colorectal Cancer Progressing After Trastuzumab and Lapatinib. NCT03418558 Unknown Phase 2 Italy Lapatinib Plus Trametinib in KRAS Mutant NSCLC NCT02230553 Archived Phase 1 Netherlands Evaluation of Trastuzumab in Combination With Lapatinib or Pertuzumab in Combination With Trastuzumab-Emtansine to Treat Patients With HER2-positive Metastatic Colorecta… NCT03225937 Unknown Phase 2 Italy Lapatinib and Cetuximab in Patients With Solid Tumors NCT01184482 Archived Phase 1 United States Phase I/II Study of Lapatinib in Combination With Oxaliplatin and Capecitabine in Subjects With Advanced Colorectal Cancer NCT00536809 Archived Phase 1 United States

See all 8 trials

At a glance

Brand name: Tykerb
Type: Targeted therapy
Route: Oral
Approved (FDA): 2007
Trials: 8 (1 recruiting)

Related drugs

CetuximabImmunotherapy372 trials PanitumumabImmunotherapy127 trials RegorafenibTargeted therapy109 trials FruquintinibTargeted therapy62 trials TrastuzumabImmunotherapy42 trials ErlotinibTargeted therapy20 trials

Medical notice

This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.

Guides that may help

Written for patients and families, in plain language.

HER2-positive colorectal cancer: what it means and which targeted treatments existBetween 3 % and 5 % of colorectal cancers have too many copies of the HER2 gene, mostly RAS wild-type tumours. It is uncommon…RAS wild-type and left-sided colon cancer: cetuximab and panitumumab explained"RAS wild-type" means your tumour has no mutations in KRAS or NRAS. In that case anti-EGFR antibodies (cetuximab, panitumumab)…Eating during chemotherapy: what the evidence supports and what it does notThere is no "anti-cancer diet" that improves the outcome of chemotherapy. What is proven is that losing weight and muscle during…

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