Lapatinib (Tykerb)
Targeted Therapy · Approved since 2007
Description
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.
Mechanism of Action
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
Side Effects
Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.
Clinical Trials
Quick Info
| Brand Name | Tykerb |
| Category | Targeted Therapy |
 Status | Off-label |
 EMA Status | EMA Approved |
 Spain Access | Hospital use off-label in CRC |
| Administration | Oral |
| Year Approved | 2007 |
| Clinical Trials | 8 |
Related Medications
Medical Disclaimer
This information is for educational purposes only and should not replace professional medical advice. Always consult your healthcare team before making treatment decisions.