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lapatinib (GW572016)
Lapatinib is a small-molecule tyrosine kinase inhibitor that blocks HER2 and EGFR signaling to inhibit cancer cell growth.
Lapatinib is a small-molecule tyrosine kinase inhibitor that blocks HER2 and EGFR signaling to inhibit cancer cell growth. Used for HER2-positive metastatic breast cancer (in combination with capecitabine), HER2-positive early-stage breast cancer (adjuvant therapy).
At a glance
| Generic name | lapatinib (GW572016) |
|---|---|
| Also known as | Tykerb |
| Sponsor | GlaxoSmithKline |
| Drug class | HER2/EGFR tyrosine kinase inhibitor |
| Target | HER2, EGFR |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | Phase 3 |
Mechanism of action
Lapatinib reversibly inhibits the intracellular tyrosine kinases of human epidermal growth factor receptors HER2 and EGFR. By blocking these kinases, it prevents downstream signaling pathways that drive proliferation in HER2-positive and EGFR-dependent cancers. This dual inhibition makes it particularly effective in breast cancers that overexpress HER2.
Approved indications
- HER2-positive metastatic breast cancer (in combination with capecitabine)
- HER2-positive early-stage breast cancer (adjuvant therapy)
Common side effects
- Diarrhea
- Hand-foot skin reaction
- Nausea
- Fatigue
- Rash
- Vomiting
- Dyspepsia
- Left ventricular dysfunction
Key clinical trials
- Multimodality Risk Adapted Tx Including Induction Chemo for SCCHN Amenable to Transoral Surgery (PHASE2)
- DS-8201a in Pre-treated HER2 Breast Cancer That Cannot be Surgically Removed or Has Spread [DESTINY-Breast02] (PHASE3)
- Effectiveness, Safety, and Tolerability of Anti-HER2 Drugs as Targeted Therapy for Egyptian Patients With ERBB2-Positive Breast Cancer
- Pilot Study of [68Ga]Ga-ABY-025 Imaging in Patients Undergoing Treatment With HER2-targeted Therapy (EARLY_PHASE1)
- HKI-272 for HER2-Positive Breast Cancer and Brain Metastases (PHASE2)
- Pilot Study of Veliparib (ABT-888) and Lapatinib (Tykerb) in Patients With Metastatic, Triple Negative Breast Cancer (NA)
- Molecular Profiling of Advanced Soft-tissue Sarcomas (PHASE3)
- A Randomized Phase II Trial Comparing Therapy Based on Tumor Molecular Profiling Versus Conventional Therapy in Patients With Refractory Cancer (PHASE2)
Primary sources
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| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |