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Tykerb (LAPATINIB)
Tykerb works by blocking the epidermal growth factor receptor, a protein that promotes cancer cell growth.
At a glance
| Generic name | LAPATINIB |
|---|---|
| Sponsor | Novartis |
| Drug class | Kinase Inhibitor |
| Target | Epidermal growth factor receptor |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2007 |
Mechanism of action
Lapatinib is 4-anilinoquinazoline kinase inhibitor of the intracellular tyrosine kinase domains of both Epidermal Growth Factor Receptor (EGFR [ErbB1]) and of Human Epidermal Receptor Type (HER2 [ErbB2]) receptors (estimated Ki app values of 3nM and 13nM, respectively) with 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 trastuzumab-conditioned cell lines. Lapatinib retained significant activity against breast cancer cell lines selected for long-term growth in trastuzumab-containing medium in vitro. These in vitro findings suggest non-cross-resistance between these two agents.Hormone receptor-positive breast cancer cells (
Approved indications
- HER2-positive carcinoma of breast
Boxed warnings
- WARNING: HEPATOTOXICITY Hepatotoxicity has been observed in clinical trials and postmarketing experience. The hepatotoxicity may be severe and deaths have been reported. Causality of the deaths is uncertain [see Warnings and Precautions ( 5.2 )] . WARNING: HEPATOTOXICITY See full prescribing information for complete boxed warning. Hepatotoxicity has been observed in clinical trials and postmarketing experience. The hepatotoxicity may be severe and deaths have been reported. Causality of the deaths is uncertain. ( 5.2 )
Common side effects
- Diarrhea
- Nausea
- Vomiting
- Stomatitis
- Dyspepsia
- Palmar-plantar erythrodysesthesia
- Rash
- Dry skin
- Mucosal inflammation
- Pain in extremity
- Back pain
- Dyspnea
Drug interactions
- High Risk QT Prolonging Agents
- P-glycoprotein Substrates
- boceprevir
- conivaptan
- dexamethasone
- fosphenytoin
- indinavir
- itraconazole
- ketoconazole
- mibefradil
- nefazodone
- nelfinavir
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)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |