Tykerb, Tyverb(lapatinib)
Lapatinib, Tykerb, Tyverb (lapatinib) is a small molecule pharmaceutical. Lapatinib was first approved as Tykerb on 2007-03-13. It is used to treat breast neoplasms in the USA. It has been approved in Europe to treat breast neoplasms. The pharmaceutical is active against receptor tyrosine-protein kinase erbB-2 and epidermal growth factor receptor.
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Commercial
Therapeutic Areas
Therapeutic Area | MeSH |
|---|---|
| neoplasms | D009369 |
| skin and connective tissue diseases | D017437 |
Trade Name
FDA
EMA
Lapatinib, Tykerb
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
|---|---|---|---|
| breast neoplasms | EFO_0003869 | D001943 | C50 |
Agency Specific
FDA
EMA
No data
Patent Expiration
Patent | Expires | Flag | FDA Information |
|---|---|---|---|
| Lapatinib Ditosylate, Tykerb, Novartis | |||
| 8821927 | 2029-09-18 | DS, DP | |
HCPCS
No data
Clinical
Clinical Trials
322 clinical trials
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Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Breast neoplasms | D001943 | EFO_0003869 | C50 | 61 | 110 | 33 | — | 15 | 198 |
| Neoplasm metastasis | D009362 | EFO_0009708 | — | 11 | 17 | 3 | — | 3 | 31 |
| Carcinoma | D002277 | — | C80.0 | 2 | 12 | 2 | — | 2 | 18 |
| Brain neoplasms | D001932 | EFO_0003833 | C71 | 4 | 10 | 1 | — | 1 | 16 |
| Male breast neoplasms | D018567 | — | — | 4 | 6 | 1 | — | — | 10 |
| Head and neck neoplasms | D006258 | — | — | 2 | 7 | 1 | — | — | 9 |
| Stomach neoplasms | D013274 | EFO_0003897 | C16 | 3 | 4 | 1 | — | — | 8 |
| Urinary bladder neoplasms | D001749 | — | C67 | 3 | 4 | 1 | — | — | 7 |
| Adenocarcinoma | D000230 | — | — | 2 | 5 | 1 | — | — | 6 |
| Esophageal neoplasms | D004938 | — | C15 | 3 | 3 | 1 | — | — | 6 |
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Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Recurrence | D012008 | — | — | 4 | 11 | — | — | 1 | 15 |
| Colorectal neoplasms | D015179 | — | — | 3 | 5 | — | — | 2 | 9 |
| Squamous cell carcinoma | D002294 | — | — | — | 8 | — | — | — | 8 |
| Prostatic neoplasms | D011471 | — | C61 | 2 | 4 | — | — | 2 | 7 |
| Squamous cell carcinoma of head and neck | D000077195 | — | — | 1 | 6 | — | — | — | 6 |
| Ovarian neoplasms | D010051 | EFO_0003893 | C56 | 4 | 3 | — | — | — | 6 |
| Non-small-cell lung carcinoma | D002289 | — | — | 2 | 3 | — | — | — | 5 |
| Central nervous system neoplasms | D016543 | — | — | 4 | 3 | — | — | — | 5 |
| Glioblastoma | D005909 | EFO_0000515 | — | 3 | 3 | — | — | — | 5 |
| Glioma | D005910 | EFO_0000520 | — | 3 | 3 | — | — | — | 5 |
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Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Renal cell carcinoma | D002292 | EFO_0000376 | — | 3 | — | — | — | — | 3 |
| Oncogenes | D009857 | — | — | 1 | — | — | — | 1 | 2 |
| Thyroid neoplasms | D013964 | EFO_0003841 | — | 1 | — | — | — | — | 1 |
| Lymphoma | D008223 | — | C85.9 | 1 | — | — | — | — | 1 |
| Chronic renal insufficiency | D051436 | — | N18 | 1 | — | — | — | — | 1 |
| Chronic kidney failure | D007676 | EFO_0003884 | N18.6 | 1 | — | — | — | — | 1 |
| Kidney diseases | D007674 | EFO_0003086 | N08 | 1 | — | — | — | — | 1 |
| Carcinosarcoma | D002296 | — | — | 1 | — | — | — | — | 1 |
| Mullerian mixed tumor | D018200 | — | — | 1 | — | — | — | — | 1 |
| Glandular and epithelial neoplasms | D009375 | — | — | 1 | — | — | — | — | 1 |
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Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
|---|---|---|---|---|---|---|---|---|---|
| Carcinoma in situ | D002278 | — | D09.9 | — | — | — | — | 2 | 2 |
| Intraductal carcinoma noninfiltrating | D002285 | — | D05.1 | — | — | — | — | 2 | 2 |
| Leukemia | D007938 | — | C95 | — | — | — | — | 1 | 1 |
| Myeloid leukemia acute | D015470 | — | C92.0 | — | — | — | — | 1 | 1 |
| Precursor cell lymphoblastic leukemia-lymphoma | D054198 | — | C91.0 | — | — | — | — | 1 | 1 |
| Myeloid leukemia | D007951 | — | C92 | — | — | — | — | 1 | 1 |
| Acute disease | D000208 | — | — | — | — | — | — | 1 | 1 |
| Lymphoid leukemia | D007945 | — | C91 | — | — | — | — | 1 | 1 |
| Exanthema | D005076 | — | — | — | — | — | — | 1 | 1 |
| Ductal carcinoma | D044584 | — | — | — | — | — | — | 1 | 1 |
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Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
| Drug common name | Lapatinib |
| INN | lapatinib |
| Description | Lapatinib is an organofluorine compound, an organochlorine compound, a member of quinazolines and a member of furans. It has a role as an antineoplastic agent and a tyrosine kinase inhibitor. It is functionally related to a monofluorobenzene. |
| Classification | Small molecule |
| Drug class | tyrosine kinase inhibitors |
| Image (chem structure or protein) |  |
| Structure (InChI/SMILES or Protein Sequence) | CS(=O)(=O)CCNCc1ccc(-c2ccc3ncnc(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)c3c2)o1 |
Identifiers
| PDB | — |
| CAS-ID | 231277-92-2 |
| RxCUI | — |
| ChEMBL ID | CHEMBL554 |
| ChEBI ID | 49603 |
| PubChem CID | 208908 |
| DrugBank | DB01259 |
| UNII ID | 0VUA21238F (ChemIDplus, GSRS) |
Target
Agency Approved
ERBB2
ERBB2
EGFR
EGFR
Organism
Homo sapiens
Gene name
ERBB2
Gene synonyms
HER2, MLN19, NEU, NGL
NCBI Gene ID
Protein name
receptor tyrosine-protein kinase erbB-2
Protein synonyms
c-erb B2/neu protein, CD340, herstatin, human epidermal growth factor receptor 2, Metastatic lymph node gene 19 protein, MLN 19, neuro/glioblastoma derived oncogene homolog, neuroblastoma/glioblastoma derived oncogene homolog, p185erbB2, Proto-oncogene c-ErbB-2, Proto-oncogene Neu, Tyrosine kinase-type cell surface receptor HER2, v-erb-b2 avian erythroblastic leukemia viral oncogene homolog 2, v-erb-b2 avian erythroblastic leukemia viral oncoprotein 2, v-erb-b2 erythroblastic leukemia viral oncogene homolog 2, neuro/glioblastoma derived oncogene homolog
Uniprot ID
Mouse ortholog
Erbb2 (13866)
receptor tyrosine-protein kinase erbB-2 (Q6ZPE0)
Alternate
No data
Variants
No data
Financial
No data
Trends
PubMed Central
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Safety
Black-box Warning
Black-box warning for: Lapatinib, Tykerb
Adverse Events
Top Adverse Reactions
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11,617 adverse events reported
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