Lapatinib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2007
- First approval year
- 2007
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Lapatinib
- Molecular weight
- 581.07
- Structure (SMILES)
- CS(=O)(=O)CCNCc1ccc(-c2ccc3ncnc(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)c3c2)o1
- tyverb
- Tyverb
- apricoxib lapatinib capecitabine
- fmm
- FMM
- gsk 572016
- GSK 572016
- GSK-572016
- gsk572016
- GSK572016
- gw 2016
- gw 572016
- gw 572016x
- GW-2016
- GW-572016
- GW-572016X
- gw2016
- GW2016
- gw572016
- GW572016
- GW572016 (lapatinib)
- GW572016 (Lapatinib)
- GW572016 oral tablets
- gw572016f
- GW572016F
- lapatanib
- Lapatanib
And 34 more, listed on the interactive page.
- ATC classification codes
- L01EH01
Sources for recorded values
- CAS registry numbers
- 231277-92-2
- ChEMBL ID
- CHEMBL554
- InChIKey
- BCFGMOOMADDAQU-UHFFFAOYSA-N
- PubChem compound IDs
- 208908
- FDA ingredient codes (UNII)
- 0VUA21238F
- 480167
- 481474
- Applicant
- TEVA PHARMS USA INC
- Approval date
- 16 Aug 2024
- Application number
- ANDA217968
- Status
- Authorised
- Status date
- 10 Jun 2008
- Authorisation date
- 10 Jun 2008
- Approved indications
- Tyverb is indicated for the treatment of patients with breast cancer, whose tumours overexpress HER2 (ErbB2): in combination with capecitabine for patients with advanced or metastatic disease with progression following prior therapy, which must have included anthracyclines and taxanes and therapy with trastuzumab in the metastatic setting; in combination with trastuzumab for patients with hormone-receptor-negative metastatic disease that has progressed on prior trastuzumab therapy or therapies in combination with chemotherapy; in combination with an aromatase inhibitor for post-menopausal women with hormone-receptor-positive metastatic disease, not currently intended for chemotherapy. The patients in the registration study had not previously been treated with trastuzumab or an aromatase inhibitor. No data are available on the efficacy of this combination relative to trastuzumab in combination with an aromatase inhibitor in this patient population.
- Product number
- EMEA/H/C/000795
- Authorisation holder
- Novartis Europharm Limited
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Breast Neoplasms
European medicines record
- Patents
- 0
- Designations
- 3
- First in class
- No
- Fast track
- Yes
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- Yes
- Orphan exclusivity
- No
- Accelerated approval
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- lapatinib
- Type
- Synthetic organic
- Drug name stem
- -tinib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- epidermal growth factor receptor
- Gene symbol
- EGFR
- Protein identifier
- P00533
- Median affinity
- 8
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- erb-b2 receptor tyrosine kinase 2
- Gene symbol
- ERBB2
- Protein identifier
- P04626
- Median affinity
- 7.89
- Affinity units
- pKi
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- erb-b2 receptor tyrosine kinase 2
- Gene symbol
- ERBB2
- Protein identifier
- P04626
- Median affinity
- 8
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- erb-b2 receptor tyrosine kinase 2
- Gene symbol
- ERBB2
- Protein identifier
- P04626
- Median affinity
- 8.15
- Affinity units
- pKd
- Primary target
- Yes
- Mechanism
- Epidermal growth factor receptor erbB1 inhibitor
- Action type
- Inhibitor
- Target
- Epidermal growth factor receptor
- Mechanism
- Receptor protein-tyrosine kinase erbB-2 inhibitor
- Action type
- Inhibitor
- Target
- Receptor tyrosine-protein kinase erbB-2
- Action type
- Agonist
- Gene symbol
- INSR
- Protein identifier
- P06213
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- EGFR
- Protein identifier
- P00533
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- ERBB2
- Protein identifier
- P04626
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000181
- Subject identifier
- D002294
- Condition
- Adenocarcinoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000228
- Subject identifier
- D000230
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000305
- Subject identifier
- D001943
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000365
- Subject identifier
- D015179
- Condition
- Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0000681
- Subject identifier
- D002292
- Condition
- Carcinoma, Squamous Cell
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000707
- Subject identifier
- D002294
- Condition
- Melanoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000756
- Subject identifier
- D008545
- Condition
- Pancreatic Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0002618
- Subject identifier
- D010190
- Condition
- Thyroid Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002892
- Subject identifier
- D013964
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 2
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0003869
- Subject identifier
- D001943
- Condition
- Renal Insufficiency, Chronic
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003884
- Subject identifier
- D051436
- Condition
- Bile Duct Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005540
- Subject identifier
- D001650
- Condition
- Brain Diseases
- Highest recorded phase
- 3
- Condition identifier
- EFO:0005774
- Subject identifier
- D001927
- Condition
- Esophageal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:0005922
- Subject identifier
- D004938
- Condition
- Head and Neck Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0005950
- Subject identifier
- D006258
- Condition
- Carcinoma, Ductal
- Highest recorded phase
- 2
- Condition identifier
- EFO:0006318
- Subject identifier
- D044584
- Condition
- Head and Neck Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0006859
- Subject identifier
- D006258
- Condition
- Breast Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:1000294
- Subject identifier
- D001943
- Condition
- Paraganglioma
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000453
- Subject identifier
- D010235
- Condition
- Pituitary Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- EFO:1000478
- Subject identifier
- D010911
- Condition
- Sarcoma
- Highest recorded phase
- 3
- Condition identifier
- EFO:1001968
- Subject identifier
- D012509
- Condition
- Stomach Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0001056
- Subject identifier
- D013274
- Condition
- Brain Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0001657
- Subject identifier
- D001932
And 11 more, listed on the interactive page.
- Condition identifier
- EFO_0000181
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000228
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000305
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000432
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000707
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000756
- Highest recorded phase
- 2
- Condition identifier
- EFO_0002618
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003060
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003863
- Highest recorded phase
- 2
- Condition identifier
- EFO_0003869
- Condition identifier
- EFO_0005774
- Highest recorded phase
- 3
- Condition identifier
- EFO_0005922
- Highest recorded phase
- 2
- Condition identifier
- EFO_0005950
- Highest recorded phase
- 3
- Condition identifier
- EFO_0006318
- Highest recorded phase
- 2
- Condition identifier
- EFO_0006859
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000453
- Highest recorded phase
- 2
- Condition identifier
- EFO_1000984
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001480
- Highest recorded phase
- 2
- Condition identifier
- EFO_1001941
- Highest recorded phase
- 2
- Condition identifier
- HP_0006767
- Highest recorded phase
- 2
- Condition identifier
- HP_0009588
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0001056
- Condition identifier
- MONDO_0001056
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0002087
- Highest recorded phase
- 2
And 64 more, listed on the interactive page.
- Warning
- Black Box Warning
- Effect
- hematological toxicity
- Country
- United States
- Warning
- Black Box Warning
- Effect
- hepatotoxicity
- Country
- United States
- Event
- alanine aminotransferase increased
- Reports
- 154
- Reporting signal score
- 108.72
- Event
- blood bilirubin increased
- Reports
- 115
- Reporting signal score
- 142.131
- Event
- breast cancer
- Reports
- 94
- Reporting signal score
- 99.5541
- Event
- breast cancer metastatic
- Reports
- 95
- Reporting signal score
- 251.392
- Event
- dehydration
- Reports
- 328
- Reporting signal score
- 336.096
- Event
- diarrhoea
- Reports
- 1,415
- Reporting signal score
- 1,605.46
- Event
- disease progression
- Reports
- 353
- Reporting signal score
- 467.062
- Event
- drug hypersensitivity
- Reports
- 8
- Reporting signal score
- 74.8113
- Event
- dry skin
- Reports
- 114
- Reporting signal score
- 123.328
- Event
- ejection fraction decreased
- Reports
- 99
- Reporting signal score
- 159.572
- Event
- febrile neutropenia
- Reports
- 150
- Reporting signal score
- 117.138
- Event
- gastrointestinal toxicity
- Reports
- 49
- Reporting signal score
- 105.192
- Event
- hepatotoxicity
- Reports
- 80
- Reporting signal score
- 95.0881
- Event
- hyperbilirubinaemia
- Reports
- 59
- Reporting signal score
- 87.7228
- Event
- hypokalaemia
- Reports
- 151
- Reporting signal score
- 156.897
- Event
- malignant neoplasm progression
- Reports
- 199
- Reporting signal score
- 227.696
- Event
- metastases to bone
- Reports
- 74
- Reporting signal score
- 122.677
- Event
- metastases to central nervous system
- Reports
- 164
- Reporting signal score
- 436.658
- Event
- metastases to liver
- Reports
- 106
- Reporting signal score
- 213.52
- Event
- metastases to lung
- Reports
- 70
- Reporting signal score
- 140.152
- Event
- metastases to lymph nodes
- Reports
- 55
- Reporting signal score
- 118.738
- Event
- metastases to skin
- Reports
- 39
- Reporting signal score
- 133.076
- Event
- mucosal inflammation
- Reports
- 119
- Reporting signal score
- 149.744
- Event
- nail disorder
- Reports
- 43
- Reporting signal score
- 82.3623
- Event
- nausea
- Reports
- 553
- Reporting signal score
- 130.859
And 9 more, listed on the interactive page.
- NCT00044330
- NCT00078572
- NCT00206427
- NCT00225758
- NCT00299286
- NCT00343759
- NCT00404066
- NCT00450892
- NCT00455039
- NCT00470704
- NCT00477464
- NCT00479856
- NCT00486668
- NCT00496366
- NCT00513058
- NCT00548184
- NCT00567554
- NCT00632489
- NCT00634088
- NCT00657137
- NCT00694252
- NCT00721630
- NCT00754702
- NCT00756470
- NCT00759642
And 161 more, listed on the interactive page.
- Dose
- 1250 mg / 1500 mg
- Route
- Oral
- How often
- Once daily
- Do not divide daily doses
- Take at least one hour before or one hour after a meal
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 2
- Polar surface area
- 106.35
- Calculated partition coefficient (ALogP)
- 6.14
- Calculated partition coefficient (XLogP)
- 5.1
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 2
- Rotatable bonds
- 11
- Heavy atoms
- 40
- Molecular formula
- C29H26ClFN4O4S
- Monoisotopic mass
- 580.1347324
- Natural product
- No
- Recorded assays
- 4,366
- Active assays
- 805
- Confirmatory
- Other
- Screening
- Summary
- Tyrosine Kinase Inhibitors
- Antineoplastic Agents
These details could not be displayed.
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- A Phase 0 of Neoadjuvant Lapatinib in Infiltrative Bladder Carcinoma Before Cystectomy
- A Phase 2 Study of Brivanib in Chinese Patients With Previously Treated Advanced HCC
- A Phase I Study of Lapatinib (Tykerb) Plus Ixabepilone (Ixempra) as 2nd-line Treatment for Patients With HER-2 Overexpressed Recurrent or Persistent Endometrial Carcinoma or Carcinosarcoma
- A Phase I Study Of Oral Topotecan And Lapatinib In Subjects With Advanced Solid Tumors
- A Phase I Study to Test Alternate Oral Formulations vs the Current Tablet Formulation of Lapatinib
- A Phase Ib/II Study of BEZ235 and Trastuzumab in Patients With HER2-positive Breast Cancer Who Failed Prior to Trastuzumab
- A Phase II Clinical Study of LCB01-0371 to Evaluate the EBA, Safety and PK
- A Phase II Neo-adjuvant Study Assessing TCH (Docetaxel, Carboplatin and Trastuzumab) and TCHL (Docetaxel, Carboplatin, Trastuzumab and Lapatinib) in HER-2 Positive Breast Cancer Patients.
- A Phase II Trial of Lapatinib (TYKERB) + Pemetrexed (ALIMTA) in Advanced Non Small Cell Lung Cancer With an Initial Dose Finding Phase
- A Phase II, Randomized, Open-label Study of Lapatinib Plus Chemotherapy Versus Trastuzumab Plus Chemotherapy in HER2-positive and p95HER2-positive Metastatic Breast Cancer
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- A Randomized Controlled Trial of HER-2 Positive Breast Cancer Patients Treated With Lapatinib vs Herceptin
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In development for (37)
- Adenocarcinoma Phase 2
- Bile duct carcinoma Phase 2
- Brain cancer Phase 2
- Brain disorder Phase 3
- Breast cancer Phase 3
- Breast carcinoma Phase 3
- Breast ductal adenocarcinoma Phase 2
- Breast neoplasm Phase 3
- Cancer Phase 3
- Cervical cancer Phase 2
- Chronic kidney disease Phase 1
- Colorectal adenocarcinoma Phase 2
- Colorectal cancer Phase 2
- Endometrial cancer Phase 1
- Esophageal cancer Phase 2
- Esophageal squamous cell carcinoma Phase 2
- Exocrine pancreatic carcinoma Phase 2
- Gallbladder cancer Phase 2
- Gastric cancer Phase 2
- Head and neck cancer Phase 3
Other linked conditions (1)
- Ductal breast carcinoma in situ