Identification
NameLapatinib
Accession NumberDB01259  (DB02584)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Lapatinib is an anti-cancer drug developed by GlaxoSmithKline (GSK) as a treatment for solid tumours such as breast and lung cancer. It was approved by the FDA on March 13, 2007, for use in patients with advanced metastatic breast cancer in conjunction with the chemotherapy drug Capecitabine. Lapatinib is human epidermal growth factor receptor type 2 (HER2/ERBB2) and epidermal growth factor receptor (HER1/EGFR/ERBB1) tyrosine kinases inhibitor. It binds to the intracellular phosphorylation domain to prevent receptor autophosphorylation upon ligand binding.

Structure
Thumb
Synonyms
FMM
GW 572016
Lapatinib tosilate hydrate
N-(3-chloro-4-((3-Fluorophenyl)methoxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furanyl)-4-quinazolinamine
N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine
Tykerb
External IDs GW 572016 / GW572016
Product Ingredients
IngredientUNIICASInChI KeyDetails
Lapatinib ditosylateG873GX646R 388082-78-8XNRVGTHNYCNCFF-UHFFFAOYSA-NDetails
Product Images
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
TykerbTablet250 mgOralNovartis2009-06-05Not applicableCanada
TykerbTablet250 mg/1OralNovartis2016-08-03Not applicableUs
TykerbTablet250 mg/1OralGlaxosmithkline Inc2007-03-162017-11-30Us00173 0752 00 nlmimage10 8318c1b6
TyverbTablet, film coated250 mgOralNovartis Europharm Limited2008-06-10Not applicableEu
TyverbTablet, film coated250 mgOralNovartis Europharm Limited2008-06-10Not applicableEu
TyverbTablet, film coated250 mgOralNovartis Europharm Limited2008-06-10Not applicableEu
TyverbTablet, film coated250 mgOralNovartis Europharm Limited2008-06-10Not applicableEu
TyverbTablet, film coated250 mgOralNovartis Europharm Limited2008-06-10Not applicableEu
TyverbTablet, film coated250 mgOralNovartis Europharm Limited2008-06-10Not applicableEu
TyverbTablet, film coated250 mgOralNovartis Europharm Limited2008-06-10Not applicableEu
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
TycerbNot Available
Brand mixturesNot Available
Categories
UNII0VUA21238F
CAS number231277-92-2
WeightAverage: 581.058
Monoisotopic: 580.134731942
Chemical FormulaC29H26ClFN4O4S
InChI KeyBCFGMOOMADDAQU-UHFFFAOYSA-N
InChI
InChI=1S/C29H26ClFN4O4S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35)
IUPAC Name
N-{3-chloro-4-[(3-fluorophenyl)methoxy]phenyl}-6-(5-{[(2-methanesulfonylethyl)amino]methyl}furan-2-yl)quinazolin-4-amine
SMILES
CS(=O)(=O)CCNCC1=CC=C(O1)C1=CC2=C(C=C1)N=CN=C2NC1=CC(Cl)=C(OCC2=CC(F)=CC=C2)C=C1
Pharmacology
Indication

Indicated in combination with capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress the human epidermal receptor type 2 (HER2) protein and who have received prior therapy including an anthracycline, a taxane, and trastuzuma.

Structured Indications
Pharmacodynamics

Lapatinib is a small molecule and a member of the 4-anilinoquinazoline class of kinase inhibitors. An anti-cancer drug, lapatinib was developed by GlaxoSmithKline (GSK) as a treatment for solid tumours such as breast and lung cancer. It was approved by the FDA on March 13, 2007, for use in patients with advanced metastatic breast cancer in conjunction with the chemotherapy drug capecitabine.

Mechanism of action

Lapatinib is a 4-anilinoquinazoline kinase inhibitor of the intracellular tyrosine kinase domains of both epidermal growth factor receptor (HER1/EGFR/ERBB1) and human epidermal growth factor receptor type 2 (HER2/ERBB2)with a dissociation half-life of ≥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-florouracil (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.

TargetKindPharmacological actionActionsOrganismUniProt ID
Epidermal growth factor receptorProteinyes
antagonist
HumanP00533 details
Receptor tyrosine-protein kinase erbB-2Proteinyes
antagonist
HumanP04626 details
Related Articles
Absorption

Absorption following oral administration of lapatinib is incomplete and variable.

Volume of distributionNot Available
Protein binding

Highly bound (>99%) to albumin and alpha-1 acid glycoprotein

Metabolism

Lapatinib undergoes extensive metabolism, primarily by CYP3A4 and CYP3A5, with minor contributions from CYP2C19 and CYP2C8 to a variety of oxidated metabolites, none of which accounts for more than 14% of the dose recovered in the feces or 10% of lapatinib concentration in plasma.

Route of elimination

Lapatinib undergoes extensive metabolism, primarily by CYP3A4 and CYP3A5, with minor contributions from CYP2C19 and CYP2C8 to a variety of oxidated metabolites, none of which accounts for more than 14% of the dose recovered in the feces or 10% of lapatinib concentration in plasma.

Half life

Single-dose terminal half life: 14.2 hours Effective multiple-dose half life: 24 hours

ClearanceNot Available
Toxicity

There has been a report of one patient who took 3,000 mg of lapatinib for 10 days. This patient had grade 3 diarrhea and vomiting on day 10.

Affected organisms
  • Humans and other mammals
PathwaysNot Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
HLA class II histocompatibility antigen, DQ alpha 1 chainHLA-DQA1*02:01Not AvailableHLA-DQA1*02:01ADR Directly StudiedHepatoxicity Details
HLA class II histocompatibility antigen, DRB1-11 beta chainHLA-DRB1*07:01Not AvailableHLA-DRB1*07:01ADR Directly StudiedHepatoxicity Details
HLA class II histocompatibility antigen, DQ beta 1 chainHLA-DQB1*02:02Not AvailableHLA-DQB1*02:02ADR Directly StudiedHepatoxicity Details
Tenascin-X---(C;C) / (C;T)T > C ADR Directly StudiedHepatoxicity Details
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Lapatinib can be increased when it is combined with Abiraterone.Approved
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Lapatinib.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Lapatinib.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Lapatinib.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Lapatinib.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Lapatinib.Approved
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Lapatinib.Experimental
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Lapatinib.Approved, Investigational
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Lapatinib.Approved, Investigational
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Lapatinib.Approved, Investigational
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Lapatinib.Approved, Withdrawn
AmiodaroneThe serum concentration of Lapatinib can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Lapatinib.Approved
AmodiaquineThe metabolism of Amodiaquine can be decreased when combined with Lapatinib.Approved
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Lapatinib.Approved
AnagrelideLapatinib may increase the QTc-prolonging activities of Anagrelide.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Lapatinib.Approved
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Lapatinib.Approved
AprepitantThe serum concentration of Lapatinib can be increased when it is combined with Aprepitant.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Lapatinib.Approved, Investigational
ArmodafinilThe metabolism of Lapatinib can be decreased when combined with Armodafinil.Approved, Investigational
Arsenic trioxideLapatinib may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherLapatinib may increase the QTc-prolonging activities of Artemether.Approved
AsenapineLapatinib may increase the QTc-prolonging activities of Asenapine.Approved
AtazanavirThe serum concentration of Lapatinib can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Atenolol can be increased when it is combined with Lapatinib.Approved
AtomoxetineThe metabolism of Lapatinib can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe metabolism of Atorvastatin can be decreased when combined with Lapatinib.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Lapatinib.Approved, Investigational
AzelastineThe metabolism of Azelastine can be decreased when combined with Lapatinib.Approved
AzithromycinLapatinib may increase the QTc-prolonging activities of Azithromycin.Approved
BedaquilineLapatinib may increase the QTc-prolonging activities of Bedaquiline.Approved
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Lapatinib.Approved
BeraprostThe metabolism of Beraprost can be decreased when combined with Lapatinib.Investigational
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Lapatinib.Approved, Vet Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Lapatinib.Approved, Investigational
BexaroteneThe serum concentration of Lapatinib can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe serum concentration of Lapatinib can be increased when it is combined with Boceprevir.Withdrawn
BortezomibThe metabolism of Lapatinib can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Lapatinib can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Lapatinib.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Lapatinib.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Lapatinib.Approved, Investigational
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Lapatinib.Approved
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Lapatinib.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Bupropion can be decreased when combined with Lapatinib.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Lapatinib.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Lapatinib.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Lapatinib.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Lapatinib.Approved
CarbamazepineThe serum concentration of Lapatinib can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Lapatinib.Approved
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Lapatinib.Approved
CelecoxibThe metabolism of Lapatinib can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Lapatinib can be increased when it is combined with Ceritinib.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Lapatinib.Withdrawn
ChloramphenicolThe metabolism of Lapatinib can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChloroquineLapatinib may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorpromazineLapatinib may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
CholecalciferolThe metabolism of Lapatinib can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Lapatinib.Approved
CiprofloxacinLapatinib may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideLapatinib may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Lapatinib.Approved
CitalopramLapatinib may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinThe serum concentration of Lapatinib can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Lapatinib can be decreased when combined with Clemastine.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Lapatinib.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Lapatinib.Approved, Investigational
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Lapatinib.Approved
ClopidogrelThe metabolism of Lapatinib can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Lapatinib can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineLapatinib may increase the QTc-prolonging activities of Clozapine.Approved
CobicistatThe serum concentration of Lapatinib can be increased when it is combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Lapatinib.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Lapatinib.Approved
ConivaptanThe serum concentration of Lapatinib can be increased when it is combined with Conivaptan.Approved, Investigational
Conjugated estrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Lapatinib.Approved
CrizotinibLapatinib may increase the QTc-prolonging activities of Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Lapatinib.Approved, Investigational
CyclosporineThe metabolism of Lapatinib can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Lapatinib.Approved
DabrafenibThe serum concentration of Lapatinib can be decreased when it is combined with Dabrafenib.Approved
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Lapatinib.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Lapatinib.Approved
DapsoneThe metabolism of Dapsone can be decreased when combined with Lapatinib.Approved, Investigational
DarunavirThe serum concentration of Lapatinib can be increased when it is combined with Darunavir.Approved
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Lapatinib.Approved
DasatinibThe serum concentration of Lapatinib can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Lapatinib.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Lapatinib.Approved
DeferasiroxThe serum concentration of Lapatinib can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Lapatinib can be decreased when combined with Delavirdine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Lapatinib.Approved
DexamethasoneThe serum concentration of Lapatinib can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Lapatinib.Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Lapatinib.Approved, Illicit, Vet Approved
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Lapatinib.Approved, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Lapatinib.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Lapatinib.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Lapatinib.Approved
DihydroergotamineThe metabolism of Lapatinib can be decreased when combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Lapatinib.Illicit
DiltiazemThe metabolism of Lapatinib can be decreased when combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Lapatinib.Approved
DisopyramideLapatinib may increase the QTc-prolonging activities of Disopyramide.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Lapatinib.Approved, Investigational
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Lapatinib.Approved
DolasetronLapatinib may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidoneLapatinib may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Lapatinib.Approved, Investigational
DoxycyclineThe metabolism of Lapatinib can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneLapatinib may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolLapatinib may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Lapatinib.Approved
EfavirenzThe serum concentration of Lapatinib can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Lapatinib.Approved, Investigational
EliglustatLapatinib may increase the QTc-prolonging activities of Eliglustat.Approved
EltrombopagThe metabolism of Eltrombopag can be decreased when combined with Lapatinib.Approved
EnzalutamideThe serum concentration of Lapatinib can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Lapatinib.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Lapatinib.Approved, Investigational
ErythromycinLapatinib may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramLapatinib may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe serum concentration of Lapatinib can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Lapatinib can be decreased when combined with Esomeprazole.Approved, Investigational
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Lapatinib.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Lapatinib.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Lapatinib.Approved
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Lapatinib.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Lapatinib.Approved
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Lapatinib.Approved
EtravirineThe serum concentration of Lapatinib can be decreased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Lapatinib.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Lapatinib.Approved
FelodipineThe metabolism of Lapatinib can be decreased when combined with Felodipine.Approved, Investigational
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Lapatinib.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Lapatinib.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Lapatinib.Approved
FlecainideLapatinib may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Lapatinib.Approved
FluconazoleThe metabolism of Lapatinib can be decreased when combined with Fluconazole.Approved
FluorouracilThe metabolism of Fluorouracil can be decreased when combined with Lapatinib.Approved
FluoxetineLapatinib may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolLapatinib may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Lapatinib.Approved
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Lapatinib.Approved
FluvoxamineThe metabolism of Lapatinib can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Lapatinib can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Lapatinib can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Lapatinib can be decreased when it is combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Lapatinib can be increased when it is combined with Fusidic Acid.Approved
Gadobenic acidLapatinib may increase the QTc-prolonging activities of Gadobenic acid.Approved
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Lapatinib.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Lapatinib.Approved
GemfibrozilThe metabolism of Lapatinib can be decreased when combined with Gemfibrozil.Approved
GemifloxacinLapatinib may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GoserelinLapatinib may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronLapatinib may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Lapatinib.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Lapatinib.Withdrawn
HalofantrineThe metabolism of Halofantrine can be decreased when combined with Lapatinib.Approved
HaloperidolLapatinib may increase the QTc-prolonging activities of Haloperidol.Approved
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Lapatinib.Approved, Illicit
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Lapatinib.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Lapatinib.Approved
IbutilideLapatinib may increase the QTc-prolonging activities of Ibutilide.Approved
IdelalisibThe serum concentration of Lapatinib can be increased when it is combined with Idelalisib.Approved
IfosfamideThe metabolism of Ifosfamide can be decreased when combined with Lapatinib.Approved
IloperidoneLapatinib may increase the QTc-prolonging activities of Iloperidone.Approved
ImatinibThe metabolism of Lapatinib can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Lapatinib.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Lapatinib.Approved
IndinavirThe serum concentration of Lapatinib can be increased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Lapatinib.Approved, Investigational
IrbesartanThe metabolism of Lapatinib can be decreased when combined with Irbesartan.Approved, Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Lapatinib.Approved, Investigational
IsavuconazoniumThe metabolism of Lapatinib can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Lapatinib can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Lapatinib can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Lapatinib can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Lapatinib can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Lapatinib.Approved, Vet Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Lapatinib.Approved
KetamineThe metabolism of Ketamine can be decreased when combined with Lapatinib.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Lapatinib.Approved
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Lapatinib.Approved
KetoconazoleThe serum concentration of Lapatinib can be increased when it is combined with Ketoconazole.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Lapatinib.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Lapatinib.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Lapatinib.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Lapatinib.Approved
LenvatinibLapatinib may increase the QTc-prolonging activities of Lenvatinib.Approved
LeuprolideLapatinib may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Lapatinib.Approved, Investigational
LevofloxacinLapatinib may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Lapatinib.Approved
LicofeloneThe metabolism of Licofelone can be decreased when combined with Lapatinib.Investigational
LidocaineThe metabolism of Lidocaine can be decreased when combined with Lapatinib.Approved, Vet Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Lapatinib.Approved
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Lapatinib.Approved
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Lapatinib.Approved
LopinavirThe serum concentration of Lapatinib can be increased when it is combined with Lopinavir.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Lapatinib.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Lapatinib.Approved
LovastatinThe metabolism of Lapatinib can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Lapatinib can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Lapatinib can be decreased when it is combined with Lumacaftor.Approved
LumefantrineLapatinib may increase the QTc-prolonging activities of Lumefantrine.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Lapatinib.Approved, Investigational
Mefenamic acidThe metabolism of Mefenamic acid can be decreased when combined with Lapatinib.Approved
MeloxicamThe metabolism of Meloxicam can be decreased when combined with Lapatinib.Approved, Vet Approved
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Lapatinib.Investigational, Withdrawn
MethadoneLapatinib may increase the QTc-prolonging activities of Methadone.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Lapatinib.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Lapatinib.Approved, Vet Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Lapatinib.Approved, Investigational
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Lapatinib.Approved, Illicit
MifepristoneThe serum concentration of Lapatinib can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Lapatinib.Approved
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Lapatinib.Approved
MitotaneThe serum concentration of Lapatinib can be decreased when it is combined with Mitotane.Approved
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Lapatinib.Approved, Investigational
MoclobemideThe metabolism of Lapatinib can be decreased when combined with Moclobemide.Approved
ModafinilThe serum concentration of Lapatinib can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Morphine can be increased when it is combined with Lapatinib.Approved, Investigational
MoxifloxacinLapatinib may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Lapatinib.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Lapatinib.Approved
NafcillinThe serum concentration of Lapatinib can be decreased when it is combined with Nafcillin.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Lapatinib.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Lapatinib.Approved, Vet Approved
NaproxenThe metabolism of Naproxen can be decreased when combined with Lapatinib.Approved, Vet Approved
NefazodoneThe serum concentration of Lapatinib can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Lapatinib can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Lapatinib can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Lapatinib can be decreased when it is combined with Nevirapine.Approved
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Lapatinib.Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Lapatinib.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Lapatinib.Approved
NilotinibLapatinib may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Lapatinib.Approved
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Lapatinib.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Lapatinib.Approved
OfloxacinLapatinib may increase the QTc-prolonging activities of Ofloxacin.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Lapatinib.Approved, Investigational
OlaparibThe metabolism of Lapatinib can be decreased when combined with Olaparib.Approved
OleandrinAnvirzel may decrease the cardiotoxic activities of Lapatinib.Experimental
OlodaterolThe metabolism of Olodaterol can be decreased when combined with Lapatinib.Approved
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Lapatinib.Approved
OmeprazoleThe metabolism of Lapatinib can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronLapatinib may increase the QTc-prolonging activities of Ondansetron.Approved
OsimertinibThe serum concentration of Lapatinib can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Lapatinib.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Lapatinib.Approved, Vet Approved
PalbociclibThe serum concentration of Lapatinib can be increased when it is combined with Palbociclib.Approved
PaliperidoneLapatinib may increase the QTc-prolonging activities of Paliperidone.Approved
PanobinostatLapatinib may increase the QTc-prolonging activities of Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Lapatinib can be decreased when combined with Pantoprazole.Approved
ParamethadioneThe metabolism of Paramethadione can be decreased when combined with Lapatinib.Approved
PazopanibLapatinib may increase the QTc-prolonging activities of Pazopanib.Approved
PentamidineLapatinib may increase the QTc-prolonging activities of Pentamidine.Approved
PentobarbitalThe serum concentration of Lapatinib can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerflutrenLapatinib may increase the QTc-prolonging activities of Perflutren.Approved
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Lapatinib.Approved
PhenobarbitalThe serum concentration of Lapatinib can be decreased when it is combined with Phenobarbital.Approved
PhenprocoumonThe metabolism of Phenprocoumon can be decreased when combined with Lapatinib.Approved
PhenytoinThe serum concentration of Lapatinib can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PimozideThe serum concentration of Pimozide can be increased when it is combined with Lapatinib.Approved
PioglitazoneThe metabolism of Lapatinib can be decreased when combined with Pioglitazone.Approved, Investigational
PiroxicamThe metabolism of Piroxicam can be decreased when combined with Lapatinib.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Lapatinib.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Lapatinib.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Lapatinib.Approved
PosaconazoleThe serum concentration of Lapatinib can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Lapatinib.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Lapatinib.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Lapatinib.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Lapatinib.Approved, Vet Approved
PrimaquineLapatinib may increase the QTc-prolonging activities of Primaquine.Approved
PrimidoneThe serum concentration of Lapatinib can be decreased when it is combined with Primidone.Approved, Vet Approved
ProcainamideLapatinib may increase the QTc-prolonging activities of Procainamide.Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Lapatinib.Approved, Vet Approved
PromazineLapatinib may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PropafenoneLapatinib may increase the QTc-prolonging activities of Propafenone.Approved
PropofolThe metabolism of Propofol can be decreased when combined with Lapatinib.Approved, Investigational, Vet Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Lapatinib.Approved, Investigational
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Lapatinib.Approved
QuetiapineLapatinib may increase the QTc-prolonging activities of Quetiapine.Approved
QuinidineLapatinib may increase the QTc-prolonging activities of Quinidine.Approved
QuinineLapatinib may increase the QTc-prolonging activities of Quinine.Approved
RabeprazoleThe metabolism of Lapatinib can be decreased when combined with Rabeprazole.Approved, Investigational
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Lapatinib.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Lapatinib.Approved, Investigational
RepaglinideThe metabolism of Repaglinide can be decreased when combined with Lapatinib.Approved, Investigational
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Lapatinib.Approved
RifabutinThe serum concentration of Lapatinib can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Lapatinib can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Lapatinib can be decreased when it is combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Lapatinib.Approved, Investigational
RiociguatThe metabolism of Riociguat can be decreased when combined with Lapatinib.Approved
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Lapatinib.Approved, Investigational
RitonavirThe serum concentration of Lapatinib can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Lapatinib.Approved
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Lapatinib.Investigational, Withdrawn
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Lapatinib.Approved, Investigational
RosiglitazoneThe metabolism of Lapatinib can be decreased when combined with Rosiglitazone.Approved, Investigational
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Lapatinib.Approved, Vet Approved
SaquinavirThe serum concentration of Lapatinib can be increased when it is combined with Saquinavir.Approved, Investigational
SecobarbitalThe metabolism of Lapatinib can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe metabolism of Selegiline can be decreased when combined with Lapatinib.Approved, Investigational, Vet Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Lapatinib.Approved
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Lapatinib.Approved
SertralineThe metabolism of Lapatinib can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Lapatinib can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Lapatinib.Approved
SiltuximabThe serum concentration of Lapatinib can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Lapatinib can be increased when it is combined with Simeprevir.Approved
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Lapatinib.Approved
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Lapatinib.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Lapatinib.Approved
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Lapatinib.Approved, Investigational
SotalolLapatinib may increase the QTc-prolonging activities of Sotalol.Approved
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Lapatinib.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Lapatinib.Experimental
St. John's WortThe serum concentration of Lapatinib can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Lapatinib can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Sulfadiazine can be decreased when combined with Lapatinib.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Lapatinib can be decreased when combined with Sulfamethoxazole.Approved
SulfinpyrazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Lapatinib.Approved
SulfisoxazoleLapatinib may increase the QTc-prolonging activities of Sulfisoxazole.Approved, Vet Approved
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Lapatinib.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Lapatinib.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Lapatinib.Experimental
TazaroteneThe metabolism of Tazarotene can be decreased when combined with Lapatinib.Approved, Investigational
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Lapatinib.Approved
TelaprevirThe serum concentration of Lapatinib can be increased when it is combined with Telaprevir.Withdrawn
TelavancinLapatinib may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinThe serum concentration of Lapatinib can be increased when it is combined with Telithromycin.Approved
TemazepamThe metabolism of Temazepam can be decreased when combined with Lapatinib.Approved
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Lapatinib.Approved
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Lapatinib.Approved, Investigational, Vet Approved
TeriflunomideThe metabolism of Lapatinib can be decreased when combined with Teriflunomide.Approved
TestosteroneThe metabolism of Testosterone can be decreased when combined with Lapatinib.Approved, Investigational
TetrabenazineLapatinib may increase the QTc-prolonging activities of Tetrabenazine.Approved
TheophyllineThe metabolism of Theophylline can be decreased when combined with Lapatinib.Approved
ThioridazineLapatinib may increase the QTc-prolonging activities of Thioridazine.Withdrawn
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Lapatinib.Approved
TiclopidineThe metabolism of Lapatinib can be decreased when combined with Ticlopidine.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Lapatinib.Approved
TocilizumabThe serum concentration of Lapatinib can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Tolbutamide can be decreased when combined with Lapatinib.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Lapatinib.Approved
TopiramateThe metabolism of Lapatinib can be decreased when combined with Topiramate.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Lapatinib.Approved, Investigational
TorasemideThe metabolism of Torasemide can be decreased when combined with Lapatinib.Approved
ToremifeneLapatinib may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
TranylcypromineThe metabolism of Lapatinib can be decreased when combined with Tranylcypromine.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Lapatinib.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lapatinib.Approved
TretinoinThe metabolism of Tretinoin can be decreased when combined with Lapatinib.Approved, Investigational, Nutraceutical
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Lapatinib.Approved
TrimethoprimThe metabolism of Lapatinib can be decreased when combined with Trimethoprim.Approved, Vet Approved
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Lapatinib.Withdrawn
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Lapatinib.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Lapatinib.Approved
VandetanibLapatinib may increase the QTc-prolonging activities of Vandetanib.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Lapatinib.Approved
VemurafenibLapatinib may increase the QTc-prolonging activities of Vemurafenib.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Lapatinib.Approved
VenlafaxineThe metabolism of Lapatinib can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Lapatinib can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Lapatinib.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Lapatinib.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Lapatinib.Approved
VoriconazoleThe serum concentration of Lapatinib can be increased when it is combined with Voriconazole.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Lapatinib.Approved
WarfarinThe metabolism of Warfarin can be decreased when combined with Lapatinib.Approved
ZafirlukastThe metabolism of Zafirlukast can be decreased when combined with Lapatinib.Approved, Investigational
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Lapatinib.Approved
ZiprasidoneLapatinib may increase the QTc-prolonging activities of Ziprasidone.Approved
ZopicloneThe metabolism of Zopiclone can be decreased when combined with Lapatinib.Approved
ZuclopenthixolLapatinib may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceUS6727256
General References
  1. Nelson MH, Dolder CR: Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. Ann Pharmacother. 2006 Feb;40(2):261-9. Epub 2006 Jan 17. [PubMed:16418322 ]
  2. Burris HA 3rd: Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. Oncologist. 2004;9 Suppl 3:10-5. [PubMed:15163842 ]
  3. Burris HA 3rd, Hurwitz HI, Dees EC, Dowlati A, Blackwell KL, O'Neil B, Marcom PK, Ellis MJ, Overmoyer B, Jones SF, Harris JL, Smith DA, Koch KM, Stead A, Mangum S, Spector NL: Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. J Clin Oncol. 2005 Aug 10;23(23):5305-13. Epub 2005 Jun 13. [PubMed:15955900 ]
  4. Geyer CE, Forster J, Lindquist D, Chan S, Romieu CG, Pienkowski T, Jagiello-Gruszfeld A, Crown J, Chan A, Kaufman B, Skarlos D, Campone M, Davidson N, Berger M, Oliva C, Rubin SD, Stein S, Cameron D: Lapatinib plus capecitabine for HER2-positive advanced breast cancer. N Engl J Med. 2006 Dec 28;355(26):2733-43. [PubMed:17192538 ]
  5. Johnston SR, Leary A: Lapatinib: a novel EGFR/HER2 tyrosine kinase inhibitor for cancer. Drugs Today (Barc). 2006 Jul;42(7):441-53. [PubMed:16894399 ]
  6. Tevaarwerk AJ, Kolesar JM: Lapatinib: a small-molecule inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor-2 tyrosine kinases used in the treatment of breast cancer. Clin Ther. 2009;31 Pt 2:2332-48. doi: 10.1016/j.clinthera.2009.11.029. [PubMed:20110044 ]
  7. Medina PJ, Goodin S: Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Clin Ther. 2008 Aug;30(8):1426-47. doi: 10.1016/j.clinthera.2008.08.008. [PubMed:18803986 ]
External Links
ATC CodesL01XE07 — Lapatinib
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
Clinical Trials
Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingDiagnosticNeoplasms, Breast1
0TerminatedNot AvailableBladder Carcinoma / Cystectomy / Infiltrative Bladder Carcinoma1
0TerminatedTreatmentEpithelial Cancer1
0Unknown StatusBasic ScienceAcoustic Schwannoma / Auditory Tumor / Neurofibromatosis 2 / NF2 / Vestibular Schwannomas1
0Unknown StatusTreatmentCancer, Breast1
1Active Not RecruitingTreatmentCancer, Advanced1
1Active Not RecruitingTreatmentHER2/Neu Positive / Invasive Breast Carcinoma / Recurrent Breast Carcinoma / Stage IV Breast Cancer1
1Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)1
1Active Not RecruitingTreatmentNeoplasms, Breast2
1CompletedNot AvailableAdvanced or Metastatic ErbB2-overexpressing Breast Cancer / Neoplasms, Breast1
1CompletedNot AvailableCancers1
1CompletedTreatmentAdvanced Cancers2
1CompletedTreatmentAdvanced Colorectal Cancer / Metastatic Colorectal Cancers / Neoplasms, Colorectal / Responsive to Fluoropyrimidines1
1CompletedTreatmentAdvanced Non-Small Cell Lung Cancer / Lung Cancer, Non-Small Cell1
1CompletedTreatmentAdvanced Solid Tumors / Cancer, Breast1
1CompletedTreatmentAdvanced or Metastatic ErbB2-overexpressing Breast Cancer / Neoplasms, Breast1
1CompletedTreatmentAnemia of Chronic Kidney Disease1
1CompletedTreatmentBladder Cancers / Brain and Central Nervous System Tumors / Cancer, Breast / Cancer, Ovarian / Esophageal Cancers / Extragonadal Germ Cell Tumor / Lung Cancers / Malignant Neoplasm of Stomach / Prostate Cancer1
1CompletedTreatmentBladder Cancers / Transitional Cell Cancer of the Renal Pelvis and Ureter1
1CompletedTreatmentCancer, Breast7
1CompletedTreatmentCancer, Breast / Cancers / Locally Recurrent and Metastatic Breast Cancer / Metastases / Metastatic Cancers / Neoplasms, Breast / Oncology / Tumors / Tumors, Breast / Tumors, Solid1
1CompletedTreatmentCancer, Breast / Metastatic Brain Tumors1
1CompletedTreatmentCancer, Breast / Metastatic Cancers1
1CompletedTreatmentCancer, Breast / Metastatic ErbB2 / Neoplasms, Breast1
1CompletedTreatmentCancer, Breast / Neoplasms, Breast1
1CompletedTreatmentCancers1
1CompletedTreatmentCancers / Neoplasms, Breast1
1CompletedTreatmentCancers / Renal Cell Adenocarcinoma1
1CompletedTreatmentColorectal Cancers / Head and Neck Carcinoma / Lung Cancers1
1CompletedTreatmentHER-2 Gene Amplification1
1CompletedTreatmentHER2 Positive / Metastatic Brain Tumors / Metastatic Breast Cancer (MBC)1
1CompletedTreatmentHER2-positive Breast Cancer / Male Breast Cancer / Recurrent Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentLocally Advanced Breast Cancer (LABC) / Metastatic Breast Cancer (MBC)1
1CompletedTreatmentMalignant Lymphomas / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentNeoplasms, Breast4
1CompletedTreatmentNeoplasms, Breast / Solid Tumor Cancers1
1CompletedTreatmentRenal Cell Adenocarcinoma1
1CompletedTreatmentSolid Tumor Cancers1
1CompletedTreatmentTumors, Solid2
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific2
1RecruitingTreatmentBRAF V600E Mutation Present / BRAF V600K Mutation Present / Metastatic Malignant Neoplasm in the Thyroid Gland / Recurrent Thyroid Gland Carcinoma / Unresectable Thyroid Gland Carcinoma1
1RecruitingTreatmentNeuroblastomas1
1TerminatedTreatmentAdenocarcinomas of the Gastroesophageal Junction / HER2-positive Breast Cancer / Male Breast Cancer / Recurrent Breast Cancer / Recurrent Esophageal Cancer / Recurrent Gastric Cancer / Stage IIIC Breast Cancer / Stage IIIC Esophageal Cancer / Stage IIIC Gastric Cancer / Stage IV Breast Cancer / Stage IV Esophageal Cancer / Stage IV Gastric Cancer1
1TerminatedTreatmentAdvanced Solid Tumors1
1TerminatedTreatmentCancer, Ovarian1
1TerminatedTreatmentEstrogen Receptor Negative / Estrogen Receptor Positive / HER2/Neu Positive / Progesterone Receptor Negative / Progesterone Receptor Positive / Recurrent Breast Carcinoma / Stage IV Breast Cancer1
1TerminatedTreatmentFailure or Contraindication of Trastuzumab Therapy / First or Second Line Therapy / HER2 Positive / Metastatic Breast Cancer (MBC)1
1TerminatedTreatmentHER-2 Positive Breast Cancer / Malignant Neoplasm of Breast1
1TerminatedTreatmentLocally Advanced or Metastatic Breast Cancer1
1TerminatedTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
1Unknown StatusTreatmentCancer, Breast1
1Unknown StatusTreatmentRecurrent Endometrial Cancer1
1WithdrawnNot AvailableCancer, Breast1
1WithdrawnTreatmentHealthy Volunteers1
1, 2Active Not RecruitingTreatmentCentral Nervous System Metastases / HER2-positive Breast Cancer / Male Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer1
1, 2Active Not RecruitingTreatmentHER2 Positive Metastatic Breast Cancers1
1, 2CompletedNot AvailableMetastatic Breast Cancer (MBC)1
1, 2CompletedTreatmentBrain and Central Nervous System Tumors1
1, 2CompletedTreatmentCancer, Breast4
1, 2CompletedTreatmentHead and Neck Carcinoma1
1, 2CompletedTreatmentMetastatic Breast Cancer (MBC)1
1, 2CompletedTreatmentOvarian Epithelial Cancer Stage III / Stage IV Breast Cancer / Stage IV Ovarian Cancer1
1, 2CompletedTreatmentRecurrent Childhood Anaplastic Astrocytoma / Recurrent Childhood Brain Stem Glioma / Recurrent Childhood Ependymoma / Recurrent Childhood Giant Cell Glioblastoma / Recurrent Childhood Glioblastoma / Recurrent Childhood Gliosarcoma / Recurrent Childhood Medulloblastoma / Recurrent Childhood Oligodendroglioma1
1, 2RecruitingTreatmentColorectal Cancers1
1, 2RecruitingTreatmentMetastatic Breast Cancer (MBC)1
1, 2SuspendedTreatmentCancer, Breast1
1, 2TerminatedTreatmentAdenocarcinoma of the Esophagus / Adenocarcinomas of the Gastroesophageal Junction1
1, 2TerminatedTreatmentCancer, Breast / Neoplasms Metastasis1
1, 2TerminatedTreatmentHER2 Positive Metastatic Breast Cancers1
1, 2TerminatedTreatmentMetastatic Breast Cancer (MBC)1
1, 2TerminatedTreatmentProstate Cancer1
1, 2Unknown StatusTreatmentMetastatic Breast Cancer (MBC)1
2Active Not RecruitingTreatmentAdvanced Breast Cancer / Cancer, Breast1
2Active Not RecruitingTreatmentCancer, Breast5
2Active Not RecruitingTreatmentCancers1
2Active Not RecruitingTreatmentGeriatric Health Services / HER2/Neu Positive / Neoplasms, Breast1
2Active Not RecruitingTreatmentHER2-Positive Early Stage Breast Cancer1
2Active Not RecruitingTreatmentHER2/Neu Positive / Recurrent Breast Carcinoma / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
2Active Not RecruitingTreatmentHead and Neck Carcinoma / Metastatic Squamous Neck Cancer With Occult Primary Squamous Cell Carcinoma / Recurrent Metastatic Squamous Neck Cancer With Occult Primary / Recurrent Salivary Gland Cancer / Recurrent Squamous Cell Carcinoma of the Hypopharynx / Recurrent Squamous Cell Carcinoma of the Larynx / Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity / Recurrent Squamous Cell Carcinoma of the Oropharynx / Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Recurrent Verrucous Carcinoma of the Larynx / Recurrent Verrucous Carcinoma of the Oral Cavity / Salivary Gland Squamous Cell Carcinoma / Stage IV Salivary Gland Cancer / Stage IV Squamous Cell Carcinoma of the Hypopharynx / Stage IV Squamous Cell Carcinoma of the Larynx / Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IV Squamous Cell Carcinoma of the Oropharynx / Stage IV Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IV Verrucous Carcinoma of the Larynx / Stage IV Verrucous Carcinoma of the Oral Cavity1
2Active Not RecruitingTreatmentHead and Neck Carcinoma / Squamous Cell Carcinoma (SCC)1
2Active Not RecruitingTreatmentHead and Neck Carcinoma / Squamous Cell Carcinoma of the Head and Neck (SCCHN)1
2Active Not RecruitingTreatmentMetastatic Breast Cancer (MBC)2
2Active Not RecruitingTreatmentMetastatic Breast Cancer With Intracranial Metastases1
2Active Not RecruitingTreatmentMetastatic Cancers1
2Active Not RecruitingTreatmentNeoplasms, Brain / Spinal Cord Tumors1
2Active Not RecruitingTreatmentNeoplasms, Breast4
2Active Not RecruitingTreatmentNon-HPV Locally Advanced Head and Neck Cancer1
2CompletedTreatment70 Years Old Patients and Over / After One Line of Chemotherapy With Trastuzumab / Metastatic Breast Cancer (MBC)1
2CompletedTreatmentAdenocarcinomas1
2CompletedTreatmentAdult Primary Hepatocellular Carcinoma / Advanced Adult Primary Liver Cancer / Localized Unresectable Adult Primary Liver Cancer / Recurrent Adult Primary Liver Cancer / Recurrent Extrahepatic Bile Duct Cancer / Recurrent Gallbladder Cancer / Unresectable Extrahepatic Bile Duct Cancer / Unresectable Gallbladder Cancer2
2CompletedTreatmentBrain Cancer / Pediatric Cancers1
2CompletedTreatmentCancer, Breast8
2CompletedTreatmentCancer, Breast / Cardiac Toxicity1
2CompletedTreatmentCancer, Breast / ErbB1 Expressing / ErbB2 Overexpressing / Inflammatory / Neoplasms, Breast / Newly Diagnosed1
2CompletedTreatmentCancer, Breast / Metastatic Breast Cancer (MBC)1
2CompletedTreatmentCancer, Breast / Metastatic Cancers1
2CompletedTreatmentCancer, Ovarian / Peritoneal Cavity Cancer1
2CompletedTreatmentCancers2
2CompletedTreatmentCentral Nervous System Metastases / HER2-positive Breast Cancer / Male Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer / Tumors Metastatic to Brain1
2CompletedTreatmentColorectal Cancers1
2CompletedTreatmentDiffuse Adenocarcinoma of the Stomach / Intestinal Adenocarcinoma of the Stomach / Mixed Adenocarcinoma of the Stomach / Recurrent Gastric Cancer / Stage III Gastric Cancer / Stage IV Gastric Cancer1
2CompletedTreatmentEstrogen Receptor Positive / Male Breast Carcinoma / Progesterone Receptor Positive / Recurrent Breast Carcinoma / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
2CompletedTreatmentGBM / Glioblastoma Multiforme / Gliomas / Gliosarcoma / GS / Neoplasms, Brain1
2CompletedTreatmentGliomas1
2CompletedTreatmentHER2-positive Breast Cancer / Stage II Breast Cancer / Stage IIIA Breast Cancer1
2CompletedTreatmentHER2-positive Refractory Advanced Cancer1
2CompletedTreatmentHigh-grade Salivary Gland Carcinoma / High-grade Salivary Gland Mucoepidermoid Carcinoma / Low-grade Salivary Gland Carcinoma / Low-grade Salivary Gland Mucoepidermoid Carcinoma / Recurrent Adenoid Cystic Carcinoma of the Oral Cavity / Recurrent Salivary Gland Cancer / Salivary Gland Acinic Cell Tumor / Salivary Gland Adenocarcinoma / Salivary Gland Adenoid Cystic Carcinoma / Salivary Gland Malignant Mixed Cell Type Tumor1
2CompletedTreatmentLung Tumors / Metastatic Brain Tumors / Tumors, Breast1
2CompletedTreatmentMalignant Neoplasm of Pancreas1
2CompletedTreatmentMetastatic Breast Cancer (MBC)1
2CompletedTreatmentMetastatic Breast Cancer (MBC) / Neoplasms, Breast1
2CompletedTreatmentMetastatic Colorectal Cancers1
2CompletedTreatmentMetastatic Squamous Neck Cancer With Occult Primary / Recurrent Metastatic Squamous Neck Cancer With Occult Primary / Recurrent Squamous Cell Carcinoma of the Hypopharynx / Recurrent Squamous Cell Carcinoma of the Larynx / Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity / Recurrent Squamous Cell Carcinoma of the Nasopharynx / Recurrent Squamous Cell Carcinoma of the Oropharynx / Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Salivary Gland Squamous Cell Carcinoma / Stage IV Squamous Cell Carcinoma of the Hypopharynx / Stage IV Squamous Cell Carcinoma of the Larynx / Stage IV Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IV Squamous Cell Carcinoma of the Nasopharynx / Stage IV Squamous Cell Carcinoma of the Oropharynx / Stage IV Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Untreated Metastatic Squamous Neck Cancer With Occult Primary1
2CompletedTreatmentNeoplasms, Breast11
2CompletedTreatmentNeoplasms, Gastrointestinal Tract1
2CompletedTreatmentNeoplasms, Head and Neck1
2CompletedTreatmentNeoplasms, Uterine Cervix / Recurrent, IV-B Cervical cancer1
2CompletedTreatmentNeurofibromatosis 2 / Vestibular Schwannomas1
2CompletedTreatmentPrimary Peritoneal Cavity Cancer / Recurrent Ovarian Epithelial Cancer1
2CompletedTreatmentProstate Cancer1
2CompletedTreatmentRecurrent Endometrial Carcinoma1
2CompletedTreatmentRecurrent Prostate Cancer / Stage I Prostate Cancer / Stage IIA Prostate Cancer / Stage IIB Prostate Cancer / Stage III Prostate Cancer1
2CompletedTreatmentRecurrent Prostate Cancer / Stage IV Prostate Cancer1
2CompletedTreatmentRecurrent Salivary Gland Cancer / Recurrent Squamous Cell Carcinoma of the Hypopharynx / Recurrent Squamous Cell Carcinoma of the Larynx / Recurrent Squamous Cell Carcinoma of the Lip and Oral Cavity / Recurrent Squamous Cell Carcinoma of the Nasopharynx / Recurrent Squamous Cell Carcinoma of the Oropharynx / Recurrent Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Recurrent Verrucous Carcinoma of the Larynx / Recurrent Verrucous Carcinoma of the Oral Cavity / Salivary Gland Squamous Cell Carcinoma / Stage IV Squamous Cell Carcinoma of the Hypopharynx / Stage IV Squamous Cell Carcinoma of the Nasopharynx / Stage IVA Salivary Gland Cancer / Stage IVA Squamous Cell Carcinoma of the Larynx / Stage IVA Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IVA Squamous Cell Carcinoma of the Oropharynx / Stage IVA Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IVA Verrucous Carcinoma of the Larynx / Stage IVA Verrucous Carcinoma of the Oral Cavity / Stage IVB Salivary Gland Cancer / Stage IVB Squamous Cell Carcinoma of the Larynx / Stage IVB Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IVB Squamous Cell Carcinoma of the Oropharynx / Stage IVB Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IVB Verrucous Carcinoma of the Larynx / Stage IVB Verrucous Carcinoma of the Oral Cavity / Stage IVC Salivary Gland Cancer / Stage IVC Squamous Cell Carcinoma of the Larynx / Stage IVC Squamous Cell Carcinoma of the Lip and Oral Cavity / Stage IVC Squamous Cell Carcinoma of the Oropharynx / Stage IVC Squamous Cell Carcinoma of the Paranasal Sinus and Nasal Cavity / Stage IVC Verrucous Carcinoma of the Larynx / Stage IVC Verrucous Carcinoma of the Oral Cavity / Tongue Cancer1
2CompletedTreatmentSquamous Cell Carcinoma of Head and Neck1
2RecruitingTreatmentCancer, Breast1
2RecruitingTreatmentCarcinoma, Ductal, Breast1
2RecruitingTreatmentCholangiocarcinoma of the Extrahepatic Bile Duct / Gallbladder Cancer1
2RecruitingTreatmentERBB2 Gene Amplification / HER2 Positive Breast Carcinoma / HER2/Neu Positive / Invasive Breast Carcinoma / Male Breast Carcinoma / Metastatic Malignant Neoplasm in the Brain / Recurrent Breast Carcinoma / Stage IV Breast Cancer1
2RecruitingTreatmentHER2 Positive Breast Cancers1
2RecruitingTreatmentHER2-positive Breast Cancer / Recurrent Breast Cancer / Stage IV Breast Cancer1
2RecruitingTreatmentHER2-positive Gastric Cancer Patients With Liver Metastasis1
2RecruitingTreatmentMalignant Solid Neoplasms1
2RecruitingTreatmentMetastatic Breast Cancer (MBC)2
2RecruitingTreatmentMetastatic Colorectal Cancers1
2RecruitingTreatmentNon-Small-Cell Lung Carcinoma (NSCLC) / Small Cell Lung Carcinoma / Thymic Carcinoma1
2RecruitingTreatmentPituitary Adenomas / Prolactinomas1
2TerminatedTreatmentAdenocarcinomas of the Gastroesophageal Junction / Malignant Neoplasm of Stomach1
2TerminatedTreatmentAdvanced Breast Cancer / Cancer, Breast / HER2/Neu-positive Breast Cancer / Metastatic Breast Cancer (MBC)1
2TerminatedTreatmentCancer of the Breast / Cancer, Breast / Neoplasms, Breast1
2TerminatedTreatmentCancer, Breast4
2TerminatedTreatmentCancers1
2TerminatedTreatmentCancer treatment / Cancers / Ovarian / Relapses1
2TerminatedTreatmentEndocrine Breast Diseases / Neoplasms Metastasis / Neoplasms, Breast1
2TerminatedTreatmentGastrooesophageal Cancer1
2TerminatedTreatmentHER2 Positive Esophagogastric Cancer1
2TerminatedTreatmentLung Cancer, Non-Small Cell / Non-Small-Cell Lung Cancer (NSCLC)1
2TerminatedTreatmentMale Breast Cancer / Recurrent Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
2TerminatedTreatmentMalignant Melanoma1
2TerminatedTreatmentMalignant Neoplasm of Pancreas1
2TerminatedTreatmentMetastatic Breast Cancer (MBC)4
2TerminatedTreatmentMetastatic or Recurrent Squamous Cell Carcinoma of the Esophagus1
2TerminatedTreatmentNeoplasms, Breast3
2TerminatedTreatmentNeoplasms, Breast / Relapsed Breast Cancer1
2TerminatedTreatmentPancreatic Cancer Metastatic1
2TerminatedTreatmentRecurrent Bladder Cancer / Stage III Bladder Cancer / Stage IV Bladder Cancer / Transitional Cell Carcinoma of the Bladder1
2TerminatedTreatmentSquamous Cell Carcinoma (SCC)1
2Unknown StatusTreatmentErbB2-Positive Stage I-III Breast Cancer1
2Unknown StatusTreatmentMetastatic Breast Cancer (MBC)1
2WithdrawnTreatmentBladder Cancers / Urothelial Cancer1
2WithdrawnTreatmentCancer, Breast2
2WithdrawnTreatmentNeoplasms, Breast3
2, 3Active Not RecruitingTreatmentBladder Cancers1
2, 3CompletedTreatmentHER-2 Positive Breast Cancer / Inflammatory carcinoma of breast stage IV / Inflammatory carcinoma of the breast / Invasive Ductal Breast Carcinoma / Malignant Neoplasm of Female Breast / Mucinous Breast Cancer Stage II / Tubular Breast Cancer Stage II / Tubular Breast Cancer Stage III1
2, 3RecruitingTreatmentHER2-positive Breast Cancer1
2, 3RecruitingTreatmentOesophagogastric Cancer1
3Active Not RecruitingTreatmentBreast Cancer Invasive Nos1
3Active Not RecruitingTreatmentCancer, Breast1
3Active Not RecruitingTreatmentCancers1
3Active Not RecruitingTreatmentEstrogen Receptor Positive / HER2 Positive Breast Carcinoma / HER2/Neu Negative / Progesterone Receptor Positive / Recurrent Breast Carcinoma / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer / Stage IV Breast Cancer1
3Active Not RecruitingTreatmentHER2/Neu Positive / Male Breast Carcinoma / Stage IIA Breast Cancer / Stage IIB Breast Cancer / Stage IIIA Breast Cancer / Stage IIIB Breast Cancer / Stage IIIC Breast Cancer1
3Active Not RecruitingTreatmentMetastatic Brain Tumors1
3Active Not RecruitingTreatmentNeoplasms, Breast5
3Active Not RecruitingTreatmentNeoplasms, Gastrointestinal Tract1
3CompletedTreatmentCancer, Breast2
3CompletedTreatmentNeoplasms, Breast3
3CompletedTreatmentNeoplasms, Gastrointestinal Tract1
3CompletedTreatmentNeoplasms, Head and Neck1
3RecruitingTreatmentCancer, Breast1
3RecruitingTreatmentHER2+ Metastatic Breast Cancer (MBC)1
3RecruitingTreatmentHER2-negative Metastatic Breast Cancer / HER2-positive Circulating Tumor Cells1
3RecruitingTreatmentMetastatic Breast Cancer (MBC)1
3TerminatedTreatmentMetastatic Breast Cancer (MBC)1
3Unknown StatusTreatmentCancer, Breast2
4Approved for MarketingNot AvailableNeoplasms, Breast1
4CompletedTreatmentCancers1
Not AvailableActive Not RecruitingNot AvailableNeoplasms, Breast1
Not AvailableActive Not RecruitingDiagnosticAdvanced Solid Tumors / Cancers1
Not AvailableCompletedNot AvailableCancer, Breast / Metastatic Cancers1
Not AvailableCompletedNot AvailableCancers2
Not AvailableCompletedTreatmentDuctal Breast Carcinoma In Situ / HER2-positive Breast Cancer1
Not AvailableRecruitingTreatmentAdult Anaplastic Astrocytoma / Adult Anaplastic Ependymoma / Adult Anaplastic Oligodendroglioma / Adult Giant Cell Glioblastoma / Adult Glioblastoma / Adult Gliosarcoma / Adult Mixed Glioma / Anaplastic Astrocytoma (AA) / Anaplastic Ependymoma / Anaplastic Oligodendroglioma (AO) / Gliosarcoma / Mixed Gliomas / Recurrent Adult Brain Neoplasm / Recurrent Glioblastoma1
Not AvailableRecruitingTreatmentMetastatic Triple Negative Breast Cancer1
Not AvailableTerminatedBasic ScienceDuctal Carcinoma In Situ1
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
TabletOral250 mg
TabletOral250 mg/1
Tablet, film coatedOral250 mg
Prices
Unit descriptionCostUnit
Tykerb 250 mg tablet28.4USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2413134 No2010-05-112021-06-28Canada
CA2317589 No2007-08-082019-01-08Canada
US6391874 No1997-07-112017-07-11Us
US6713485 No2000-09-292020-09-29Us
US6727256 No1999-01-082019-01-08Us
US6828320 No1997-07-112017-07-11Us
US8821927 No2009-09-182029-09-18Us
US8513262 No1999-01-082019-01-08Us
US7157466 No2001-11-192021-11-19Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP5.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0223 mg/mLALOGPS
logP5.18ALOGPS
logP4.64ChemAxon
logS-4.4ALOGPS
pKa (Strongest Acidic)15.99ChemAxon
pKa (Strongest Basic)7.2ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area106.35 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity152.42 m3·mol-1ChemAxon
Polarizability61.19 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.6201
Caco-2 permeable-0.5858
P-glycoprotein substrateSubstrate0.7403
P-glycoprotein inhibitor IInhibitor0.5414
P-glycoprotein inhibitor IINon-inhibitor0.7799
Renal organic cation transporterNon-inhibitor0.7442
CYP450 2C9 substrateNon-substrate0.6688
CYP450 2D6 substrateNon-substrate0.7644
CYP450 3A4 substrateSubstrate0.6619
CYP450 1A2 substrateInhibitor0.5386
CYP450 2C9 inhibitorNon-inhibitor0.5544
CYP450 2D6 inhibitorNon-inhibitor0.7861
CYP450 2C19 inhibitorInhibitor0.5274
CYP450 3A4 inhibitorInhibitor0.8065
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9104
Ames testNon AMES toxic0.543
CarcinogenicityNon-carcinogens0.6788
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5867 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.537
hERG inhibition (predictor II)Inhibitor0.8417
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
LC-MS/MSLC-MS/MS Spectrum - , positivesplash10-00lr-0009070000-0d55ba750eaa2fb12020View in MoNA
LC-MS/MSLC-MS/MS Spectrum - , positivesplash10-0ab9-0649800000-87742edfe3489dab4ac8View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-qTof , PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as quinazolinamines. These are heterocyclic aromatic compounds containing a quianazoline moiety substituted by one or more amine groups.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazanaphthalenes
Sub ClassBenzodiazines
Direct ParentQuinazolinamines
Alternative ParentsPhenoxy compounds / Phenol ethers / Aniline and substituted anilines / Alkyl aryl ethers / Aminopyrimidines and derivatives / Aralkylamines / Chlorobenzenes / Fluorobenzenes / Aryl chlorides / Aryl fluorides
SubstituentsQuinazolinamine / Phenol ether / Phenoxy compound / Aniline or substituted anilines / Halobenzene / Alkyl aryl ether / Aminopyrimidine / Fluorobenzene / Aralkylamine / Chlorobenzene
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptorsorganofluorine compound, organochlorine compound, furans, quinazolines (CHEBI:49603 )

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Ubiquitin protein ligase binding
Specific Function:
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses. Known ligands include EGF, TGFA/TGF-alpha, amphiregulin, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF. Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on ke...
Gene Name:
EGFR
Uniprot ID:
P00533
Uniprot Name:
Epidermal growth factor receptor
Molecular Weight:
134276.185 Da
References
  1. Xia W, Mullin RJ, Keith BR, Liu LH, Ma H, Rusnak DW, Owens G, Alligood KJ, Spector NL: Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. Oncogene. 2002 Sep 12;21(41):6255-63. [PubMed:12214266 ]
  2. Grana TM, Sartor CI, Cox AD: Epidermal growth factor receptor autocrine signaling in RIE-1 cells transformed by the Ras oncogene enhances radiation resistance. Cancer Res. 2003 Nov 15;63(22):7807-14. [PubMed:14633707 ]
  3. Xia W, Liu LH, Ho P, Spector NL: Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016. Oncogene. 2004 Jan 22;23(3):646-53. [PubMed:14737100 ]
  4. Zhou H, Kim YS, Peletier A, McCall W, Earp HS, Sartor CI: Effects of the EGFR/HER2 kinase inhibitor GW572016 on EGFR- and HER2-overexpressing breast cancer cell line proliferation, radiosensitization, and resistance. Int J Radiat Oncol Biol Phys. 2004 Feb 1;58(2):344-52. [PubMed:14751502 ]
  5. Langer CJ: Emerging role of epidermal growth factor receptor inhibition in therapy for advanced malignancy: focus on NSCLC. Int J Radiat Oncol Biol Phys. 2004 Mar 1;58(3):991-1002. [PubMed:14967461 ]
  6. Burris HA 3rd: Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. Oncologist. 2004;9 Suppl 3:10-5. [PubMed:15163842 ]
  7. Wood ER, Truesdale AT, McDonald OB, Yuan D, Hassell A, Dickerson SH, Ellis B, Pennisi C, Horne E, Lackey K, Alligood KJ, Rusnak DW, Gilmer TM, Shewchuk L: A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res. 2004 Sep 15;64(18):6652-9. [PubMed:15374980 ]
  8. Vazquez-Martin A, Oliveras-Ferraros C, Cufi S, Del Barco S, Martin-Castillo B, Menendez JA: Lapatinib, a dual HER1/HER2 tyrosine kinase inhibitor, augments basal cleavage of HER2 extracellular domain (ECD) to inhibit HER2-driven cancer cell growth. J Cell Physiol. 2011 Jan;226(1):52-7. doi: 10.1002/jcp.22333. [PubMed:20658522 ]
  9. Johnston SR, Leary A: Lapatinib: a novel EGFR/HER2 tyrosine kinase inhibitor for cancer. Drugs Today (Barc). 2006 Jul;42(7):441-53. [PubMed:16894399 ]
  10. Tevaarwerk AJ, Kolesar JM: Lapatinib: a small-molecule inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor-2 tyrosine kinases used in the treatment of breast cancer. Clin Ther. 2009;31 Pt 2:2332-48. doi: 10.1016/j.clinthera.2009.11.029. [PubMed:20110044 ]
  11. Medina PJ, Goodin S: Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Clin Ther. 2008 Aug;30(8):1426-47. doi: 10.1016/j.clinthera.2008.08.008. [PubMed:18803986 ]
  12. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Transmembrane signaling receptor activity
Specific Function:
Protein tyrosine kinase that is part of several cell surface receptor complexes, but that apparently needs a coreceptor for ligand binding. Essential component of a neuregulin-receptor complex, although neuregulins do not interact with it alone. GP30 is a potential ligand for this receptor. Regulates outgrowth and stabilization of peripheral microtubules (MTs). Upon ERBB2 activation, the MEMO1-...
Gene Name:
ERBB2
Uniprot ID:
P04626
Uniprot Name:
Receptor tyrosine-protein kinase erbB-2
Molecular Weight:
137909.27 Da
References
  1. Xia W, Liu LH, Ho P, Spector NL: Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016. Oncogene. 2004 Jan 22;23(3):646-53. [PubMed:14737100 ]
  2. Zhou H, Kim YS, Peletier A, McCall W, Earp HS, Sartor CI: Effects of the EGFR/HER2 kinase inhibitor GW572016 on EGFR- and HER2-overexpressing breast cancer cell line proliferation, radiosensitization, and resistance. Int J Radiat Oncol Biol Phys. 2004 Feb 1;58(2):344-52. [PubMed:14751502 ]
  3. Langer CJ: Emerging role of epidermal growth factor receptor inhibition in therapy for advanced malignancy: focus on NSCLC. Int J Radiat Oncol Biol Phys. 2004 Mar 1;58(3):991-1002. [PubMed:14967461 ]
  4. Burris HA 3rd: Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. Oncologist. 2004;9 Suppl 3:10-5. [PubMed:15163842 ]
  5. Wood ER, Truesdale AT, McDonald OB, Yuan D, Hassell A, Dickerson SH, Ellis B, Pennisi C, Horne E, Lackey K, Alligood KJ, Rusnak DW, Gilmer TM, Shewchuk L: A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res. 2004 Sep 15;64(18):6652-9. [PubMed:15374980 ]
  6. Grana TM, Sartor CI, Cox AD: Epidermal growth factor receptor autocrine signaling in RIE-1 cells transformed by the Ras oncogene enhances radiation resistance. Cancer Res. 2003 Nov 15;63(22):7807-14. [PubMed:14633707 ]
  7. Xia W, Mullin RJ, Keith BR, Liu LH, Ma H, Rusnak DW, Owens G, Alligood KJ, Spector NL: Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. Oncogene. 2002 Sep 12;21(41):6255-63. [PubMed:12214266 ]
  8. Vazquez-Martin A, Oliveras-Ferraros C, Cufi S, Del Barco S, Martin-Castillo B, Menendez JA: Lapatinib, a dual HER1/HER2 tyrosine kinase inhibitor, augments basal cleavage of HER2 extracellular domain (ECD) to inhibit HER2-driven cancer cell growth. J Cell Physiol. 2011 Jan;226(1):52-7. doi: 10.1002/jcp.22333. [PubMed:20658522 ]
  9. Johnston SR, Leary A: Lapatinib: a novel EGFR/HER2 tyrosine kinase inhibitor for cancer. Drugs Today (Barc). 2006 Jul;42(7):441-53. [PubMed:16894399 ]
  10. Tevaarwerk AJ, Kolesar JM: Lapatinib: a small-molecule inhibitor of epidermal growth factor receptor and human epidermal growth factor receptor-2 tyrosine kinases used in the treatment of breast cancer. Clin Ther. 2009;31 Pt 2:2332-48. doi: 10.1016/j.clinthera.2009.11.029. [PubMed:20110044 ]
  11. Medina PJ, Goodin S: Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Clin Ther. 2008 Aug;30(8):1426-47. doi: 10.1016/j.clinthera.2008.08.008. [PubMed:18803986 ]
  12. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Uniprot Name:
Cytochrome P450 3A4
Molecular Weight:
57342.67 Da
References
  1. Medina PJ, Goodin S: Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Clin Ther. 2008 Aug;30(8):1426-47. doi: 10.1016/j.clinthera.2008.08.008. [PubMed:18803986 ]
  2. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
  3. Teng WC, Oh JW, New LS, Wahlin MD, Nelson SD, Ho HK, Chan EC: Mechanism-based inactivation of cytochrome P450 3A4 by lapatinib. Mol Pharmacol. 2010 Oct;78(4):693-703. doi: 10.1124/mol.110.065839. Epub 2010 Jul 12. [PubMed:20624855 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Uniprot Name:
Cytochrome P450 3A5
Molecular Weight:
57108.065 Da
References
  1. Medina PJ, Goodin S: Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Clin Ther. 2008 Aug;30(8):1426-47. doi: 10.1016/j.clinthera.2008.08.008. [PubMed:18803986 ]
  2. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Uniprot Name:
Cytochrome P450 2C8
Molecular Weight:
55824.275 Da
References
  1. Medina PJ, Goodin S: Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Clin Ther. 2008 Aug;30(8):1426-47. doi: 10.1016/j.clinthera.2008.08.008. [PubMed:18803986 ]
  2. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Uniprot Name:
Cytochrome P450 2C19
Molecular Weight:
55930.545 Da
References
  1. Medina PJ, Goodin S: Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases. Clin Ther. 2008 Aug;30(8):1426-47. doi: 10.1016/j.clinthera.2008.08.008. [PubMed:18803986 ]
  2. van Erp NP, Gelderblom H, Guchelaar HJ: Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009 Dec;35(8):692-706. doi: 10.1016/j.ctrv.2009.08.004. Epub 2009 Sep 5. [PubMed:19733976 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Uniprot Name:
Multidrug resistance protein 1
Molecular Weight:
141477.255 Da
References
  1. Dai CL, Tiwari AK, Wu CP, Su XD, Wang SR, Liu DG, Ashby CR Jr, Huang Y, Robey RW, Liang YJ, Chen LM, Shi CJ, Ambudkar SV, Chen ZS, Fu LW: Lapatinib (Tykerb, GW572016) reverses multidrug resistance in cancer cells by inhibiting the activity of ATP-binding cassette subfamily B member 1 and G member 2. Cancer Res. 2008 Oct 1;68(19):7905-14. doi: 10.1158/0008-5472.CAN-08-0499. [PubMed:18829547 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Tap2 binding
Specific Function:
Involved in the transport of antigens from the cytoplasm to the endoplasmic reticulum for association with MHC class I molecules. Also acts as a molecular scaffold for the final stage of MHC class I folding, namely the binding of peptide. Nascent MHC class I molecules associate with TAP via tapasin. Inhibited by the covalent attachment of herpes simplex virus ICP47 protein, which blocks the pep...
Gene Name:
TAP1
Uniprot ID:
Q03518
Uniprot Name:
Antigen peptide transporter 1
Molecular Weight:
87216.855 Da
References
  1. Dai CL, Tiwari AK, Wu CP, Su XD, Wang SR, Liu DG, Ashby CR Jr, Huang Y, Robey RW, Liang YJ, Chen LM, Shi CJ, Ambudkar SV, Chen ZS, Fu LW: Lapatinib (Tykerb, GW572016) reverses multidrug resistance in cancer cells by inhibiting the activity of ATP-binding cassette subfamily B member 1 and G member 2. Cancer Res. 2008 Oct 1;68(19):7905-14. doi: 10.1158/0008-5472.CAN-08-0499. [PubMed:18829547 ]
Drug created on May 16, 2007 11:27 / Updated on August 08, 2017 11:08