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Identification
NameLapatinib
Accession NumberDB01259  (DB02584)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionLapatinib 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 Identifiers
  • GW 572016
  • GW572016
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Tykerbtablet250 mg/1oralGlaxo Smith Kline Llc2007-03-16Not applicableUs
Tykerbtablet250 mgoralNovartis Pharmaceuticals Canada Inc2009-06-05Not applicableCanada
TyverbFilm-coated tablet250 mgOral useNovartis Europharm Limited2008-06-10Not applicableEu
TyverbFilm-coated tablet250 mgOral useNovartis Europharm Limited2008-06-10Not applicableEu
TyverbFilm-coated tablet250 mgOral useNovartis Europharm Limited2008-06-10Not applicableEu
TyverbFilm-coated tablet250 mgOral useNovartis Europharm Limited2008-06-10Not applicableEu
TyverbFilm-coated tablet250 mgOral useNovartis Europharm Limited2008-06-10Not applicableEu
TyverbFilm-coated tablet250 mgOral useNovartis Europharm Limited2008-06-10Not applicableEu
TyverbFilm-coated tablet250 mgOral useNovartis 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
Salts
Name/CASStructureProperties
Lapatinib ditosylate
388082-78-8
Thumb
  • InChI Key: XNRVGTHNYCNCFF-UHFFFAOYSA-N
  • Monoisotopic Mass: 942.1841276
  • Average Mass: 943.47
DBSALT001785
Categories
UNII0VUA21238F
CAS number231277-92-2
WeightAverage: 581.058
Monoisotopic: 580.134731942
Chemical FormulaC29H26ClFN4O4S
InChI KeyInChIKey=BCFGMOOMADDAQU-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
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
ClassNaphthyridines
Sub ClassQuinazolines
Direct ParentQuinazolinamines
Alternative Parents
Substituents
  • Quinazolinamine
  • Phenol ether
  • Aralkylamine
  • Halobenzene
  • Fluorobenzene
  • Chlorobenzene
  • Aminopyrimidine
  • Alkyl aryl ether
  • Imidolactam
  • Benzenoid
  • Pyrimidine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Aryl chloride
  • Heteroaromatic compound
  • Sulfonyl
  • Sulfone
  • Furan
  • Oxacycle
  • Azacycle
  • Secondary amine
  • Ether
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationIndicated 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.
PharmacodynamicsLapatinib 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 actionLapatinib 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.
Related Articles
AbsorptionAbsorption following oral administration of lapatinib is incomplete and variable.
Volume of distributionNot Available
Protein bindingHighly 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 eliminationLapatinib 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 lifeSingle-dose terminal half life: 14.2 hours Effective multiple-dose half life: 24 hours
ClearanceNot Available
ToxicityThere 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
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral250 mg/1
Tabletoral250 mg
Film-coated tabletOral use250 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)
CA2317589 No2007-08-082019-01-08Canada
CA2413134 No2010-05-112021-06-28Canada
US6391874 No1997-07-112017-07-11Us
US6713485 No2000-09-292020-09-29Us
US6727256 No1999-01-082019-01-08Us
US6828320 No1997-07-112017-07-11Us
US7157466 No2001-11-192021-11-19Us
US8513262 No1999-01-082019-01-08Us
US8821927 No2009-09-182029-09-18Us
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 FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
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
References
Synthesis Reference

DrugSyn.org

US6727256
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
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Lapatinib can be increased when it is combined with Abiraterone.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Lapatinib.
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Lapatinib.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Lapatinib.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Lapatinib.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Lapatinib.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Lapatinib.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Lapatinib.
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Lapatinib.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Lapatinib.
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Lapatinib.
AmiodaroneThe serum concentration of Lapatinib can be increased when it is combined with Amiodarone.
AmiodaroneThe metabolism of Amiodarone can be decreased when combined with Lapatinib.
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Lapatinib.
AmodiaquineThe metabolism of Amodiaquine can be decreased when combined with Lapatinib.
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Lapatinib.
AnagrelideLapatinib may increase the QTc-prolonging activities of Anagrelide.
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Lapatinib.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Lapatinib.
AprepitantThe serum concentration of Lapatinib can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Lapatinib.
ArmodafinilThe metabolism of Lapatinib can be decreased when combined with Armodafinil.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Lapatinib.
ArtemetherLapatinib may increase the QTc-prolonging activities of Artemether.
AsenapineLapatinib may increase the QTc-prolonging activities of Asenapine.
AtazanavirThe serum concentration of Lapatinib can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Atenolol can be increased when it is combined with Lapatinib.
AtomoxetineThe metabolism of Lapatinib can be decreased when combined with Atomoxetine.
AtorvastatinThe metabolism of Atorvastatin can be decreased when combined with Lapatinib.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Lapatinib.
AzelastineThe metabolism of Azelastine can be decreased when combined with Lapatinib.
AzithromycinLapatinib may increase the QTc-prolonging activities of Azithromycin.
BedaquilineLapatinib may increase the QTc-prolonging activities of Bedaquiline.
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Lapatinib.
BeraprostThe metabolism of Beraprost can be decreased when combined with Lapatinib.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Lapatinib.
BevacizumabBevacizumab may increase the cardiotoxic activities of Lapatinib.
BexaroteneThe serum concentration of Lapatinib can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Lapatinib can be increased when it is combined with Boceprevir.
BortezomibThe metabolism of Lapatinib can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Lapatinib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Lapatinib.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Lapatinib.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Lapatinib.
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Lapatinib.
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Lapatinib.
BupropionThe metabolism of Bupropion can be decreased when combined with Lapatinib.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Lapatinib.
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Lapatinib.
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Lapatinib.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Lapatinib.
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Lapatinib.
CarbamazepineThe serum concentration of Lapatinib can be decreased when it is combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Lapatinib.
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Lapatinib.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Lapatinib.
CelecoxibThe metabolism of Lapatinib can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Lapatinib can be increased when it is combined with Ceritinib.
CeritinibLapatinib may increase the QTc-prolonging activities of Ceritinib.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Lapatinib.
ChloramphenicolThe metabolism of Lapatinib can be decreased when combined with Chloramphenicol.
ChloroquineLapatinib may increase the QTc-prolonging activities of Chloroquine.
ChlorpromazineLapatinib may increase the QTc-prolonging activities of Chlorpromazine.
CholecalciferolThe metabolism of Lapatinib can be decreased when combined with Cholecalciferol.
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Lapatinib.
CimetidineThe metabolism of Lapatinib can be decreased when combined with Cimetidine.
CiprofloxacinLapatinib may increase the QTc-prolonging activities of Ciprofloxacin.
CisaprideThe metabolism of Cisapride can be decreased when combined with Lapatinib.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Lapatinib.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Lapatinib.
CitalopramThe metabolism of Lapatinib can be decreased when combined with Citalopram.
ClarithromycinThe serum concentration of Lapatinib can be increased when it is combined with Clarithromycin.
ClarithromycinLapatinib may increase the QTc-prolonging activities of Clarithromycin.
ClemastineThe metabolism of Lapatinib can be decreased when combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Lapatinib.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Lapatinib.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Lapatinib.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Lapatinib.
ClopidogrelThe metabolism of Lapatinib can be decreased when combined with Clopidogrel.
ClotrimazoleThe metabolism of Lapatinib can be decreased when combined with Clotrimazole.
ClozapineLapatinib may increase the QTc-prolonging activities of Clozapine.
CobicistatThe serum concentration of Lapatinib can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Lapatinib.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Lapatinib.
ConivaptanThe serum concentration of Lapatinib can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Lapatinib.
CrizotinibLapatinib may increase the QTc-prolonging activities of Crizotinib.
CrizotinibThe metabolism of Lapatinib can be decreased when combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Lapatinib.
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Lapatinib.
CyclosporineThe metabolism of Lapatinib can be decreased when combined with Cyclosporine.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Lapatinib.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Lapatinib.
DabrafenibThe serum concentration of Lapatinib can be decreased when it is combined with Dabrafenib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Lapatinib.
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Lapatinib.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Lapatinib.
DapsoneThe metabolism of Dapsone can be decreased when combined with Lapatinib.
DarunavirThe serum concentration of Lapatinib can be increased when it is combined with Darunavir.
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Lapatinib.
DasatinibThe serum concentration of Lapatinib can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Lapatinib.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Lapatinib.
DeferasiroxThe serum concentration of Lapatinib can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Lapatinib can be decreased when combined with Delavirdine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Lapatinib.
DexamethasoneThe serum concentration of Lapatinib can be decreased when it is combined with Dexamethasone.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Lapatinib.
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Lapatinib.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Lapatinib.
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Lapatinib.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Lapatinib.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Lapatinib.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Lapatinib.
DigoxinDigoxin may decrease the cardiotoxic activities of Lapatinib.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Lapatinib.
DihydroergotamineThe metabolism of Lapatinib can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Lapatinib.
DiltiazemThe metabolism of Lapatinib can be decreased when combined with Diltiazem.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Lapatinib.
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Lapatinib.
DisopyramideLapatinib may increase the QTc-prolonging activities of Disopyramide.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Lapatinib.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Lapatinib.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Lapatinib.
DolasetronLapatinib may increase the QTc-prolonging activities of Dolasetron.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Lapatinib.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Lapatinib.
DoxycyclineThe metabolism of Lapatinib can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Lapatinib can be decreased when combined with Dronedarone.
DronedaroneLapatinib may increase the QTc-prolonging activities of Dronedarone.
DroperidolLapatinib may increase the QTc-prolonging activities of Droperidol.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Lapatinib.
EfavirenzThe serum concentration of Lapatinib can be decreased when it is combined with Efavirenz.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Lapatinib.
EliglustatLapatinib may increase the QTc-prolonging activities of Eliglustat.
EltrombopagThe metabolism of Eltrombopag can be decreased when combined with Lapatinib.
EnzalutamideThe serum concentration of Lapatinib can be decreased when it is combined with Enzalutamide.
EnzalutamideThe metabolism of Enzalutamide can be decreased when combined with Lapatinib.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Lapatinib.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Lapatinib.
ErythromycinLapatinib may increase the QTc-prolonging activities of Erythromycin.
ErythromycinThe metabolism of Lapatinib can be decreased when combined with Erythromycin.
EscitalopramLapatinib may increase the QTc-prolonging activities of Escitalopram.
Eslicarbazepine acetateThe serum concentration of Lapatinib can be decreased when it is combined with Eslicarbazepine acetate.
EsomeprazoleThe metabolism of Lapatinib can be decreased when combined with Esomeprazole.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Lapatinib.
EstriolThe serum concentration of Estriol can be increased when it is combined with Lapatinib.
EstroneThe serum concentration of Estrone can be increased when it is combined with Lapatinib.
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Lapatinib.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Lapatinib.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Lapatinib.
EtravirineThe serum concentration of Lapatinib can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Lapatinib.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Lapatinib.
FelodipineThe metabolism of Lapatinib can be decreased when combined with Felodipine.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Lapatinib.
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Lapatinib.
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Lapatinib.
FlecainideLapatinib may increase the QTc-prolonging activities of Flecainide.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Lapatinib.
FluconazoleThe metabolism of Lapatinib can be decreased when combined with Fluconazole.
FluorouracilThe metabolism of Fluorouracil can be decreased when combined with Lapatinib.
FluoxetineLapatinib may increase the QTc-prolonging activities of Fluoxetine.
FluoxetineThe metabolism of Lapatinib can be decreased when combined with Fluoxetine.
FlupentixolLapatinib may increase the QTc-prolonging activities of Flupentixol.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Lapatinib.
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Lapatinib.
FluvoxamineThe metabolism of Lapatinib can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Lapatinib can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Lapatinib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Lapatinib can be decreased when it is combined with Fosphenytoin.
FosphenytoinThe metabolism of Fosphenytoin can be decreased when combined with Lapatinib.
Fusidic AcidThe serum concentration of Lapatinib can be increased when it is combined with Fusidic Acid.
Gadobenic acidLapatinib may increase the QTc-prolonging activities of Gadobenic acid.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Lapatinib.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Lapatinib.
GemfibrozilThe metabolism of Lapatinib can be decreased when combined with Gemfibrozil.
GemifloxacinLapatinib may increase the QTc-prolonging activities of Gemifloxacin.
GoserelinLapatinib may increase the QTc-prolonging activities of Goserelin.
GranisetronLapatinib may increase the QTc-prolonging activities of Granisetron.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Lapatinib.
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Lapatinib.
HalofantrineThe metabolism of Halofantrine can be decreased when combined with Lapatinib.
HaloperidolLapatinib may increase the QTc-prolonging activities of Haloperidol.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Lapatinib.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Lapatinib.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Lapatinib.
IbutilideLapatinib may increase the QTc-prolonging activities of Ibutilide.
IdelalisibThe serum concentration of Lapatinib can be increased when it is combined with Idelalisib.
IfosfamideThe metabolism of Ifosfamide can be decreased when combined with Lapatinib.
IloperidoneLapatinib may increase the QTc-prolonging activities of Iloperidone.
ImatinibThe metabolism of Lapatinib can be decreased when combined with Imatinib.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Lapatinib.
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Lapatinib.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Lapatinib.
IndinavirThe serum concentration of Lapatinib can be increased when it is combined with Indinavir.
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Lapatinib.
IrbesartanThe metabolism of Lapatinib can be decreased when combined with Irbesartan.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Lapatinib.
IsavuconazoniumThe metabolism of Lapatinib can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Lapatinib can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Lapatinib can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Lapatinib can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Lapatinib can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Lapatinib.
IxazomibThe metabolism of Ixazomib can be decreased when combined with Lapatinib.
KetamineThe metabolism of Ketamine can be decreased when combined with Lapatinib.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Lapatinib.
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Lapatinib.
KetoconazoleThe serum concentration of Lapatinib can be increased when it is combined with Ketoconazole.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Lapatinib.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Lapatinib.
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Lapatinib.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Lapatinib.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Lapatinib.
LenvatinibLapatinib may increase the QTc-prolonging activities of Lenvatinib.
LeuprolideLapatinib may increase the QTc-prolonging activities of Leuprolide.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Lapatinib.
LevofloxacinLapatinib may increase the QTc-prolonging activities of Levofloxacin.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Lapatinib.
LicofeloneThe metabolism of Licofelone can be decreased when combined with Lapatinib.
LidocaineThe metabolism of Lidocaine can be decreased when combined with Lapatinib.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Lapatinib.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Lapatinib.
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Lapatinib.
LopinavirThe serum concentration of Lapatinib can be increased when it is combined with Lopinavir.
LopinavirLapatinib may increase the QTc-prolonging activities of Lopinavir.
LoratadineThe metabolism of Loratadine can be decreased when combined with Lapatinib.
LosartanThe serum concentration of Losartan can be increased when it is combined with Lapatinib.
LosartanThe metabolism of Lapatinib can be decreased when combined with Losartan.
LovastatinThe metabolism of Lapatinib can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Lapatinib can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Lapatinib can be decreased when it is combined with Lumacaftor.
LumefantrineLapatinib may increase the QTc-prolonging activities of Lumefantrine.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Lapatinib.
Mefenamic acidThe metabolism of Mefenamic acid can be decreased when combined with Lapatinib.
MeloxicamThe metabolism of Meloxicam can be decreased when combined with Lapatinib.
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Lapatinib.
MethadoneLapatinib may increase the QTc-prolonging activities of Methadone.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Lapatinib.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Lapatinib.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Lapatinib.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Lapatinib.
MifepristoneThe metabolism of Lapatinib can be decreased when combined with Mifepristone.
MifepristoneLapatinib may increase the QTc-prolonging activities of Mifepristone.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Lapatinib.
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Lapatinib.
MitotaneThe serum concentration of Lapatinib can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Lapatinib.
MoclobemideThe metabolism of Lapatinib can be decreased when combined with Moclobemide.
ModafinilThe serum concentration of Lapatinib can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Morphine can be increased when it is combined with Lapatinib.
MoxifloxacinLapatinib may increase the QTc-prolonging activities of Moxifloxacin.
muraglitazarThe metabolism of muraglitazar can be decreased when combined with Lapatinib.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Lapatinib.
NadololThe serum concentration of Nadolol can be increased when it is combined with Lapatinib.
NafcillinThe serum concentration of Lapatinib can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Lapatinib.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Lapatinib.
NaproxenThe metabolism of Naproxen can be decreased when combined with Lapatinib.
NefazodoneThe serum concentration of Lapatinib can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Lapatinib can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Lapatinib can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Lapatinib can be decreased when it is combined with Nevirapine.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Lapatinib.
NicardipineThe metabolism of Lapatinib can be decreased when combined with Nicardipine.
NicotineThe metabolism of Nicotine can be decreased when combined with Lapatinib.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Lapatinib.
NilotinibThe metabolism of Lapatinib can be decreased when combined with Nilotinib.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Lapatinib.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Lapatinib.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Lapatinib.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Lapatinib.
OfloxacinLapatinib may increase the QTc-prolonging activities of Ofloxacin.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Lapatinib.
OlaparibThe metabolism of Lapatinib can be decreased when combined with Olaparib.
OlodaterolThe metabolism of Olodaterol can be decreased when combined with Lapatinib.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Lapatinib.
OmeprazoleThe metabolism of Lapatinib can be decreased when combined with Omeprazole.
OndansetronLapatinib may increase the QTc-prolonging activities of Ondansetron.
OsimertinibThe serum concentration of Lapatinib can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Lapatinib.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Lapatinib.
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Lapatinib.
PalbociclibThe serum concentration of Lapatinib can be increased when it is combined with Palbociclib.
PaliperidoneLapatinib may increase the QTc-prolonging activities of Paliperidone.
PanobinostatLapatinib may increase the QTc-prolonging activities of Panobinostat.
PantoprazoleThe metabolism of Lapatinib can be decreased when combined with Pantoprazole.
ParamethadioneThe metabolism of Paramethadione can be decreased when combined with Lapatinib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Lapatinib.
PentamidineLapatinib may increase the QTc-prolonging activities of Pentamidine.
PentobarbitalThe serum concentration of Lapatinib can be decreased when it is combined with Pentobarbital.
PerflutrenLapatinib may increase the QTc-prolonging activities of Perflutren.
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Lapatinib.
PhenobarbitalThe serum concentration of Lapatinib can be decreased when it is combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Lapatinib.
PhenprocoumonThe metabolism of Phenprocoumon can be decreased when combined with Lapatinib.
PhenytoinThe serum concentration of Lapatinib can be decreased when it is combined with Phenytoin.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Lapatinib.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Lapatinib.
PioglitazoneThe metabolism of Lapatinib can be decreased when combined with Pioglitazone.
PiroxicamThe metabolism of Piroxicam can be decreased when combined with Lapatinib.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Lapatinib.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Lapatinib.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Lapatinib.
PosaconazoleThe serum concentration of Lapatinib can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Lapatinib.
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Lapatinib.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Lapatinib.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Lapatinib.
PrimaquineLapatinib may increase the QTc-prolonging activities of Primaquine.
PrimidoneThe serum concentration of Lapatinib can be decreased when it is combined with Primidone.
ProcainamideLapatinib may increase the QTc-prolonging activities of Procainamide.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Lapatinib.
PromazineLapatinib may increase the QTc-prolonging activities of Promazine.
PropafenoneLapatinib may increase the QTc-prolonging activities of Propafenone.
PropofolThe metabolism of Propofol can be decreased when combined with Lapatinib.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Lapatinib.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Lapatinib.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Lapatinib.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Lapatinib.
QuinineThe serum concentration of Quinine can be increased when it is combined with Lapatinib.
QuinineThe metabolism of Lapatinib can be decreased when combined with Quinine.
RabeprazoleThe metabolism of Lapatinib can be decreased when combined with Rabeprazole.
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Lapatinib.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Lapatinib.
RanolazineThe metabolism of Lapatinib can be decreased when combined with Ranolazine.
RepaglinideThe metabolism of Repaglinide can be decreased when combined with Lapatinib.
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Lapatinib.
RifabutinThe serum concentration of Lapatinib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Lapatinib can be decreased when it is combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Lapatinib.
RifapentineThe serum concentration of Lapatinib can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Lapatinib.
RiociguatThe metabolism of Riociguat can be decreased when combined with Lapatinib.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Lapatinib.
RitonavirThe serum concentration of Lapatinib can be increased when it is combined with Ritonavir.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Lapatinib.
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Lapatinib.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Lapatinib.
RosiglitazoneThe metabolism of Lapatinib can be decreased when combined with Rosiglitazone.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Lapatinib.
SaquinavirThe serum concentration of Lapatinib can be increased when it is combined with Saquinavir.
SaquinavirLapatinib may increase the QTc-prolonging activities of Saquinavir.
SecobarbitalThe metabolism of Lapatinib can be increased when combined with Secobarbital.
SelegilineThe metabolism of Selegiline can be decreased when combined with Lapatinib.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Lapatinib.
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Lapatinib.
SertralineThe metabolism of Lapatinib can be decreased when combined with Sertraline.
SildenafilThe metabolism of Lapatinib can be decreased when combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Lapatinib.
SiltuximabThe serum concentration of Lapatinib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Lapatinib can be increased when it is combined with Simeprevir.
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Lapatinib.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Lapatinib.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Lapatinib.
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Lapatinib.
SotalolLapatinib may increase the QTc-prolonging activities of Sotalol.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Lapatinib.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Lapatinib.
St. John's WortThe serum concentration of Lapatinib can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Lapatinib can be increased when it is combined with Stiripentol.
SulfadiazineThe metabolism of Sulfadiazine can be decreased when combined with Lapatinib.
SulfamethoxazoleThe metabolism of Lapatinib can be decreased when combined with Sulfamethoxazole.
SulfinpyrazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Lapatinib.
SulfisoxazoleLapatinib may increase the QTc-prolonging activities of Sulfisoxazole.
SulfisoxazoleThe metabolism of Lapatinib can be decreased when combined with Sulfisoxazole.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Lapatinib.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Lapatinib.
TamoxifenThe metabolism of Lapatinib can be decreased when combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Lapatinib.
TazaroteneThe metabolism of Tazarotene can be decreased when combined with Lapatinib.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Lapatinib.
TelaprevirThe serum concentration of Lapatinib can be increased when it is combined with Telaprevir.
TelavancinLapatinib may increase the QTc-prolonging activities of Telavancin.
TelithromycinThe serum concentration of Lapatinib can be increased when it is combined with Telithromycin.
TelithromycinLapatinib may increase the QTc-prolonging activities of Telithromycin.
TemazepamThe metabolism of Temazepam can be decreased when combined with Lapatinib.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Lapatinib.
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Lapatinib.
TeriflunomideThe metabolism of Lapatinib can be decreased when combined with Teriflunomide.
TestosteroneThe metabolism of Testosterone can be decreased when combined with Lapatinib.
TetrabenazineLapatinib may increase the QTc-prolonging activities of Tetrabenazine.
TheophyllineThe metabolism of Theophylline can be decreased when combined with Lapatinib.
ThioridazineLapatinib may increase the QTc-prolonging activities of Thioridazine.
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Lapatinib.
TiclopidineThe metabolism of Lapatinib can be decreased when combined with Ticlopidine.
TimololThe serum concentration of Timolol can be increased when it is combined with Lapatinib.
TocilizumabThe serum concentration of Lapatinib can be decreased when it is combined with Tocilizumab.
TolbutamideThe metabolism of Tolbutamide can be decreased when combined with Lapatinib.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Lapatinib.
TopiramateThe metabolism of Lapatinib can be decreased when combined with Topiramate.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Lapatinib.
TorasemideThe metabolism of Torasemide can be decreased when combined with Lapatinib.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Lapatinib.
TranylcypromineThe metabolism of Lapatinib can be decreased when combined with Tranylcypromine.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Lapatinib.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Lapatinib.
TretinoinThe metabolism of Tretinoin can be decreased when combined with Lapatinib.
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Lapatinib.
TrimethoprimThe metabolism of Lapatinib can be decreased when combined with Trimethoprim.
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Lapatinib.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Lapatinib.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Lapatinib.
VandetanibLapatinib may increase the QTc-prolonging activities of Vandetanib.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Lapatinib.
VemurafenibLapatinib may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineThe metabolism of Lapatinib can be decreased when combined with Venlafaxine.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Lapatinib.
VerapamilThe metabolism of Lapatinib can be decreased when combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Lapatinib.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Lapatinib.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Lapatinib.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Lapatinib.
VoriconazoleThe serum concentration of Lapatinib can be increased when it is combined with Voriconazole.
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Lapatinib.
WarfarinThe metabolism of Warfarin can be decreased when combined with Lapatinib.
ZafirlukastThe metabolism of Zafirlukast can be decreased when combined with Lapatinib.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Lapatinib.
ZiprasidoneThe metabolism of Lapatinib can be decreased when combined with Ziprasidone.
ZiprasidoneLapatinib may increase the QTc-prolonging activities of Ziprasidone.
ZopicloneThe metabolism of Zopiclone can be decreased when combined with Lapatinib.
ZuclopenthixolLapatinib may increase the QTc-prolonging activities of Zuclopenthixol.
Food InteractionsNot Available

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
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
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
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
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
substrate
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
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
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
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
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 ]
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Drug created on May 16, 2007 11:27 / Updated on September 29, 2016 02:25