Details of the Drug

General Information of Drug (ID: DM3BH1Y)

Drug Name

Lapatinib

Synonyms

FMM; Tycerb; Lapatinib Ditosylate; Lapatinib [INN]; Lapatinib tosilate hydrate; GSK 572016; GSK572016; GW 572016; GW 572016X; GW572016; Lapatinib (INN); Tykerb (TN); Lapatinib, Tykerb, GW572016; N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine; N-{3-CHLORO-4-[(3-FLUOROBENZYL)OXY]PHENYL}-6-[5-({[2-(METHYLSULFONYL)ETHYL]AMINO}METHYL)-2-FURYL]-4-QUINAZOLINAMINE; N-(3-Chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-((2-methylsulfonylethylamino)methyl)-2-furyl)quinazolin-4-amine; N-(3-Chloro-4-{[(3-fluorophenyl)methyl]oxy}phenyl)-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furanyl]-4-quinazolinamine; 4-[[3-Chloro-4-(3-fluorobenzyloxy)phenyl]amino]-6-[5-[[(2-methanesulfonylethyl)amino]methyl]furan-2-yl]quinazoline; Lapatinib (ERBB2 inhibitor)

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Approved	[1]
Gastroesophageal junction adenocarcinoma	2B71	Approved	[2]
Melanoma	2C30	Approved	[2]
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Therapeutic Class

Anticancer Agents

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 3

Molecular Weight (mw)

581.1

Logarithm of the Partition Coefficient (xlogp)

5.1

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Elimination: 1% of drug is excreted from urine in the unchanged form [3]
Half-life: The concentration or amount of drug in body reduced by one-half in 14.2 hours [4]
Metabolism: The drug is metabolized via the CYP3A4 and CYP3A5, with minor contributions from CYP2C19 and CYP2C8 to a variety of oxidated metabolites []
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 30.73146 micromolar/kg/day [5]
Water Solubility: The ability of drug to dissolve in water is measured as 0.001 mg/mL [3]

Adverse Drug Reaction (ADR)

ADR Term	Variation	Related DOT	DOT ID	REF
Hepatotoxicty	rs12153855	TNXB	OTVBWAV5	[6]
Hepatotoxicty	HLA-DQB1*02	HLA-DQB1	OTVVI3UI	[6]
Hepatotoxicty	HLA-DQA1*02	HLA-DQA1	OTC6GISG	[6]
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Chemical Identifiers

Formula: C29H26ClFN4O4S
IUPAC Name: N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine
Canonical SMILES: CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl
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)
InChIKey: BCFGMOOMADDAQU-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 208908
ChEBI ID: CHEBI:49603
CAS Number: 231277-92-2
DrugBank ID: DB01259
TTD ID: D08CDI
VARIDT ID: DR00120
INTEDE ID: DR0917
ACDINA ID: D00351

Combinatorial Drugs (CBD)

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Repurposed Drugs (RPD)

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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Epidermal growth factor receptor (EGFR)	TTGKNB4	EGFR_HUMAN	Inhibitor	[7]
Erbb2 tyrosine kinase receptor (HER2)	TT6EO5L	ERBB2_HUMAN	Inhibitor	[7]
Eukaryotic elongation factor 2 kinase (eEF-2K)	TT1QFLA	EF2K_HUMAN	Inhibitor	[8]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Substrate	[9]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[10]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)_{Main DME}	DE4LYSA	CP3A4_HUMAN	Substrate	[11]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Substrate	[12]
Cytochrome P450 3A5 (CYP3A5)_{Main DME}	DEIBDNY	CP3A5_HUMAN	Substrate	[12]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Substrate	[11]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Alanine aminotransferase 1 (GPT)	OTOXOA0Q	ALAT1_HUMAN	Protein Interaction/Cellular Processes	[13]
Apoptosis regulator BAX (BAX)	OTAW0V4V	BAX_HUMAN	Gene/Protein Processing	[14]
Apoptosis regulator Bcl-2 (BCL2)	OT9DVHC0	BCL2_HUMAN	Gene/Protein Processing	[14]
Baculoviral IAP repeat-containing protein 5 (BIRC5)	OTILXZYL	BIRC5_HUMAN	Gene/Protein Processing	[15]
Bile salt export pump (ABCB11)	OTRU7THO	ABCBB_HUMAN	Gene/Protein Processing	[16]
Caspase-3 (CASP3)	OTIJRBE7	CASP3_HUMAN	Gene/Protein Processing	[17]
Caspase-7 (CASP7)	OTAPJ040	CASP7_HUMAN	Gene/Protein Processing	[17]
Caspase-9 (CASP9)	OTD4RFFG	CASP9_HUMAN	Gene/Protein Processing	[17]
Cyclin-A2 (CCNA2)	OTPHHYZJ	CCNA2_HUMAN	Gene/Protein Processing	[18]
Cyclin-dependent kinase inhibitor 1B (CDKN1B)	OTNY5LLZ	CDN1B_HUMAN	Gene/Protein Processing	[19]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Molecular Expression Atlas of This Drug

The Studied Disease

Breast cancer

ICD Disease Classification

2C60-2C65

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Epidermal growth factor receptor (EGFR)	DTT	EGFR	5.84E-05	0.32	0.55
P-glycoprotein 1 (ABCB1)	DTP	P-GP	1.42E-02	-2.10E-01	-5.11E-01
Breast cancer resistance protein (ABCG2)	DTP	BCRP	1.07E-06	-3.94E-01	-6.94E-01
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	2.90E-11	-1.06E-01	-1.42E-01
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	2.45E-13	-2.29E+00	-1.44E+00
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	1.49E-08	-1.53E-01	-6.35E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	5.04E-04	-9.90E-02	-3.91E-01

Molecular Expression Atlas (MEA)

MEA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Lapatinib

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Eribulin	DM1DX4Q	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Eribulin.	Breast cancer [2C60-2C6Y]	[20]
Talazoparib	DM1KS78	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Talazoparib.	Breast cancer [2C60-2C6Y]	[21]
Ixabepilone	DM2OZ3G	Moderate	Decreased metabolism of Lapatinib caused by Ixabepilone mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[22]
LY2835219	DM93VBZ	Moderate	Decreased metabolism of Lapatinib caused by LY2835219 mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[23]
Esterified estrogens	DM9KZDO	Moderate	Decreased metabolism of Lapatinib caused by Esterified estrogens mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[24]
Tucatinib	DMBESUA	Major	Decreased metabolism of Lapatinib caused by Tucatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[25]
Quinestrol	DMJ6H1Z	Moderate	Decreased metabolism of Lapatinib caused by Quinestrol mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[24]
Cabazitaxel	DMPAZHC	Moderate	Decreased metabolism of Lapatinib caused by Cabazitaxel mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[26]
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⏷ Show the Full List of 8 DDI Information of This Drug

Coadministration of a Drug Treating the Disease Different from Lapatinib (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Remdesivir	DMBFZ6L	Moderate	Increased risk of hepatotoxicity by the combination of Lapatinib and Remdesivir.	1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019]	[25]
Ivosidenib	DM8S6T7	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Ivosidenib.	Acute myeloid leukaemia [2A60]	[27]
Arn-509	DMT81LZ	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Arn-509.	Acute myeloid leukaemia [2A60]	[25]
Gilteritinib	DMTI0ZO	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Gilteritinib.	Acute myeloid leukaemia [2A60]	[21]
Oliceridine	DM6MDCF	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Oliceridine.	Acute pain [MG31]	[20]
Ivabradine	DM0L594	Major	Increased risk of ventricular arrhythmias by the combination of Lapatinib and Ivabradine.	Angina pectoris [BA40]	[21]
Dronedarone	DMA8FS5	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Dronedarone.	Angina pectoris [BA40]	[20]
Bedaquiline	DM3906J	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Bedaquiline.	Antimicrobial drug resistance [MG50-MG52]	[28]
Posaconazole	DMUL5EW	Major	Decreased metabolism of Lapatinib caused by Posaconazole mediated inhibition of CYP450 enzyme.	Aspergillosis [1F20]	[25]
Levalbuterol	DM5YBO1	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Levalbuterol.	Asthma [CA23]	[29]
Pirbuterol	DMI5678	Moderate	Increased risk of ventricular arrhythmias by the combination of Lapatinib and Pirbuterol.	Asthma [CA23]	[30]
Troleandomycin	DMUZNIG	Major	Decreased metabolism of Lapatinib caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[25]
Ag-221	DMS0ZBI	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Ag-221.	BCR-ABL1-negative chronic myeloid leukaemia [2A41]	[25]
Retigabine	DMGNYIH	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Retigabine.	Behcet disease [4A62]	[20]
Cariprazine	DMJYDVK	Moderate	Decreased metabolism of Lapatinib caused by Cariprazine mediated inhibition of CYP450 enzyme.	Bipolar disorder [6A60]	[21]
Erdafitinib	DMI782S	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Erdafitinib.	Bladder cancer [2C94]	[31]
Pexidartinib	DMS2J0Z	Major	Increased risk of hepatotoxicity by the combination of Lapatinib and Pexidartinib.	Bone/articular cartilage neoplasm [2F7B]	[32]
Macitentan	DMP79A1	Moderate	Decreased metabolism of Lapatinib caused by Macitentan mediated inhibition of CYP450 enzyme.	Cardiovascular disease [BA00-BE2Z]	[33]
PF-04449913	DMSB068	Moderate	Decreased metabolism of Lapatinib caused by PF-04449913 mediated inhibition of CYP450 enzyme.	Chronic myelomonocytic leukaemia [2A40]	[34]
Olodaterol	DM62B78	Moderate	Increased risk of ventricular arrhythmias by the combination of Lapatinib and Olodaterol.	Chronic obstructive pulmonary disease [CA22]	[30]
Vilanterol	DMF5EK1	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Vilanterol.	Chronic obstructive pulmonary disease [CA22]	[29]
Revefenacin	DMMP5SI	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Revefenacin.	Chronic obstructive pulmonary disease [CA22]	[35]
Indacaterol	DMQJHR7	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Indacaterol.	Chronic obstructive pulmonary disease [CA22]	[30]
Arformoterol	DMYM974	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Arformoterol.	Chronic obstructive pulmonary disease [CA22]	[30]
Dihydrocodeine	DMB0FWL	Moderate	Decreased metabolism of Lapatinib caused by Dihydrocodeine mediated inhibition of CYP450 enzyme.	Chronic pain [MG30]	[36]
Fidaxomicin	DMFP6MV	Minor	Decreased clearance of Lapatinib due to the transporter inhibition by Fidaxomicin.	Clostridium difficile enterocolitis [1A04]	[25]
Intedanib	DMSTA36	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Intedanib.	Colorectal cancer [2B91]	[37]
Drospirenone	DM1A9W3	Moderate	Decreased metabolism of Lapatinib caused by Drospirenone mediated inhibition of CYP450 enzyme.	Contraceptive management [QA21]	[24]
Levonorgestrel	DM1DP7T	Moderate	Decreased metabolism of Lapatinib caused by Levonorgestrel mediated inhibition of CYP450 enzyme.	Contraceptive management [QA21]	[24]
Probucol	DMVZQ2M	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Probucol.	Coronary atherosclerosis [BA80]	[20]
Pasireotide	DMHM7JS	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Pasireotide.	Cushing syndrome [5A70]	[20]
Osilodrostat	DMIJC9X	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Osilodrostat.	Cushing syndrome [5A70]	[21]
Ivacaftor	DMZC1HS	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Ivacaftor.	Cystic fibrosis [CA25]	[38]
MK-8228	DMOB58Q	Moderate	Decreased metabolism of Lapatinib caused by MK-8228 mediated inhibition of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[24]
Rivaroxaban	DMQMBZ1	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Rivaroxaban.	Deep vein thrombosis [BD71]	[39]
Polatuzumab vedotin	DMF6Y0L	Moderate	Decreased metabolism of Lapatinib caused by Polatuzumab vedotin mediated inhibition of CYP450 enzyme.	Diffuse large B-cell lymphoma [2A81]	[40]
[3H]estrone-3-sulphate	DMGPF0N	Moderate	Decreased metabolism of Lapatinib caused by [3H]estrone-3-sulphate mediated inhibition of CYP450 enzyme.	Discovery agent [N.A.]	[36]
Tetrabenazine	DMYWQ0O	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Tetrabenazine.	Dissociative neurological symptom disorder [6B60]	[20]
Deutetrabenazine	DMUPFLI	Moderate	Additive CNS depression effects by the combination of Lapatinib and Deutetrabenazine.	Dystonic disorder [8A02]	[41]
Ingrezza	DMVPLNC	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Ingrezza.	Dystonic disorder [8A02]	[42]
Cenobamate	DM8KLU9	Moderate	Increased metabolism of Lapatinib caused by Cenobamate mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[25]
Stiripentol	DMMSDOY	Moderate	Decreased metabolism of Lapatinib caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[21]
Fosphenytoin	DMOX3LB	Moderate	Increased metabolism of Lapatinib caused by Fosphenytoin mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[25]
Cannabidiol	DM0659E	Moderate	Increased risk of hepatotoxicity by the combination of Lapatinib and Cannabidiol.	Epileptic encephalopathy [8A62]	[21]
Bay 80-6946	DMLOS5R	Moderate	Decreased metabolism of Lapatinib caused by Bay 80-6946 mediated inhibition of CYP450 enzyme.	Follicular lymphoma [2A80]	[43]
Tazemetostat	DMWP1BH	Moderate	Increased metabolism of Lapatinib caused by Tazemetostat mediated induction of CYP450 enzyme.	Follicular lymphoma [2A80]	[25]
Solifenacin	DMG592Q	Moderate	Decreased metabolism of Lapatinib caused by Solifenacin mediated inhibition of CYP450 enzyme.	Functional bladder disorder [GC50]	[44]
Mirabegron	DMS1GYT	Minor	Decreased metabolism of Lapatinib caused by Mirabegron mediated inhibition of CYP450 enzyme.	Functional bladder disorder [GC50]	[45]
Dexlansoprazole	DM1DBV5	Moderate	Decreased absorption of Lapatinib due to altered gastric pH caused by Dexlansoprazole.	Gastro-oesophageal reflux disease [DA22]	[21]
Ripretinib	DM958QB	Moderate	Decreased metabolism of Lapatinib caused by Ripretinib mediated inhibition of CYP450 enzyme.	Gastrointestinal stromal tumour [2B5B]	[25]
Sunitinib	DMCBJSR	Moderate	Decreased metabolism of Lapatinib caused by Sunitinib mediated inhibition of CYP450 enzyme.	Gastrointestinal stromal tumour [2B5B]	[24]
Avapritinib	DMK2GZX	Moderate	Decreased metabolism of Lapatinib caused by Avapritinib mediated inhibition of CYP450 enzyme.	Gastrointestinal stromal tumour [2B5B]	[21]
Digitoxin	DMWVIGP	Moderate	Decreased metabolism of Lapatinib caused by Digitoxin mediated inhibition of CYP450 enzyme.	Heart failure [BD10-BD1Z]	[24]
Boceprevir	DMBSHMF	Major	Decreased metabolism of Lapatinib caused by Boceprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[24]
Telaprevir	DMMRV29	Major	Decreased metabolism of Lapatinib caused by Telaprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[25]
GS-5885	DMSL3DX	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by GS-5885.	Hepatitis virus infection [1E50-1E51]	[46]
GS-9857	DMYU6P5	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by GS-9857.	Hepatitis virus infection [1E50-1E51]	[47]
Brentuximab vedotin	DMWLC57	Moderate	Increased risk of hepatotoxicity by the combination of Lapatinib and Brentuximab vedotin.	Hodgkin lymphoma [2B30]	[48]
MK-1439	DM215WE	Minor	Decreased metabolism of Lapatinib caused by MK-1439 mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[49]
Fosamprenavir	DM4W9B3	Major	Decreased metabolism of Lapatinib caused by Fosamprenavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[25]
Fostemsavir	DM50ILT	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Fostemsavir.	Human immunodeficiency virus disease [1C60-1C62]	[50]
Cobicistat	DM6L4H2	Major	Decreased metabolism of Lapatinib caused by Cobicistat mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[25]
Etravirine	DMGV8QU	Moderate	Increased metabolism of Lapatinib caused by Etravirine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[25]
Rilpivirine	DMJ0QOW	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Rilpivirine.	Human immunodeficiency virus disease [1C60-1C62]	[20]
Darunavir	DMN3GCH	Moderate	Decreased metabolism of Lapatinib caused by Darunavir mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[24]
Mipomersen	DMGSRN1	Major	Increased risk of hepatotoxicity by the combination of Lapatinib and Mipomersen.	Hyper-lipoproteinaemia [5C80]	[51]
Teriflunomide	DMQ2FKJ	Major	Increased risk of hepatotoxicity by the combination of Lapatinib and Teriflunomide.	Hyper-lipoproteinaemia [5C80]	[20]
BMS-201038	DMQTAGO	Major	Increased risk of hepatotoxicity by the combination of Lapatinib and BMS-201038.	Hyper-lipoproteinaemia [5C80]	[52]
Aliskiren	DM1BV7W	Moderate	Decreased metabolism of Lapatinib caused by Aliskiren mediated inhibition of CYP450 enzyme.	Hypertension [BA00-BA04]	[20]
Levamlodipine	DM92S6N	Moderate	Decreased metabolism of Lapatinib caused by Levamlodipine mediated inhibition of CYP450 enzyme.	Hypertension [BA00-BA04]	[24]
Tolvaptan	DMIWFRL	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Tolvaptan.	Hypo-osmolality/hyponatraemia [5C72]	[53]
Berotralstat	DMWA2DZ	Major	Decreased clearance of Lapatinib due to the transporter inhibition by Berotralstat.	Innate/adaptive immunodeficiency [4A00]	[54]
Suvorexant	DM0E6S3	Moderate	Decreased metabolism of Lapatinib caused by Suvorexant mediated inhibition of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[25]
Amobarbital	DM0GQ8N	Moderate	Increased metabolism of Lapatinib caused by Amobarbital mediated induction of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[25]
ITI-007	DMUQ1DO	Moderate	Decreased metabolism of Lapatinib caused by ITI-007 mediated inhibition of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[55]
Quazepam	DMY4D87	Moderate	Decreased metabolism of Lapatinib caused by Quazepam mediated inhibition of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[24]
Polyethylene glycol	DM4I1JP	Moderate	Increased risk of ventricular arrhythmias by the combination of Lapatinib and Polyethylene glycol.	Irritable bowel syndrome [DD91]	[21]
Phenolphthalein	DM5SICT	Moderate	Increased risk of ventricular arrhythmias by the combination of Lapatinib and Phenolphthalein.	Irritable bowel syndrome [DD91]	[20]
Eluxadoline	DMYZ0P1	Major	Decreased clearance of Lapatinib due to the transporter inhibition by Eluxadoline.	Irritable bowel syndrome [DD91]	[21]
Naloxegol	DML0B41	Minor	Decreased metabolism of Lapatinib caused by Naloxegol mediated inhibition of CYP450 enzyme.	Large intestine motility disorder [DB32]	[56]
Pemigatinib	DM819JF	Moderate	Decreased metabolism of Lapatinib caused by Pemigatinib mediated inhibition of CYP450 enzyme.	Liver cancer [2C12]	[21]
Crizotinib	DM4F29C	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Crizotinib.	Lung cancer [2C25]	[57]
Brigatinib	DM7W94S	Moderate	Decreased metabolism of Lapatinib caused by Brigatinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[25]
Ceritinib	DMB920Z	Major	Decreased metabolism of Lapatinib caused by Ceritinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[25]
Lurbinectedin	DMEFRTZ	Moderate	Decreased metabolism of Lapatinib caused by Lurbinectedin mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[58]
Osimertinib	DMRJLAT	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Osimertinib.	Lung cancer [2C25]	[59]
Pralsetinib	DMWU0I2	Moderate	Decreased metabolism of Lapatinib caused by Pralsetinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[60]
Capmatinib	DMYCXKL	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Capmatinib.	Lung cancer [2C25]	[61]
Selpercatinib	DMZR15V	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Selpercatinib.	Lung cancer [2C25]	[21]
Artesunate	DMR27C8	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Artesunate.	Malaria [1F40-1F45]	[24]
Hydroxychloroquine	DMSIVND	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Hydroxychloroquine.	Malaria [1F40-1F45]	[62]
Inotuzumab ozogamicin	DMAC130	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Inotuzumab ozogamicin.	Malignant haematopoietic neoplasm [2B33]	[21]
Calaspargase pegol	DMQZBXI	Moderate	Increased risk of hepatotoxicity by the combination of Lapatinib and Calaspargase pegol.	Malignant haematopoietic neoplasm [2B33]	[63]
Idelalisib	DM602WT	Major	Decreased metabolism of Lapatinib caused by Idelalisib mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[25]
GDC-0199	DMH0QKA	Major	Decreased clearance of Lapatinib due to the transporter inhibition by GDC-0199.	Mature B-cell leukaemia [2A82]	[25]
IPI-145	DMWA24P	Moderate	Decreased metabolism of Lapatinib caused by IPI-145 mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[24]
Acalabrutinib	DM7GCVW	Moderate	Decreased metabolism of Lapatinib caused by Acalabrutinib mediated inhibition of CYP450 enzyme.	Mature B-cell lymphoma [2A85]	[64]
Ibrutinib	DMHZCPO	Moderate	Decreased metabolism of Lapatinib caused by Ibrutinib mediated inhibition of CYP450 enzyme.	Mature B-cell lymphoma [2A85]	[65]
Arry-162	DM1P6FR	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Arry-162.	Melanoma [2C30]	[25]
Vemurafenib	DM62UG5	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Vemurafenib.	Melanoma [2C30]	[20]
Selumetinib	DMC7W6R	Moderate	Decreased metabolism of Lapatinib caused by Selumetinib mediated inhibition of CYP450 enzyme.	Melanoma [2C30]	[66]
LGX818	DMNQXV8	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and LGX818.	Melanoma [2C30]	[67]
Dabrafenib	DMX6OE3	Moderate	Increased metabolism of Lapatinib caused by Dabrafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[25]
Danazol	DML8KTN	Moderate	Decreased metabolism of Lapatinib caused by Danazol mediated inhibition of CYP450 enzyme.	Menstrual cycle bleeding disorder [GA20]	[24]
Ubrogepant	DM749I3	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Ubrogepant.	Migraine [8A80]	[68]
Rimegepant	DMHOAUG	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Rimegepant.	Migraine [8A80]	[69]
Lasmiditan	DMXLVDT	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Lasmiditan.	Migraine [8A80]	[70]
Exjade	DMHPRWG	Moderate	Decreased metabolism of Lapatinib caused by Exjade mediated inhibition of CYP450 enzyme.	Mineral absorption/transport disorder [5C64]	[71]
Flibanserin	DM70DTN	Moderate	Decreased metabolism of Lapatinib caused by Flibanserin mediated inhibition of CYP450 enzyme.	Mood disorder [6A60-6E23]	[72]
Panobinostat	DM58WKG	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Panobinostat.	Multiple myeloma [2A83]	[73]
Siponimod	DM2R86O	Major	Increased risk of ventricular arrhythmias by the combination of Lapatinib and Siponimod.	Multiple sclerosis [8A40]	[25]
Fingolimod	DM5JVAN	Major	Increased risk of ventricular arrhythmias by the combination of Lapatinib and Fingolimod.	Multiple sclerosis [8A40]	[20]
Ozanimod	DMT6AM2	Major	Increased risk of ventricular arrhythmias by the combination of Lapatinib and Ozanimod.	Multiple sclerosis [8A40]	[74]
Romidepsin	DMT5GNL	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Romidepsin.	Mycosis fungoides [2B01]	[20]
Nilotinib	DM7HXWT	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Nilotinib.	Myeloproliferative neoplasm [2A20]	[20]
Ruxolitinib	DM7Q98D	Minor	Decreased metabolism of Lapatinib caused by Ruxolitinib mediated inhibition of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[21]
Rolapitant	DM8XP26	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Rolapitant.	Nausea/vomiting [MD90]	[75]
Entrectinib	DMMPTLH	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Entrectinib.	Non-small cell lung cancer [2C25]	[25]
S-297995	DM26IH8	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by S-297995.	Opioid use disorder [6C43]	[21]
Olaparib	DM8QB1D	Moderate	Decreased metabolism of Lapatinib caused by Olaparib mediated inhibition of CYP450 enzyme.	Ovarian cancer [2C73]	[76]
Rucaparib	DM9PVX8	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Rucaparib.	Ovarian cancer [2C73]	[20]
Triclabendazole	DMPWGBR	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Triclabendazole.	Parasitic worm infestation [1F90]	[20]
Pimavanserin	DMR7IVC	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Pimavanserin.	Parkinsonism [8A00]	[77]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Lapatinib caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[78]
Macimorelin	DMQYJIR	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Macimorelin.	Pituitary gland disorder [5A60-5A61]	[79]
Lefamulin	DME6G97	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Lefamulin.	Pneumonia [CA40]	[80]
Lonafarnib	DMGM2Z6	Major	Decreased metabolism of Lapatinib caused by Lonafarnib mediated inhibition of CYP450 enzyme.	Premature ageing appearance [LD2B]	[25]
Degarelix	DM3O8QY	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Degarelix.	Prostate cancer [2C82]	[21]
ABIRATERONE	DM8V75C	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and ABIRATERONE.	Prostate cancer [2C82]	[21]
Enzalutamide	DMGL19D	Moderate	Decreased metabolism of Lapatinib caused by Enzalutamide mediated inhibition of CYP450 enzyme.	Prostate cancer [2C82]	[25]
Relugolix	DMK7IWL	Major	Decreased clearance of Lapatinib due to the transporter inhibition by Relugolix.	Prostate cancer [2C82]	[81]
Darolutamide	DMV7YFT	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Darolutamide.	Prostate cancer [2C82]	[82]
Silodosin	DMJSBT6	Moderate	Decreased metabolism of Lapatinib caused by Silodosin mediated inhibition of CYP450 enzyme.	Prostate hyperplasia [GA90]	[83]
Levomepromazine	DMIKFEL	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Levomepromazine.	Psychotic disorder [6A20-6A25]	[20]
Selexipag	DMAHSU0	Moderate	Decreased metabolism of Lapatinib caused by Selexipag mediated inhibition of CYP450 enzyme.	Pulmonary hypertension [BB01]	[84]
Riociguat	DMXBLMP	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Riociguat.	Pulmonary hypertension [BB01]	[25]
Everolimus	DM8X2EH	Moderate	Decreased metabolism of Lapatinib caused by Everolimus mediated inhibition of CYP450 enzyme.	Renal cell carcinoma [2C90]	[85]
Axitinib	DMGVH6N	Moderate	Decreased metabolism of Lapatinib caused by Axitinib mediated inhibition of CYP450 enzyme.	Renal cell carcinoma [2C90]	[21]
Temsirolimus	DMS104F	Moderate	Decreased metabolism of Lapatinib caused by Temsirolimus mediated inhibition of CYP450 enzyme.	Renal cell carcinoma [2C90]	[86]
Iloperidone	DM6AUFY	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Iloperidone.	Schizophrenia [6A20]	[20]
Paliperidone	DM7NPJS	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Paliperidone.	Schizophrenia [6A20]	[20]
Amisulpride	DMSJVAM	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Amisulpride.	Schizophrenia [6A20]	[87]
Asenapine	DMSQZE2	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Asenapine.	Schizophrenia [6A20]	[20]
Voxelotor	DMCS6M5	Moderate	Decreased metabolism of Lapatinib caused by Voxelotor mediated inhibition of CYP450 enzyme.	Sickle-cell disorder [3A51]	[24]
Tedizolid	DMG2SKR	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Tedizolid.	Skin and skin-structure infection [1F28-1G0Z]	[21]
LDE225	DMM9F25	Moderate	Decreased metabolism of Lapatinib caused by LDE225 mediated inhibition of CYP450 enzyme.	Skin cancer [2C30-2C37]	[88]
Telotristat ethyl	DMDIYFZ	Moderate	Increased metabolism of Lapatinib caused by Telotristat ethyl mediated induction of CYP450 enzyme.	Small intestine developmental anomaly [DA90]	[21]
Larotrectinib	DM26CQR	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Larotrectinib.	Solid tumour/cancer [2A00-2F9Z]	[25]
Trabectedin	DMG3Y89	Moderate	Decreased metabolism of Lapatinib caused by Trabectedin mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[21]
Armodafinil	DMGB035	Moderate	Decreased metabolism of Lapatinib caused by Armodafinil mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[24]
LEE011	DMMX75K	Major	Decreased metabolism of Lapatinib caused by LEE011 mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[20]
Vandetanib	DMRICNP	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Vandetanib.	Solid tumour/cancer [2A00-2F9Z]	[20]
Triptorelin	DMTK4LS	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Triptorelin.	Solid tumour/cancer [2A00-2F9Z]	[21]
Pitolisant	DM8RFNJ	Moderate	Increased metabolism of Lapatinib caused by Pitolisant mediated induction of CYP450 enzyme.	Somnolence [MG42]	[21]
Telavancin	DM58VQX	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Telavancin.	Staphylococcal/streptococcal disease [1B5Y]	[20]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Lapatinib caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[89]
Lusutrombopag	DMH6IKO	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Lusutrombopag.	Thrombocytopenia [3B64]	[90]
Eltrombopag	DMOGFIX	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Eltrombopag.	Thrombocytopenia [3B64]	[91]
Apixaban	DM89JLN	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Apixaban.	Thrombosis [DB61-GB90]	[21]
Lenvatinib	DMB1IU4	Moderate	Increased risk of prolong QT interval by the combination of Lapatinib and Lenvatinib.	Thyroid cancer [2D10]	[20]
Cabozantinib	DMIYDT4	Major	Increased risk of prolong QT interval by the combination of Lapatinib and Cabozantinib.	Thyroid cancer [2D10]	[21]
Saxagliptin	DMGXENV	Moderate	Decreased metabolism of Lapatinib caused by Saxagliptin mediated inhibition of CYP450 enzyme.	Type 2 diabetes mellitus [5A11]	[21]
Elagolix	DMB2C0E	Moderate	Increased metabolism of Lapatinib caused by Elagolix mediated induction of CYP450 enzyme.	Uterine fibroid [2E86]	[25]
Fluticasone	DMGCSVF	Moderate	Decreased clearance of Lapatinib due to the transporter inhibition by Fluticasone.	Vasomotor/allergic rhinitis [CA08]	[24]
-----------


⏷ Show the Full List of 164 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Sunset yellow FCF	E00255	17730	Colorant
Hypromellose	E00634	Not Available	Coating agent
Magnesium stearate	E00208	11177	lubricant
Polyethylene glycol 400	E00653	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polysorbate 80	E00665	Not Available	Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
Povidone	E00667	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Certolake sunset yellow	E00351	61817	Colorant
Cellulose microcrystalline	E00698	Not Available	Adsorbent; Suspending agent; Diluent
--------------------


⏷ Show the Full List of 9 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Lapatinib 250 mg tablet	250 mg	Oral Tablet	Oral
Lapatinib Ditosylate eq 250mg base tablet	eq 250mg base	Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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