Canertinib

Identification

Name
Canertinib
Accession Number
DB05424
Type
Small Molecule
Groups
Investigational
Description

Canertinib is a pan-erbB tyrosine kinase inhibitor which work against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantly affects tumour metabolism, proliferation and hypoxia as determined by PET.

Structure
Thumb
Synonyms
Not Available
External IDs
PD-183805
Product Ingredients
IngredientUNIICASInChI Key
Canertinib dihydrochlorideICJ93X8X90289499-45-2JZZFDCXSFTVOJY-UHFFFAOYSA-N
Categories
UNII
C78W1K5ASF
CAS number
267243-28-7
Weight
Average: 485.938
Monoisotopic: 485.162995603
Chemical Formula
C24H25ClFN5O3
InChI Key
OMZCMEYTWSXEPZ-UHFFFAOYSA-N
InChI
InChI=1S/C24H25ClFN5O3/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29)
IUPAC Name
N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(morpholin-4-yl)propoxy]quinazolin-6-yl}prop-2-enamide
SMILES
FC1=C(Cl)C=C(NC2=NC=NC3=CC(OCCCN4CCOCC4)=C(NC(=O)C=C)C=C23)C=C1

Pharmacology

Indication

Investigated for use/treatment in breast cancer and lung cancer.

Pharmacodynamics
Not Available
Mechanism of action

CI-1033 effectively inhibits the growth of esophageal squamous cell carcinoma which co-expresses both EGFR and HER2 with the inhibition of phosphorylation of both MAPK and AKT. Some studies suggest that CI-1033 holds significant clinical potential in esophageal cancer.

TargetActionsOrganism
UEpidermal growth factor receptorNot AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
7-NitroindazoleThe risk or severity of adverse effects can be increased when 7-Nitroindazole is combined with Canertinib.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Canertinib.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Canertinib.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Canertinib.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Canertinib.Experimental
AdipiplonThe risk or severity of adverse effects can be increased when Canertinib is combined with Adipiplon.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Canertinib is combined with Agomelatine.Approved, Investigational
AlaproclateThe risk or severity of adverse effects can be increased when Canertinib is combined with Alaproclate.Experimental
AlfaxaloneThe risk or severity of adverse effects can be increased when Canertinib is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Canertinib.Approved, Illicit
AllopregnanoloneThe risk or severity of adverse effects can be increased when Canertinib is combined with Allopregnanolone.Investigational
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Canertinib.Experimental, Illicit
AlphaprodineThe risk or severity of adverse effects can be increased when Canertinib is combined with Alphaprodine.Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Canertinib.Approved, Illicit, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Canertinib is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Canertinib.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Canertinib.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Canertinib.Approved
AmperozideThe risk or severity of adverse effects can be increased when Canertinib is combined with Amperozide.Experimental
AncestimThe risk or severity of cytotoxicity can be increased when Ancestim is combined with Canertinib.Approved, Investigational, Withdrawn
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Canertinib.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Canertinib is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Canertinib.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Canertinib is combined with Azaperone.Investigational, Vet Approved
AzelastineCanertinib may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Canertinib.Approved
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Canertinib.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Canertinib is combined with Benperidol.Approved, Investigational
BevacizumabBevacizumab may increase the cardiotoxic activities of Canertinib.Approved, Investigational
BrexpiprazoleThe risk or severity of adverse effects can be increased when Brexpiprazole is combined with Canertinib.Approved, Investigational
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Canertinib.Approved
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Canertinib.Approved, Illicit, Investigational
BromisovalThe risk or severity of adverse effects can be increased when Canertinib is combined with Bromisoval.Experimental
BromperidolThe risk or severity of adverse effects can be increased when Canertinib is combined with Bromperidol.Approved, Investigational
BrotizolamThe risk or severity of adverse effects can be increased when Canertinib is combined with Brotizolam.Approved, Investigational, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Canertinib.Approved, Investigational
BuprenorphineCanertinib may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Canertinib.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Canertinib.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Canertinib is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Butalbital is combined with Canertinib.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Canertinib is combined with Butamben.Approved, Withdrawn
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Canertinib.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Canertinib.Approved, Illicit, Vet Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Canertinib.Approved
CarbinoxamineThe risk or severity of adverse effects can be increased when Carbinoxamine is combined with Canertinib.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Canertinib.Illicit, Investigational, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Carisoprodol is combined with Canertinib.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Canertinib.Approved, Illicit, Investigational, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Canertinib.Approved, Illicit, Investigational
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Canertinib.Approved, Investigational, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Canertinib.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Canertinib.Approved, Investigational, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Canertinib.Approved, Investigational, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Chlorzoxazone is combined with Canertinib.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Canertinib.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Canertinib is combined with Citalopram.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Clidinium is combined with Canertinib.Approved
ClobazamThe risk or severity of adverse effects can be increased when Clobazam is combined with Canertinib.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when Canertinib is combined with clomethiazole.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Canertinib.Approved, Investigational, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Clonazepam is combined with Canertinib.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Clonidine is combined with Canertinib.Approved
ClopenthixolThe risk or severity of adverse effects can be increased when Canertinib is combined with Clopenthixol.Experimental
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Canertinib.Approved, Illicit
ClothiapineThe risk or severity of adverse effects can be increased when Canertinib is combined with Clothiapine.Experimental
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Canertinib.Approved
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Canertinib.Approved, Illicit
CyclizineThe risk or severity of adverse effects can be increased when Cyclizine is combined with Canertinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Canertinib.Approved, Investigational
CyclopropaneThe risk or severity of adverse effects can be increased when Canertinib is combined with Cyclopropane.Experimental
CymarinCymarin may decrease the cardiotoxic activities of Canertinib.Experimental
CyproheptadineThe risk or severity of adverse effects can be increased when Cyproheptadine is combined with Canertinib.Approved
DantroleneThe risk or severity of adverse effects can be increased when Dantrolene is combined with Canertinib.Approved, Investigational
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Canertinib.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Canertinib is combined with Dapoxetine.Investigational
DeramciclaneThe risk or severity of adverse effects can be increased when Canertinib is combined with Deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Canertinib.Approved
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Canertinib.Approved, Investigational
DeslanosideDeslanoside may decrease the cardiotoxic activities of Canertinib.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Desloratadine is combined with Canertinib.Approved, Investigational
DetomidineThe risk or severity of adverse effects can be increased when Canertinib is combined with Detomidine.Vet Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Canertinib.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Canertinib.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Canertinib.Approved, Illicit, Investigational, Withdrawn
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Canertinib.Approved, Illicit, Investigational, Vet Approved
Diethyl etherThe risk or severity of adverse effects can be increased when Canertinib is combined with Diethyl ether.Experimental
DifenoxinThe risk or severity of adverse effects can be increased when Difenoxin is combined with Canertinib.Approved, Illicit
DigitoxinDigitoxin may decrease the cardiotoxic activities of Canertinib.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Canertinib.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Canertinib.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Canertinib.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Canertinib.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Canertinib.Experimental, Illicit
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Canertinib.Approved, Illicit
DixyrazineThe risk or severity of adverse effects can be increased when Canertinib is combined with Dixyrazine.Experimental
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Canertinib.Approved, Investigational
DoramectinThe risk or severity of adverse effects can be increased when Canertinib is combined with Doramectin.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Canertinib.Approved, Investigational
DPDPEThe risk or severity of adverse effects can be increased when Canertinib is combined with DPDPE.Experimental
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Canertinib.Approved, Illicit
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Canertinib.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Canertinib.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Canertinib is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Canertinib.Approved
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Canertinib.Experimental, Illicit
EcopipamThe risk or severity of adverse effects can be increased when Canertinib is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Efavirenz is combined with Canertinib.Approved, Investigational
EltanoloneThe risk or severity of adverse effects can be increased when Canertinib is combined with Eltanolone.Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Canertinib.Approved, Investigational, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Entacapone is combined with Canertinib.Approved, Investigational
EscitalopramThe risk or severity of adverse effects can be increased when Canertinib is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Canertinib.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Canertinib.Approved, Investigational
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Canertinib.Approved, Illicit, Withdrawn
EthotoinThe risk or severity of adverse effects can be increased when Ethotoin is combined with Canertinib.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Canertinib.Withdrawn
Ethyl chlorideThe risk or severity of adverse effects can be increased when Canertinib is combined with Ethyl chloride.Approved, Experimental, Investigational
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Canertinib.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Canertinib.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Canertinib is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Canertinib is combined with Etifoxine.Investigational, Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Canertinib is combined with Etizolam.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Canertinib is combined with Etoperidone.Withdrawn
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Canertinib.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Ezogabine is combined with Canertinib.Approved, Investigational
FelbamateThe risk or severity of adverse effects can be increased when Felbamate is combined with Canertinib.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Canertinib.Approved, Illicit, Withdrawn
FexofenadineThe risk or severity of adverse effects can be increased when Fexofenadine is combined with Canertinib.Approved, Investigational
FlibanserinThe risk or severity of adverse effects can be increased when Flibanserin is combined with Canertinib.Approved, Investigational
FluanisoneThe risk or severity of adverse effects can be increased when Canertinib is combined with Fluanisone.Experimental
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Canertinib.Approved, Illicit
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Canertinib.Approved, Illicit
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Canertinib.Approved, Investigational, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Canertinib.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Canertinib.Approved, Illicit, Investigational
FosphenytoinThe risk or severity of adverse effects can be increased when Fosphenytoin is combined with Canertinib.Approved, Investigational
FospropofolThe risk or severity of adverse effects can be increased when Canertinib is combined with Fospropofol.Approved, Illicit, Investigational
Gabapentin EnacarbilThe risk or severity of adverse effects can be increased when Gabapentin Enacarbil is combined with Canertinib.Approved, Investigational
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Canertinib.Approved, Illicit, Investigational
GepironeThe risk or severity of adverse effects can be increased when Canertinib is combined with Gepirone.Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Canertinib.Experimental
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Canertinib.Approved, Illicit
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Canertinib.Approved, Illicit, Withdrawn
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Canertinib.Approved
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Canertinib.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Canertinib.Approved, Illicit, Investigational
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Canertinib.Approved
HyaluronidaseThe risk or severity of adverse effects can be increased when Hyaluronidase is combined with Canertinib.Approved, Investigational
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Canertinib.Approved, Illicit
IloperidoneThe risk or severity of adverse effects can be increased when Iloperidone is combined with Canertinib.Approved
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Canertinib.Approved
IndalpineThe risk or severity of adverse effects can be increased when Canertinib is combined with Indalpine.Investigational, Withdrawn
IndiplonThe risk or severity of adverse effects can be increased when Canertinib is combined with Indiplon.Investigational
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Canertinib.Approved, Vet Approved
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Canertinib.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Canertinib.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Canertinib is combined with Ketobemidone.Approved, Investigational
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Canertinib.Experimental
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Canertinib.Approved, Investigational
LevocabastineThe risk or severity of adverse effects can be increased when Canertinib is combined with Levocabastine.Approved, Investigational
LevocetirizineThe risk or severity of adverse effects can be increased when Levocetirizine is combined with Canertinib.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Canertinib.Approved, Investigational
LevomilnacipranThe risk or severity of adverse effects can be increased when Canertinib is combined with Levomilnacipran.Approved, Investigational
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Canertinib.Approved
Lithium cationThe risk or severity of adverse effects can be increased when Lithium is combined with Canertinib.Experimental
LofentanilThe risk or severity of adverse effects can be increased when Canertinib is combined with Lofentanil.Illicit
LofexidineThe therapeutic efficacy of Canertinib can be increased when used in combination with Lofexidine.Approved, Investigational
LoprazolamThe risk or severity of adverse effects can be increased when Canertinib is combined with Loprazolam.Experimental
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Canertinib.Approved
LormetazepamThe risk or severity of adverse effects can be increased when Canertinib is combined with Lormetazepam.Approved
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Canertinib.Approved
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Canertinib.Approved, Investigational
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Canertinib.Approved, Investigational
MebicarThe risk or severity of adverse effects can be increased when Canertinib is combined with Mebicar.Experimental
MedazepamThe risk or severity of adverse effects can be increased when Canertinib is combined with Medazepam.Experimental
MedetomidineThe risk or severity of adverse effects can be increased when Canertinib is combined with Medetomidine.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Canertinib.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Canertinib is combined with Melperone.Approved, Investigational
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Canertinib.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Canertinib.Approved, Illicit
MeptazinolThe risk or severity of adverse effects can be increased when Canertinib is combined with Meptazinol.Experimental
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Canertinib.Approved, Investigational
MetaxaloneThe risk or severity of adverse effects can be increased when Metaxalone is combined with Canertinib.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Canertinib.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Canertinib.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Canertinib.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Canertinib.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Methocarbamol is combined with Canertinib.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Canertinib.Approved
MethotrimeprazineCanertinib may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved, Investigational
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Canertinib.Approved, Investigational, Vet Approved
MethylecgonineThe risk or severity of adverse effects can be increased when Methylecgonine is combined with Canertinib.Experimental
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Canertinib.Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Canertinib.Experimental
MetyrosineCanertinib may increase the sedative activities of Metyrosine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Canertinib.Approved, Illicit
MilnacipranThe risk or severity of adverse effects can be increased when Canertinib is combined with Milnacipran.Approved, Investigational
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Canertinib.Approved, Investigational
MirtazapineCanertinib may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Canertinib.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Canertinib.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Canertinib.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Canertinib.Approved
NefazodoneThe risk or severity of adverse effects can be increased when Canertinib is combined with Nefazodone.Approved, Withdrawn
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Canertinib.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Canertinib.Approved, Vet Approved
NordazepamThe risk or severity of adverse effects can be increased when Canertinib is combined with Nordazepam.Approved
NorfluraneThe risk or severity of adverse effects can be increased when Canertinib is combined with Norflurane.Approved, Investigational
NormethadoneThe risk or severity of adverse effects can be increased when Canertinib is combined with Normethadone.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Canertinib.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Canertinib.Approved, Investigational
OleandrinOleandrin may decrease the cardiotoxic activities of Canertinib.Experimental, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Olopatadine is combined with Canertinib.Approved
OpiumThe risk or severity of adverse effects can be increased when Canertinib is combined with Opium.Approved, Illicit
OrphenadrineCanertinib may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Canertinib.Investigational
OuabainOuabain may decrease the cardiotoxic activities of Canertinib.Approved
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Canertinib.Approved
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Canertinib.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Canertinib.Approved, Investigational
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Canertinib.Approved, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Canertinib.Approved
ParaldehydeCanertinib may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Canertinib.Approved, Vet Approved
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Canertinib.Approved, Investigational, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Canertinib.Approved
PerazineThe risk or severity of adverse effects can be increased when Canertinib is combined with Perazine.Approved, Investigational
PerospironeThe risk or severity of adverse effects can be increased when Canertinib is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Canertinib.Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Canertinib.Experimental
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Canertinib.Approved
PhenazocineThe risk or severity of adverse effects can be increased when Canertinib is combined with Phenazocine.Experimental
PhenibutThe risk or severity of adverse effects can be increased when Canertinib is combined with Phenibut.Experimental
PhenoperidineThe risk or severity of adverse effects can be increased when Canertinib is combined with Phenoperidine.Experimental
PhenoxyethanolThe risk or severity of adverse effects can be increased when Canertinib is combined with Phenoxyethanol.Approved
PhenytoinThe risk or severity of adverse effects can be increased when Phenytoin is combined with Canertinib.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Canertinib.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Canertinib is combined with Pipamperone.Approved, Investigational
PipotiazineThe risk or severity of adverse effects can be increased when Pipotiazine is combined with Canertinib.Approved, Investigational
PiritramideThe risk or severity of adverse effects can be increased when Canertinib is combined with Piritramide.Approved, Investigational
PizotifenThe risk or severity of adverse effects can be increased when Pizotifen is combined with Canertinib.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Pomalidomide is combined with Canertinib.Approved
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Canertinib.Approved, Illicit
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Canertinib.Approved
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Canertinib.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Canertinib.Approved, Investigational, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Canertinib.Approved, Vet Approved
PropanididThe risk or severity of adverse effects can be increased when Canertinib is combined with Propanidid.Experimental
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Canertinib.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Canertinib.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Canertinib is combined with Propoxycaine.Approved
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Canertinib.Experimental
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Canertinib.Approved
ProxibarbalThe risk or severity of adverse effects can be increased when Canertinib is combined with Proxibarbal.Experimental
PSD502The risk or severity of adverse effects can be increased when Canertinib is combined with PSD502.Investigational
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Canertinib.Approved, Illicit
QuinisocaineThe risk or severity of adverse effects can be increased when Canertinib is combined with Quinisocaine.Experimental
RacloprideThe risk or severity of adverse effects can be increased when Canertinib is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Ramelteon is combined with Canertinib.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Canertinib.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Canertinib.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Canertinib.Approved, Investigational
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Canertinib.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Canertinib is combined with Ritanserin.Investigational
RomifidineThe risk or severity of adverse effects can be increased when Canertinib is combined with Romifidine.Vet Approved
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Canertinib.Approved
RotigotineCanertinib may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Canertinib.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Canertinib.Approved, Vet Approved
SepranoloneThe risk or severity of adverse effects can be increased when Canertinib is combined with Sepranolone.Investigational
SertindoleThe risk or severity of adverse effects can be increased when Canertinib is combined with Sertindole.Approved, Investigational, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Canertinib is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Canertinib.Approved, Vet Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Canertinib.Approved
StiripentolThe risk or severity of adverse effects can be increased when Stiripentol is combined with Canertinib.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Canertinib.Approved, Investigational
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Canertinib.Approved, Investigational
SultoprideThe risk or severity of adverse effects can be increased when Canertinib is combined with Sultopride.Experimental
SuvorexantCanertinib may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved, Investigational
TandospironeThe risk or severity of adverse effects can be increased when Canertinib is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Canertinib.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Tasimelteon is combined with Canertinib.Approved, Investigational
Technetium Tc-99m tilmanoceptCanertinib may decrease effectiveness of Technetium Tc-99m tilmanocept as a diagnostic agent.Approved, Investigational
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Canertinib.Approved, Investigational
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Canertinib.Approved, Investigational
TetracaineThe risk or severity of adverse effects can be increased when Canertinib is combined with Tetracaine.Approved, Vet Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Canertinib.Investigational
ThalidomideCanertinib may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Canertinib.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Canertinib.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Canertinib.Approved, Withdrawn
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Canertinib.Approved
TiagabineThe risk or severity of adverse effects can be increased when Tiagabine is combined with Canertinib.Approved, Investigational
TiaprideThe risk or severity of adverse effects can be increased when Canertinib is combined with Tiapride.Approved, Investigational
TiletamineThe risk or severity of adverse effects can be increased when Canertinib is combined with Tiletamine.Vet Approved
TilidineThe risk or severity of adverse effects can be increased when Canertinib is combined with Tilidine.Experimental
TizanidineThe risk or severity of adverse effects can be increased when Tizanidine is combined with Canertinib.Approved, Investigational
TolcaponeThe risk or severity of adverse effects can be increased when Tolcapone is combined with Canertinib.Approved, Withdrawn
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Canertinib.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Canertinib.Approved, Investigational
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Canertinib.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Canertinib.Approved, Investigational
Tricaine methanesulfonateThe risk or severity of adverse effects can be increased when Canertinib is combined with Tricaine methanesulfonate.Vet Approved
TrichloroethyleneThe risk or severity of adverse effects can be increased when Canertinib is combined with Trichloroethylene.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Canertinib.Approved, Investigational
TrifluperidolThe risk or severity of adverse effects can be increased when Canertinib is combined with Trifluperidol.Experimental
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Canertinib.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Canertinib.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Triprolidine is combined with Canertinib.Approved
VeraliprideThe risk or severity of adverse effects can be increased when Canertinib is combined with Veralipride.Experimental
VigabatrinThe risk or severity of adverse effects can be increased when Vigabatrin is combined with Canertinib.Approved
Vinyl etherThe risk or severity of adverse effects can be increased when Canertinib is combined with Vinyl ether.Experimental
VortioxetineThe risk or severity of adverse effects can be increased when Canertinib is combined with Vortioxetine.Approved, Investigational
XenonThe risk or severity of adverse effects can be increased when Canertinib is combined with Xenon.Experimental
XylazineThe risk or severity of adverse effects can be increased when Canertinib is combined with Xylazine.Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Canertinib.Approved, Illicit, Investigational
ZimelidineThe risk or severity of adverse effects can be increased when Canertinib is combined with Zimelidine.Withdrawn
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Canertinib.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Canertinib is combined with Zolazepam.Vet Approved
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Canertinib.Approved
ZotepineThe risk or severity of adverse effects can be increased when Canertinib is combined with Zotepine.Approved, Investigational, Withdrawn
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Canertinib.Approved, Investigational
Food Interactions
Not Available

References

General References
  1. Simon GR, Garrett CR, Olson SC, Langevin M, Eiseman IA, Mahany JJ, Williams CC, Lush R, Daud A, Munster P, Chiappori A, Fishman M, Bepler G, Lenehan PF, Sullivan DM: Increased bioavailability of intravenous versus oral CI-1033, a pan erbB tyrosine kinase inhibitor: results of a phase I pharmacokinetic study. Clin Cancer Res. 2006 Aug 1;12(15):4645-51. [PubMed:16899614]
  2. Sequist LV: Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. Oncologist. 2007 Mar;12(3):325-30. [PubMed:17405897]
External Links
PubChem Compound
156414
PubChem Substance
175427000
ChemSpider
137741
BindingDB
4779
ChEBI
61399
ChEMBL
CHEMBL31965
Wikipedia
Canertinib

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentNeoplasms, Breast1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0155 mg/mLALOGPS
logP4.09ALOGPS
logP3.9ChemAxon
logS-4.5ALOGPS
pKa (Strongest Acidic)12.54ChemAxon
pKa (Strongest Basic)6.87ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area88.61 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity130.55 m3·mol-1ChemAxon
Polarizability50.36 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9917
Blood Brain Barrier+0.9577
Caco-2 permeable-0.5685
P-glycoprotein substrateSubstrate0.6999
P-glycoprotein inhibitor IInhibitor0.9152
P-glycoprotein inhibitor IIInhibitor0.9592
Renal organic cation transporterInhibitor0.5
CYP450 2C9 substrateNon-substrate0.8114
CYP450 2D6 substrateNon-substrate0.7455
CYP450 3A4 substrateSubstrate0.6732
CYP450 1A2 substrateNon-inhibitor0.5366
CYP450 2C9 inhibitorInhibitor0.5958
CYP450 2D6 inhibitorNon-inhibitor0.8724
CYP450 2C19 inhibitorInhibitor0.5504
CYP450 3A4 inhibitorInhibitor0.827
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8911
Ames testNon AMES toxic0.5465
CarcinogenicityNon-carcinogens0.8916
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.7549 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.5387
hERG inhibition (predictor II)Inhibitor0.8273
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazanaphthalenes
Sub Class
Benzodiazines
Direct Parent
Quinazolinamines
Alternative Parents
Aniline and substituted anilines / N-arylamides / Alkyl aryl ethers / Aminopyrimidines and derivatives / Chlorobenzenes / Fluorobenzenes / Aryl chlorides / Aryl fluorides / Imidolactams / Morpholines
show 15 more
Substituents
Quinazolinamine / N-arylamide / Aniline or substituted anilines / Alkyl aryl ether / Halobenzene / Fluorobenzene / Aminopyrimidine / Chlorobenzene / Pyrimidine / Aryl chloride
show 33 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
organofluorine compound, monochlorobenzenes, quinazolines, morpholines (CHEBI:61399)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
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, TG...
Gene Name
EGFR
Uniprot ID
P00533
Uniprot Name
Epidermal growth factor receptor
Molecular Weight
134276.185 Da

Drug created on November 18, 2007 11:24 / Updated on August 02, 2018 05:30