Identification

Name
Crizotinib
Accession Number
DB08865  (DB08700)
Type
Small Molecule
Groups
Approved
Description

Crizotinib an inhibitor of receptor tyrosine kinase for the treatment of non-small cell lung cancer (NSCLC). Verification of the presence of ALK fusion gene is done by Abbott Molecular's Vysis ALK Break Apart FISH Probe Kit. This verification is used to select for patients suitable for treatment. FDA approved in August 26, 2011.

Structure
Thumb
Synonyms
  • (R)-crizotinib
  • Crizotinib
  • Crizotinibum
External IDs
1066 / PF 02341066 / PF 2341066 / PF-02341066 / PF-2341066
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
XalkoriCapsule200 mgOralPfizer2012-05-10Not applicableCanada
XalkoriCapsule250 mgOralPfizer2012-10-23Not applicableEu
XalkoriCapsule200 mgOralPfizer2012-10-23Not applicableEu
XalkoriCapsule200 mg/1OralPfizer Laboratories Div Pfizer Inc.2011-08-26Not applicableUs
XalkoriCapsule250 mgOralPfizer2012-10-23Not applicableEu
XalkoriCapsule250 mgOralPfizer2012-05-10Not applicableCanada
XalkoriCapsule250 mg/1OralPfizer Laboratories Div Pfizer Inc.2011-08-26Not applicableUs
XalkoriCapsule200 mgOralPfizer2012-10-23Not applicableEu
Categories
UNII
53AH36668S
CAS number
877399-52-5
Weight
Average: 450.337
Monoisotopic: 449.11854397
Chemical Formula
C21H22Cl2FN5O
InChI Key
KTEIFNKAUNYNJU-GFCCVEGCSA-N
InChI
InChI=1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m1/s1
IUPAC Name
3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]pyridin-2-amine
SMILES
C[[email protected]@H](OC1=CC(=CN=C1N)C1=CN(N=C1)C1CCNCC1)C1=C(Cl)C=CC(F)=C1Cl

Pharmacology

Indication

Crizotinib is used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) that is anaplastic-lymphoma kinase (ALK)-positive as detected by a FDA-approved test.

Structured Indications
Pharmacodynamics
Not Available
Mechanism of action

Crizotinib is a tyrosine kinase receptor inhibitor. More specifically, it inhibits anaplastic lymphoma kinase (ALK), hepatocyte growth factor receptor (HGFR, c-MET), and Recepteur d'Origine Nantais (RON). Abnormalities in the ALK gene caused by mutations or translocations may lead to expression of oncogenic fusion proteins. In patients with NSCLC, they have the EML4-ALK gene. Crizotinib inhibits ALK tyrosine kinase which ultimately results in decreased proliferation of cells that carry the genetic mutation and tumour survivability.

TargetActionsOrganism
AALK tyrosine kinase receptor
inhibitor
Human
AHepatocyte growth factor receptor
inhibitor
Human
Absorption

The peak serum concentration was reached in 4 to 6 hours following an oral single-dose administration. Steady state was reached within 15 days when a dose of 250 mg twice daily was administered. The mean absolute bioavailability was 43% (range of 32% to 66%) following a single 250 mg oral dose. When taken with high-fat meal, AUC and Cmax were reduced.

Volume of distribution

Mean volume of distribution (Vss) is 1772 L following intravenous administration of a 50 mg dose. This high volume of distribution suggest extensive distribution into tissue from plasma.

Protein binding

Crizotinib is 91% bound to plasma protein. This is not affected by drug concentration.

Metabolism

Crizotinib is metabolized by CYP3A4 and CYP3A5 in which these enzymes mediates the O-dealkylation of the drug.

Route of elimination

Following the administration of a single 250 mg radiolabeled crizotinib dose to healthy subjects, 63% and 22% of the administered dose was recovered in feces and urine, respectively. Unchanged crizotinib represented approximately 53% and 2.3% of the administered dose in feces and urine, respectively.

Half life

Plasma terminal half-life, patients = 42 hours

Clearance

The mean apparent clearance (CL/F) of crizotinib was lower at steady state (60 L/hr) after 250 mg twice daily than that after a single 250 mg oral dose (100 L/hr), which was likely due to autoinhibition of CYP3A by crizotinib after multiple dosing.

Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbemaciclibThe metabolism of Abemaciclib can be decreased when combined with Crizotinib.Approved
AbirateroneThe metabolism of Abiraterone can be decreased when combined with Crizotinib.Approved
AcenocoumarolThe metabolism of Acenocoumarol can be decreased when combined with Crizotinib.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Crizotinib.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Crizotinib.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Crizotinib.Experimental
AdinazolamThe metabolism of Adinazolam can be decreased when combined with Crizotinib.Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Crizotinib.Approved
AlbendazoleThe metabolism of Albendazole can be decreased when combined with Crizotinib.Approved, Vet Approved
AlclometasoneThe metabolism of Alclometasone can be decreased when combined with Crizotinib.Approved
AlfentanilThe serum concentration of Alfentanil can be increased when it is combined with Crizotinib.Approved, Illicit
AlfuzosinThe metabolism of Alfuzosin can be decreased when combined with Crizotinib.Approved, Investigational
AliskirenThe metabolism of Aliskiren can be decreased when combined with Crizotinib.Approved, Investigational
AllylestrenolThe metabolism of Allylestrenol can be decreased when combined with Crizotinib.Approved
AlmotriptanThe metabolism of Almotriptan can be decreased when combined with Crizotinib.Approved, Investigational
AlogliptinThe metabolism of Alogliptin can be decreased when combined with Crizotinib.Approved
AlosetronThe metabolism of Alosetron can be decreased when combined with Crizotinib.Approved, Withdrawn
AlprazolamThe metabolism of Alprazolam can be decreased when combined with Crizotinib.Approved, Illicit, Investigational
AmbrisentanThe metabolism of Ambrisentan can be decreased when combined with Crizotinib.Approved, Investigational
AmbroxolThe metabolism of Ambroxol can be decreased when combined with Crizotinib.Approved, Investigational
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Crizotinib.Approved, Withdrawn
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Crizotinib.Approved
AmiodaroneThe serum concentration of Crizotinib can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Crizotinib.Approved
AmlodipineThe metabolism of Amlodipine can be decreased when combined with Crizotinib.Approved
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Crizotinib.Approved
AncestimThe risk or severity of cytotoxicity can be increased when Ancestim is combined with Crizotinib.Approved, Investigational, Withdrawn
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Crizotinib.Approved
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Crizotinib.Approved
ApremilastThe metabolism of Apremilast can be decreased when combined with Crizotinib.Approved, Investigational
AprepitantThe serum concentration of Crizotinib can be increased when it is combined with Aprepitant.Approved, Investigational
ArgatrobanThe metabolism of Argatroban can be decreased when combined with Crizotinib.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Crizotinib.Approved, Investigational
ArtemetherThe metabolism of Artemether can be decreased when combined with Crizotinib.Approved
AsenapineThe metabolism of Asenapine can be decreased when combined with Crizotinib.Approved
AstemizoleThe metabolism of Astemizole can be decreased when combined with Crizotinib.Approved, Withdrawn
AtazanavirThe serum concentration of Crizotinib can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Crizotinib can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Crizotinib is combined with Atorvastatin.Approved
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Crizotinib.Approved
AxitinibThe metabolism of Axitinib can be decreased when combined with Crizotinib.Approved, Investigational
AzelastineThe metabolism of Azelastine can be decreased when combined with Crizotinib.Approved
AzithromycinThe metabolism of Azithromycin can be decreased when combined with Crizotinib.Approved
BanoxantroneThe metabolism of Banoxantrone can be decreased when combined with Crizotinib.Investigational
BaricitinibThe metabolism of Baricitinib can be decreased when combined with Crizotinib.Approved, Investigational
BedaquilineThe metabolism of Bedaquiline can be decreased when combined with Crizotinib.Approved
BenzphetamineThe metabolism of Benzphetamine can be decreased when combined with Crizotinib.Approved, Illicit
Benzyl alcoholThe metabolism of Benzyl alcohol can be decreased when combined with Crizotinib.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Crizotinib.Approved, Investigational
BexaroteneThe metabolism of Bexarotene can be decreased when combined with Crizotinib.Approved, Investigational
BezafibrateThe metabolism of Bezafibrate can be decreased when combined with Crizotinib.Approved
BicalutamideThe metabolism of Bicalutamide can be decreased when combined with Crizotinib.Approved
BisoprololThe metabolism of Bisoprolol can be decreased when combined with Crizotinib.Approved
BlonanserinThe metabolism of Blonanserin can be decreased when combined with Crizotinib.Approved, Investigational
BoceprevirThe serum concentration of Crizotinib can be increased when it is combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Crizotinib can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Bosentan can be increased when it is combined with Crizotinib.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Crizotinib.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Crizotinib.Approved
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Crizotinib.Approved
BrigatinibThe metabolism of Brigatinib can be decreased when combined with Crizotinib.Approved
BrinzolamideThe metabolism of Brinzolamide can be decreased when combined with Crizotinib.Approved
BrivaracetamThe metabolism of Brivaracetam can be decreased when combined with Crizotinib.Approved, Investigational
BromazepamThe metabolism of Bromazepam can be decreased when combined with Crizotinib.Approved, Illicit
BromocriptineThe metabolism of Bromocriptine can be decreased when combined with Crizotinib.Approved, Investigational
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Crizotinib.Approved
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Crizotinib.Approved
BupivacaineThe metabolism of Bupivacaine can be decreased when combined with Crizotinib.Approved, Investigational
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Crizotinib.Approved, Illicit, Investigational, Vet Approved
BupropionThe serum concentration of Bupropion can be increased when it is combined with Crizotinib.Approved
BuspironeThe metabolism of Buspirone can be decreased when combined with Crizotinib.Approved, Investigational
BusulfanThe metabolism of Busulfan can be decreased when combined with Crizotinib.Approved, Investigational
CabazitaxelThe metabolism of Cabazitaxel can be decreased when combined with Crizotinib.Approved
CabergolineThe metabolism of Cabergoline can be decreased when combined with Crizotinib.Approved
CabozantinibThe metabolism of Cabozantinib can be decreased when combined with Crizotinib.Approved
CaffeineThe metabolism of Caffeine can be decreased when combined with Crizotinib.Approved
CalcitriolThe metabolism of Calcitriol can be decreased when combined with Crizotinib.Approved, Nutraceutical
CanagliflozinThe metabolism of Canagliflozin can be decreased when combined with Crizotinib.Approved
CannabidiolThe metabolism of Cannabidiol can be decreased when combined with Crizotinib.Approved, Investigational
CarbamazepineThe serum concentration of Crizotinib can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Crizotinib.Approved
CariprazineThe metabolism of Cariprazine can be decreased when combined with Crizotinib.Approved
CarvedilolThe metabolism of Carvedilol can be decreased when combined with Crizotinib.Approved, Investigational
CelecoxibThe metabolism of Celecoxib can be decreased when combined with Crizotinib.Approved, Investigational
CeliprololThe metabolism of Celiprolol can be decreased when combined with Crizotinib.Approved, Investigational
CephalexinThe metabolism of Cephalexin can be decreased when combined with Crizotinib.Approved, Vet Approved
CeritinibThe serum concentration of Crizotinib can be increased when it is combined with Ceritinib.Approved
CerivastatinThe metabolism of Cerivastatin can be decreased when combined with Crizotinib.Withdrawn
CevimelineThe metabolism of Cevimeline can be decreased when combined with Crizotinib.Approved
Chenodeoxycholic acidThe metabolism of Chenodeoxycholic acid can be decreased when combined with Crizotinib.Approved
ChlordiazepoxideThe metabolism of Chlordiazepoxide can be decreased when combined with Crizotinib.Approved, Illicit
ChloroquineThe metabolism of Chloroquine can be decreased when combined with Crizotinib.Approved, Vet Approved
ChlorphenamineThe metabolism of Chlorphenamine can be decreased when combined with Crizotinib.Approved
ChlorpromazineThe metabolism of Chlorpromazine can be decreased when combined with Crizotinib.Approved, Vet Approved
ChlorzoxazoneThe metabolism of Chlorzoxazone can be decreased when combined with Crizotinib.Approved
CholecalciferolThe metabolism of Cholecalciferol can be decreased when combined with Crizotinib.Approved, Nutraceutical
CiclesonideThe metabolism of Ciclesonide can be decreased when combined with Crizotinib.Approved, Investigational
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Crizotinib.Approved
CinacalcetThe metabolism of Cinacalcet can be decreased when combined with Crizotinib.Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Crizotinib.Approved, Investigational
CisaprideThe metabolism of Cisapride can be decreased when combined with Crizotinib.Approved, Investigational, Withdrawn
CitalopramThe metabolism of Citalopram can be decreased when combined with Crizotinib.Approved
ClarithromycinThe serum concentration of Crizotinib can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Crizotinib can be decreased when combined with Clemastine.Approved
ClindamycinThe metabolism of Clindamycin can be decreased when combined with Crizotinib.Approved, Vet Approved
ClobazamThe metabolism of Clobazam can be decreased when combined with Crizotinib.Approved, Illicit
ClofazimineThe metabolism of Clofazimine can be decreased when combined with Crizotinib.Approved, Investigational
ClofibrateThe metabolism of Clofibrate can be decreased when combined with Crizotinib.Approved, Investigational
clomethiazoleThe metabolism of clomethiazole can be decreased when combined with Crizotinib.Investigational
ClomipramineThe metabolism of Clomipramine can be decreased when combined with Crizotinib.Approved, Vet Approved
ClonazepamThe metabolism of Clonazepam can be decreased when combined with Crizotinib.Approved, Illicit
ClonidineThe metabolism of Clonidine can be decreased when combined with Crizotinib.Approved
ClopidogrelThe metabolism of Clopidogrel can be decreased when combined with Crizotinib.Approved
ClorazepateThe metabolism of Clorazepate can be decreased when combined with Crizotinib.Approved, Illicit
ClotiazepamThe metabolism of Clotiazepam can be decreased when combined with Crizotinib.Approved, Illicit
ClotrimazoleThe metabolism of Crizotinib can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Clozapine can be decreased when combined with Crizotinib.Approved
CobicistatThe serum concentration of Crizotinib can be increased when it is combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Crizotinib.Approved
CocaineThe metabolism of Cocaine can be decreased when combined with Crizotinib.Approved, Illicit
CodeineThe metabolism of Codeine can be decreased when combined with Crizotinib.Approved, Illicit
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Crizotinib.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Crizotinib.Approved, Investigational
Conjugated estrogensThe metabolism of Conjugated estrogens can be decreased when combined with Crizotinib.Approved
CopanlisibThe metabolism of Copanlisib can be decreased when combined with Crizotinib.Approved
Cortisone acetateThe metabolism of Cortisone acetate can be decreased when combined with Crizotinib.Approved
CyclobenzaprineThe metabolism of Cyclobenzaprine can be decreased when combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Crizotinib.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Crizotinib.Approved, Investigational, Vet Approved
CymarinCymarin may decrease the cardiotoxic activities of Crizotinib.Experimental
CytarabineThe metabolism of Cytarabine can be decreased when combined with Crizotinib.Approved, Investigational
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Crizotinib.Approved
DabrafenibThe serum concentration of Crizotinib can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe metabolism of Daclatasvir can be decreased when combined with Crizotinib.Approved
DantroleneThe metabolism of Dantrolene can be decreased when combined with Crizotinib.Approved
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Crizotinib.Approved
DapoxetineThe serum concentration of Dapoxetine can be increased when it is combined with Crizotinib.Investigational
DapsoneThe metabolism of Dapsone can be decreased when combined with Crizotinib.Approved, Investigational
DarifenacinThe metabolism of Darifenacin can be decreased when combined with Crizotinib.Approved, Investigational
DarunavirThe serum concentration of Crizotinib can be increased when it is combined with Darunavir.Approved
DasabuvirThe metabolism of Dasabuvir can be decreased when combined with Crizotinib.Approved
DasatinibThe serum concentration of Crizotinib can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe metabolism of Daunorubicin can be decreased when combined with Crizotinib.Approved
DeferasiroxThe serum concentration of Crizotinib can be decreased when it is combined with Deferasirox.Approved, Investigational
DeflazacortThe metabolism of Deflazacort can be decreased when combined with Crizotinib.Approved, Investigational
DelavirdineThe metabolism of Crizotinib can be decreased when combined with Delavirdine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Crizotinib.Approved
DesvenlafaxineThe metabolism of Desvenlafaxine can be decreased when combined with Crizotinib.Approved
DeutetrabenazineThe metabolism of Deutetrabenazine can be decreased when combined with Crizotinib.Approved, Investigational
DexamethasoneThe metabolism of Dexamethasone can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
Dexchlorpheniramine maleateThe metabolism of Dexchlorpheniramine maleate can be decreased when combined with Crizotinib.Approved
DexlansoprazoleThe metabolism of Dexlansoprazole can be decreased when combined with Crizotinib.Approved
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Crizotinib.Approved
DextropropoxypheneThe metabolism of Dextropropoxyphene can be decreased when combined with Crizotinib.Approved, Illicit, Investigational, Withdrawn
DiazepamThe metabolism of Diazepam can be decreased when combined with Crizotinib.Approved, Illicit, Vet Approved
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Crizotinib.Approved, Vet Approved
DienogestThe metabolism of Dienogest can be decreased when combined with Crizotinib.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Crizotinib.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Crizotinib.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Crizotinib.Approved
DihydrocodeineThe metabolism of Dihydrocodeine can be decreased when combined with Crizotinib.Approved, Illicit
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Crizotinib.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Crizotinib.Approved, Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Crizotinib.Experimental
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Crizotinib.Approved
DiltiazemThe metabolism of Crizotinib can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Crizotinib.Approved
DisopyramideThe metabolism of Disopyramide can be decreased when combined with Crizotinib.Approved
DisulfiramThe metabolism of Disulfiram can be decreased when combined with Crizotinib.Approved
DocetaxelThe metabolism of Docetaxel can be decreased when combined with Crizotinib.Approved, Investigational
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Crizotinib.Approved
DolasetronThe metabolism of Dolasetron can be decreased when combined with Crizotinib.Approved
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Crizotinib.Approved, Investigational, Vet Approved
DonepezilThe metabolism of Donepezil can be decreased when combined with Crizotinib.Approved
DorzolamideThe metabolism of Dorzolamide can be decreased when combined with Crizotinib.Approved
DoxepinThe metabolism of Doxepin can be decreased when combined with Crizotinib.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Crizotinib.Approved, Investigational
DoxorubicinThe metabolism of Doxorubicin can be decreased when combined with Crizotinib.Approved, Investigational
DoxycyclineThe metabolism of Crizotinib can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Crizotinib.Approved, Illicit
DronedaroneThe metabolism of Crizotinib can be decreased when combined with Dronedarone.Approved
DutasterideThe metabolism of Dutasteride can be decreased when combined with Crizotinib.Approved, Investigational
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Crizotinib.Approved
EfavirenzThe metabolism of Efavirenz can be decreased when combined with Crizotinib.Approved, Investigational
ElbasvirThe metabolism of Elbasvir can be decreased when combined with Crizotinib.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Crizotinib.Approved, Investigational
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Crizotinib.Approved
ElvitegravirThe metabolism of Elvitegravir can be decreased when combined with Crizotinib.Approved
EnalaprilThe metabolism of Enalapril can be decreased when combined with Crizotinib.Approved, Vet Approved
EnasidenibThe metabolism of Enasidenib can be decreased when combined with Crizotinib.Approved
EnzalutamideThe serum concentration of Crizotinib can be decreased when it is combined with Enzalutamide.Approved
EpinastineThe metabolism of Epinastine can be decreased when combined with Crizotinib.Approved, Investigational
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Crizotinib.Approved
ErgocalciferolThe metabolism of Ergocalciferol can be decreased when combined with Crizotinib.Approved, Nutraceutical
Ergoloid mesylateThe metabolism of Ergoloid mesylate can be decreased when combined with Crizotinib.Approved
ErgonovineThe metabolism of Ergonovine can be decreased when combined with Crizotinib.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Crizotinib.Approved
ErlotinibThe metabolism of Erlotinib can be decreased when combined with Crizotinib.Approved, Investigational
ErythromycinThe metabolism of Crizotinib can be decreased when combined with Erythromycin.Approved, Vet Approved
EscitalopramThe metabolism of Escitalopram can be decreased when combined with Crizotinib.Approved, Investigational
EsomeprazoleThe metabolism of Esomeprazole can be decreased when combined with Crizotinib.Approved, Investigational
EstazolamThe metabolism of Estazolam can be decreased when combined with Crizotinib.Approved, Illicit
EstradiolThe metabolism of Estradiol can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
Estradiol acetateThe metabolism of Estradiol acetate can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
Estradiol benzoateThe metabolism of Estradiol benzoate can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
Estradiol cypionateThe metabolism of Estradiol cypionate can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
Estradiol dienanthateThe metabolism of Estradiol dienanthate can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
Estradiol valerateThe metabolism of Estradiol valerate can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
EstramustineThe metabolism of Estramustine can be decreased when combined with Crizotinib.Approved
Estrogens, esterifiedThe metabolism of Estrogens, esterified can be decreased when combined with Crizotinib.Approved
EstroneThe metabolism of Estrone can be decreased when combined with Crizotinib.Approved
Estrone sulfateThe metabolism of Estrone sulfate can be decreased when combined with Crizotinib.Approved
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Crizotinib.Approved
EthanolThe metabolism of Ethanol can be decreased when combined with Crizotinib.Approved
Ethinyl EstradiolThe metabolism of Ethinyl Estradiol can be decreased when combined with Crizotinib.Approved
EthosuximideThe metabolism of Ethosuximide can be decreased when combined with Crizotinib.Approved
EthylmorphineThe metabolism of Ethylmorphine can be decreased when combined with Crizotinib.Approved, Illicit
EtizolamThe metabolism of Etizolam can be decreased when combined with Crizotinib.Approved
EtonogestrelThe metabolism of Etonogestrel can be decreased when combined with Crizotinib.Approved, Investigational
EtoposideThe metabolism of Etoposide can be decreased when combined with Crizotinib.Approved
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Crizotinib.Approved, Investigational
EtravirineThe metabolism of Etravirine can be decreased when combined with Crizotinib.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Crizotinib.Approved
ExemestaneThe metabolism of Exemestane can be decreased when combined with Crizotinib.Approved, Investigational
FamciclovirThe metabolism of Famciclovir can be decreased when combined with Crizotinib.Approved
FelbamateThe metabolism of Felbamate can be decreased when combined with Crizotinib.Approved
FelodipineThe metabolism of Felodipine can be decreased when combined with Crizotinib.Approved, Investigational
FenofibrateThe metabolism of Fenofibrate can be decreased when combined with Crizotinib.Approved
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Crizotinib.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe metabolism of Fesoterodine can be decreased when combined with Crizotinib.Approved
FinasterideThe metabolism of Finasteride can be decreased when combined with Crizotinib.Approved
FingolimodThe metabolism of Fingolimod can be decreased when combined with Crizotinib.Approved, Investigational
FlibanserinThe risk or severity of adverse effects can be increased when Crizotinib is combined with Flibanserin.Approved
FluconazoleThe metabolism of Crizotinib can be decreased when combined with Fluconazole.Approved
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Crizotinib.Approved
FlunisolideThe metabolism of Flunisolide can be decreased when combined with Crizotinib.Approved, Investigational
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Crizotinib.Approved, Illicit
FluorometholoneThe metabolism of Fluorometholone can be decreased when combined with Crizotinib.Approved
FluoxetineThe metabolism of Fluoxetine can be decreased when combined with Crizotinib.Approved, Vet Approved
FlurazepamThe metabolism of Flurazepam can be decreased when combined with Crizotinib.Approved, Illicit
FlutamideThe metabolism of Flutamide can be decreased when combined with Crizotinib.Approved
Fluticasone furoateThe metabolism of Fluticasone furoate can be decreased when combined with Crizotinib.Approved
Fluticasone propionateThe metabolism of Fluticasone propionate can be decreased when combined with Crizotinib.Approved
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Crizotinib.Approved
FluvoxamineThe metabolism of Crizotinib can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Crizotinib can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Crizotinib can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of Crizotinib can be decreased when it is combined with Fosphenytoin.Approved
FulvestrantThe metabolism of Fulvestrant can be decreased when combined with Crizotinib.Approved, Investigational
Fusidic AcidThe serum concentration of Crizotinib can be increased when it is combined with Fusidic Acid.Approved
GalantamineThe metabolism of Galantamine can be decreased when combined with Crizotinib.Approved
GefitinibThe metabolism of Gefitinib can be decreased when combined with Crizotinib.Approved, Investigational
GemfibrozilThe metabolism of Gemfibrozil can be decreased when combined with Crizotinib.Approved
GitoformateGitoformate may decrease the cardiotoxic activities of Crizotinib.Experimental
GlipizideThe metabolism of Glipizide can be decreased when combined with Crizotinib.Approved
GlyburideThe metabolism of Glyburide can be decreased when combined with Crizotinib.Approved
GranisetronThe metabolism of Granisetron can be decreased when combined with Crizotinib.Approved, Investigational
GrazoprevirThe metabolism of Grazoprevir can be decreased when combined with Crizotinib.Approved
GrepafloxacinThe metabolism of Grepafloxacin can be decreased when combined with Crizotinib.Investigational, Withdrawn
GuanfacineThe metabolism of Guanfacine can be decreased when combined with Crizotinib.Approved, Investigational
HalofantrineThe serum concentration of Halofantrine can be increased when it is combined with Crizotinib.Approved
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Crizotinib.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Crizotinib.Approved, Vet Approved
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Crizotinib.Approved
HistamineThe metabolism of Histamine can be decreased when combined with Crizotinib.Approved, Investigational
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Crizotinib.Approved, Illicit
HydrocortisoneThe metabolism of Hydrocortisone can be decreased when combined with Crizotinib.Approved, Vet Approved
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Crizotinib.Approved, Illicit
Hydroxyprogesterone caproateThe metabolism of Hydroxyprogesterone caproate can be decreased when combined with Crizotinib.Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Crizotinib.Approved
IcotinibThe metabolism of Icotinib can be decreased when combined with Crizotinib.Approved, Investigational
IdelalisibThe serum concentration of Crizotinib can be increased when it is combined with Idelalisib.Approved
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be reduced when Ifosfamide is used in combination with Crizotinib resulting in a loss in efficacy.Approved
IloperidoneThe metabolism of Iloperidone can be decreased when combined with Crizotinib.Approved
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Crizotinib.Approved
ImidafenacinThe metabolism of Imidafenacin can be decreased when combined with Crizotinib.Approved, Investigational
ImipramineThe metabolism of Imipramine can be decreased when combined with Crizotinib.Approved
ImiquimodThe metabolism of Imiquimod can be decreased when combined with Crizotinib.Approved, Investigational
IndacaterolThe metabolism of Indacaterol can be decreased when combined with Crizotinib.Approved
IndapamideThe metabolism of Indapamide can be decreased when combined with Crizotinib.Approved
IndinavirThe serum concentration of Crizotinib can be increased when it is combined with Indinavir.Approved
Ipratropium bromideThe metabolism of Ipratropium bromide can be decreased when combined with Crizotinib.Approved
IrinotecanThe metabolism of Irinotecan can be decreased when combined with Crizotinib.Approved, Investigational
IsavuconazoniumThe metabolism of Isavuconazonium can be decreased when combined with Crizotinib.Approved, Investigational
IsofluraneThe metabolism of Isoflurane can be decreased when combined with Crizotinib.Approved, Vet Approved
Isosorbide DinitrateThe metabolism of Isosorbide Dinitrate can be decreased when combined with Crizotinib.Approved
Isosorbide MononitrateThe metabolism of Isosorbide Mononitrate can be decreased when combined with Crizotinib.Approved
IsradipineThe metabolism of Crizotinib can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of Crizotinib can be increased when it is combined with Itraconazole.Approved, Investigational
IvabradineThe metabolism of Ivabradine can be decreased when combined with Crizotinib.Approved
IvacaftorThe serum concentration of Ivacaftor can be increased when it is combined with Crizotinib.Approved
IvermectinThe metabolism of Ivermectin can be decreased when combined with Crizotinib.Approved, Vet Approved
IxabepiloneThe metabolism of Ixabepilone can be decreased when combined with Crizotinib.Approved, Investigational
IxazomibThe metabolism of Ixazomib can be decreased when combined with Crizotinib.Approved
KetamineThe metabolism of Ketamine can be decreased when combined with Crizotinib.Approved, Vet Approved
KetazolamThe metabolism of Ketazolam can be decreased when combined with Crizotinib.Approved
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Crizotinib.Approved, Investigational
KetoconazoleThe serum concentration of Crizotinib can be increased when it is combined with Ketoconazole.Approved, Investigational
LacidipineThe metabolism of Lacidipine can be decreased when combined with Crizotinib.Approved, Investigational
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Crizotinib.Experimental
LansoprazoleThe metabolism of Lansoprazole can be decreased when combined with Crizotinib.Approved, Investigational
LapatinibThe metabolism of Lapatinib can be decreased when combined with Crizotinib.Approved, Investigational
LaquinimodThe metabolism of Laquinimod can be decreased when combined with Crizotinib.Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Crizotinib.Approved
LenvatinibThe metabolism of Lenvatinib can be decreased when combined with Crizotinib.Approved
LercanidipineThe metabolism of Lercanidipine can be decreased when combined with Crizotinib.Approved, Investigational
LetrozoleThe metabolism of Letrozole can be decreased when combined with Crizotinib.Approved, Investigational
LevobupivacaineThe metabolism of Levobupivacaine can be decreased when combined with Crizotinib.Approved, Investigational
LevocetirizineThe metabolism of Levocetirizine can be decreased when combined with Crizotinib.Approved
Levomethadyl AcetateThe metabolism of Levomethadyl Acetate can be decreased when combined with Crizotinib.Approved, Investigational
LevomilnacipranThe metabolism of Levomilnacipran can be decreased when combined with Crizotinib.Approved
LevonorgestrelThe metabolism of Levonorgestrel can be decreased when combined with Crizotinib.Approved, Investigational
LevothyroxineThe metabolism of Levothyroxine can be decreased when combined with Crizotinib.Approved
LidocaineThe metabolism of Lidocaine can be decreased when combined with Crizotinib.Approved, Vet Approved
LisurideThe metabolism of Lisuride can be decreased when combined with Crizotinib.Approved, Investigational
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Crizotinib.Approved
LoperamideThe metabolism of Loperamide can be decreased when combined with Crizotinib.Approved
LopinavirThe serum concentration of Crizotinib can be increased when it is combined with Lopinavir.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Crizotinib.Approved
LorcaserinThe metabolism of Lorcaserin can be decreased when combined with Crizotinib.Approved
LosartanThe metabolism of Losartan can be decreased when combined with Crizotinib.Approved
LovastatinThe metabolism of Crizotinib can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Crizotinib can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Crizotinib can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Lumefantrine can be decreased when combined with Crizotinib.Approved
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Crizotinib.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Crizotinib.Illicit, Investigational, Withdrawn
MacimorelinThe metabolism of Macimorelin can be decreased when combined with Crizotinib.Approved, Investigational
MacitentanThe metabolism of Macitentan can be decreased when combined with Crizotinib.Approved
MalathionThe metabolism of Malathion can be decreased when combined with Crizotinib.Approved, Investigational
MaravirocThe metabolism of Maraviroc can be decreased when combined with Crizotinib.Approved, Investigational
MebendazoleThe metabolism of Mebendazole can be decreased when combined with Crizotinib.Approved, Vet Approved
Medroxyprogesterone acetateThe metabolism of Medroxyprogesterone acetate can be decreased when combined with Crizotinib.Approved, Investigational
MefloquineThe metabolism of Mefloquine can be decreased when combined with Crizotinib.Approved
MeloxicamThe metabolism of Meloxicam can be decreased when combined with Crizotinib.Approved, Vet Approved
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Crizotinib.Investigational, Withdrawn
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Crizotinib.Experimental
MethadoneThe metabolism of Methadone can be decreased when combined with Crizotinib.Approved
MethaqualoneThe metabolism of Methaqualone can be decreased when combined with Crizotinib.Illicit, Withdrawn
MethoxsalenThe metabolism of Methoxsalen can be decreased when combined with Crizotinib.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Crizotinib.Approved
MethylphenobarbitalThe metabolism of Methylphenobarbital can be decreased when combined with Crizotinib.Approved
MethylprednisoloneThe metabolism of Methylprednisolone can be decreased when combined with Crizotinib.Approved, Vet Approved
MethyltestosteroneThe metabolism of Methyltestosterone can be decreased when combined with Crizotinib.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Crizotinib.Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Crizotinib.Experimental
MetronidazoleThe metabolism of Metronidazole can be decreased when combined with Crizotinib.Approved
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Crizotinib.Experimental
MexiletineThe metabolism of Mexiletine can be decreased when combined with Crizotinib.Approved
MianserinThe metabolism of Mianserin can be decreased when combined with Crizotinib.Approved, Investigational
MibefradilThe metabolism of Mibefradil can be decreased when combined with Crizotinib.Investigational, Withdrawn
MiconazoleThe metabolism of Miconazole can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
MidazolamThe metabolism of Midazolam can be decreased when combined with Crizotinib.Approved, Illicit
MidostaurinThe metabolism of Midostaurin can be decreased when combined with Crizotinib.Approved
MifepristoneThe serum concentration of Crizotinib can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe metabolism of Mirabegron can be decreased when combined with Crizotinib.Approved
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Crizotinib.Approved
MitotaneThe serum concentration of Crizotinib can be decreased when it is combined with Mitotane.Approved
ModafinilThe metabolism of Modafinil can be decreased when combined with Crizotinib.Approved, Investigational
MontelukastThe metabolism of Montelukast can be decreased when combined with Crizotinib.Approved
MorphineThe metabolism of Morphine can be decreased when combined with Crizotinib.Approved, Investigational
Mycophenolate mofetilThe metabolism of Mycophenolate mofetil can be decreased when combined with Crizotinib.Approved, Investigational
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Crizotinib.Approved
NaloxoneThe metabolism of Naloxone can be decreased when combined with Crizotinib.Approved, Vet Approved
NateglinideThe metabolism of Nateglinide can be decreased when combined with Crizotinib.Approved, Investigational
NefazodoneThe serum concentration of Crizotinib can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Crizotinib can be increased when it is combined with Nelfinavir.Approved
NeratinibThe metabolism of Neratinib can be decreased when combined with Crizotinib.Approved, Investigational
NetupitantThe serum concentration of Crizotinib can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of Crizotinib can be decreased when it is combined with Nevirapine.Approved
NicardipineThe metabolism of Nicardipine can be decreased when combined with Crizotinib.Approved
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Crizotinib.Approved, Investigational
NicotineThe metabolism of Nicotine can be decreased when combined with Crizotinib.Approved
NifedipineThe metabolism of Nifedipine can be decreased when combined with Crizotinib.Approved
NilotinibThe metabolism of Crizotinib can be decreased when combined with Nilotinib.Approved, Investigational
NilvadipineThe metabolism of Nilvadipine can be decreased when combined with Crizotinib.Approved, Investigational
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Crizotinib.Approved
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Crizotinib.Approved
NisoldipineThe metabolism of Nisoldipine can be decreased when combined with Crizotinib.Approved
NitrazepamThe metabolism of Nitrazepam can be decreased when combined with Crizotinib.Approved
NitrendipineThe metabolism of Nitrendipine can be decreased when combined with Crizotinib.Approved, Investigational
NorethisteroneThe metabolism of Norethisterone can be decreased when combined with Crizotinib.Approved
NorgestrelThe metabolism of Norgestrel can be decreased when combined with Crizotinib.Approved
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Crizotinib.Approved
OdanacatibThe metabolism of Odanacatib can be decreased when combined with Crizotinib.Investigational
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Crizotinib.Approved
OleandrinOleandrin may decrease the cardiotoxic activities of Crizotinib.Experimental, Investigational
OlopatadineThe metabolism of Olopatadine can be decreased when combined with Crizotinib.Approved
OmeprazoleThe metabolism of Omeprazole can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
OndansetronThe metabolism of Ondansetron can be decreased when combined with Crizotinib.Approved
OrphenadrineThe metabolism of Orphenadrine can be decreased when combined with Crizotinib.Approved
OsimertinibThe serum concentration of Crizotinib can be increased when it is combined with Osimertinib.Approved
OspemifeneThe metabolism of Ospemifene can be decreased when combined with Crizotinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Crizotinib.Approved
OxazepamThe metabolism of Oxazepam can be decreased when combined with Crizotinib.Approved
OxybutyninThe metabolism of Oxybutynin can be decreased when combined with Crizotinib.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Crizotinib is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe metabolism of Oxymorphone can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
PaclitaxelThe metabolism of Paclitaxel can be decreased when combined with Crizotinib.Approved, Vet Approved
PalbociclibThe serum concentration of Crizotinib can be increased when it is combined with Palbociclib.Approved
PalonosetronThe metabolism of Palonosetron can be decreased when combined with Crizotinib.Approved, Investigational
PanobinostatThe metabolism of Panobinostat can be decreased when combined with Crizotinib.Approved, Investigational
PantoprazoleThe metabolism of Pantoprazole can be decreased when combined with Crizotinib.Approved
ParamethadioneThe metabolism of Paramethadione can be decreased when combined with Crizotinib.Approved
ParamethasoneThe metabolism of Paramethasone can be decreased when combined with Crizotinib.Approved
ParecoxibThe metabolism of Parecoxib can be decreased when combined with Crizotinib.Approved
ParicalcitolThe metabolism of Paricalcitol can be decreased when combined with Crizotinib.Approved, Investigational
ParitaprevirThe metabolism of Paritaprevir can be decreased when combined with Crizotinib.Approved
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Crizotinib.Approved
PentamidineThe metabolism of Pentamidine can be decreased when combined with Crizotinib.Approved
PentobarbitalThe serum concentration of Crizotinib can be decreased when it is combined with Pentobarbital.Approved, Vet Approved
PerampanelThe metabolism of Perampanel can be decreased when combined with Crizotinib.Approved
PergolideThe metabolism of Pergolide can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved, Withdrawn
PerhexilineThe metabolism of Perhexiline can be decreased when combined with Crizotinib.Approved, Investigational
PermethrinThe metabolism of Permethrin can be decreased when combined with Crizotinib.Approved, Investigational
PerospironeThe metabolism of Perospirone can be decreased when combined with Crizotinib.Approved
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Crizotinib.Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Crizotinib.Experimental
PethidineThe metabolism of Pethidine can be decreased when combined with Crizotinib.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Crizotinib.Withdrawn
PhenobarbitalThe serum concentration of Crizotinib can be decreased when it is combined with Phenobarbital.Approved
PhenoxybenzamineThe metabolism of Phenoxybenzamine can be decreased when combined with Crizotinib.Approved
PhenprocoumonThe metabolism of Phenprocoumon can be decreased when combined with Crizotinib.Approved, Investigational
PhenytoinThe serum concentration of Crizotinib can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PilocarpineThe metabolism of Pilocarpine can be decreased when combined with Crizotinib.Approved
PimecrolimusThe metabolism of Pimecrolimus can be decreased when combined with Crizotinib.Approved, Investigational
PimozideCrizotinib may increase the QTc-prolonging activities of Pimozide.Approved
PinacidilThe metabolism of Pinacidil can be decreased when combined with Crizotinib.Withdrawn
PioglitazoneThe metabolism of Pioglitazone can be decreased when combined with Crizotinib.Approved, Investigational
PipotiazineThe metabolism of Pipotiazine can be decreased when combined with Crizotinib.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Crizotinib.Approved
PodofiloxThe metabolism of Podofilox can be decreased when combined with Crizotinib.Approved
PomalidomideThe metabolism of Pomalidomide can be decreased when combined with Crizotinib.Approved
PonatinibThe metabolism of Ponatinib can be decreased when combined with Crizotinib.Approved
PosaconazoleThe serum concentration of Crizotinib can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PrasteroneThe metabolism of Prasterone can be decreased when combined with Crizotinib.Approved, Nutraceutical
PrasugrelThe metabolism of Prasugrel can be decreased when combined with Crizotinib.Approved
PravastatinThe metabolism of Pravastatin can be decreased when combined with Crizotinib.Approved
PrazepamThe metabolism of Prazepam can be decreased when combined with Crizotinib.Approved, Illicit
PraziquantelThe metabolism of Praziquantel can be decreased when combined with Crizotinib.Approved, Vet Approved
PrednisoloneThe metabolism of Prednisolone can be decreased when combined with Crizotinib.Approved, Vet Approved
PrednisoneThe metabolism of Prednisone can be decreased when combined with Crizotinib.Approved, Vet Approved
PrimaquineThe metabolism of Primaquine can be decreased when combined with Crizotinib.Approved
PrimidoneThe serum concentration of Crizotinib can be decreased when it is combined with Primidone.Approved, Vet Approved
ProchlorperazineThe metabolism of Prochlorperazine can be decreased when combined with Crizotinib.Approved, Vet Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Crizotinib.Approved, Vet Approved
ProguanilThe metabolism of Proguanil can be decreased when combined with Crizotinib.Approved
PromazineThe metabolism of Promazine can be decreased when combined with Crizotinib.Approved, Vet Approved
PromethazineThe metabolism of Promethazine can be decreased when combined with Crizotinib.Approved
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Crizotinib.Approved
PropofolThe metabolism of Propofol can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
Propoxyphene napsylateThe metabolism of Propoxyphene napsylate can be decreased when combined with Crizotinib.Approved
PropranololThe metabolism of Propranolol can be decreased when combined with Crizotinib.Approved, Investigational
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Crizotinib.Experimental
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Crizotinib.Approved
PyrazinamideThe metabolism of Pyrazinamide can be decreased when combined with Crizotinib.Approved
QuazepamThe metabolism of Quazepam can be decreased when combined with Crizotinib.Approved, Illicit
QuetiapineThe metabolism of Quetiapine can be decreased when combined with Crizotinib.Approved
QuinacrineThe metabolism of Quinacrine can be decreased when combined with Crizotinib.Approved, Investigational
QuinidineCrizotinib may increase the QTc-prolonging activities of Quinidine.Approved
QuinineThe metabolism of Quinine can be decreased when combined with Crizotinib.Approved
RabeprazoleThe metabolism of Rabeprazole can be decreased when combined with Crizotinib.Approved, Investigational
RaloxifeneThe metabolism of Raloxifene can be decreased when combined with Crizotinib.Approved, Investigational
RamelteonThe metabolism of Ramelteon can be decreased when combined with Crizotinib.Approved, Investigational
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Crizotinib.Approved, Investigational
ReboxetineThe metabolism of Reboxetine can be decreased when combined with Crizotinib.Approved, Investigational
RegorafenibThe metabolism of Regorafenib can be decreased when combined with Crizotinib.Approved
RepaglinideThe metabolism of Repaglinide can be decreased when combined with Crizotinib.Approved, Investigational
RetapamulinThe metabolism of Retapamulin can be decreased when combined with Crizotinib.Approved
RifabutinThe serum concentration of Crizotinib can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Crizotinib can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Crizotinib can be decreased when it is combined with Rifapentine.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Crizotinib.Approved, Investigational
RilpivirineThe serum concentration of Rilpivirine can be increased when it is combined with Crizotinib.Approved
RimonabantThe metabolism of Rimonabant can be decreased when combined with Crizotinib.Approved, Investigational
RiociguatThe metabolism of Riociguat can be decreased when combined with Crizotinib.Approved
RisperidoneThe metabolism of Risperidone can be decreased when combined with Crizotinib.Approved, Investigational
RitonavirThe metabolism of Ritonavir can be decreased when combined with Crizotinib.Approved, Investigational
RivaroxabanThe metabolism of Rivaroxaban can be decreased when combined with Crizotinib.Approved
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Crizotinib.Investigational, Withdrawn
RolapitantThe metabolism of Rolapitant can be decreased when combined with Crizotinib.Approved
RomidepsinThe metabolism of Romidepsin can be decreased when combined with Crizotinib.Approved, Investigational
RopiniroleThe metabolism of Ropinirole can be decreased when combined with Crizotinib.Approved, Investigational
RopivacaineThe metabolism of Ropivacaine can be decreased when combined with Crizotinib.Approved
RosuvastatinThe metabolism of Rosuvastatin can be decreased when combined with Crizotinib.Approved
RotigotineThe metabolism of Rotigotine can be decreased when combined with Crizotinib.Approved
RoxithromycinThe metabolism of Roxithromycin can be decreased when combined with Crizotinib.Approved, Investigational, Withdrawn
RucaparibThe metabolism of Rucaparib can be decreased when combined with Crizotinib.Approved, Investigational
RupatadineThe metabolism of Rupatadine can be decreased when combined with Crizotinib.Approved
RuxolitinibThe metabolism of Ruxolitinib can be decreased when combined with Crizotinib.Approved
SafinamideThe metabolism of Safinamide can be decreased when combined with Crizotinib.Approved
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Crizotinib.Approved
SaquinavirThe serum concentration of Crizotinib can be increased when it is combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Crizotinib can be decreased when used in combination with Sarilumab.Approved
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Crizotinib.Approved
SelegilineThe metabolism of Selegiline can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
SelexipagThe metabolism of Selexipag can be decreased when combined with Crizotinib.Approved
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Crizotinib.Approved
SertindoleThe metabolism of Sertindole can be decreased when combined with Crizotinib.Approved, Investigational, Withdrawn
SertralineThe metabolism of Sertraline can be decreased when combined with Crizotinib.Approved
SevofluraneThe metabolism of Sevoflurane can be decreased when combined with Crizotinib.Approved, Vet Approved
SibutramineThe metabolism of Sibutramine can be decreased when combined with Crizotinib.Approved, Illicit, Investigational, Withdrawn
SildenafilThe metabolism of Crizotinib can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Crizotinib.Approved
SiltuximabThe serum concentration of Crizotinib can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Crizotinib can be increased when it is combined with Simeprevir.Approved
SimvastatinThe metabolism of Simvastatin can be decreased when combined with Crizotinib.Approved
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Crizotinib.Approved, Investigational
SitagliptinThe metabolism of Sitagliptin can be decreased when combined with Crizotinib.Approved, Investigational
SolifenacinThe metabolism of Solifenacin can be decreased when combined with Crizotinib.Approved
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Crizotinib.Approved, Investigational
SorafenibThe metabolism of Sorafenib can be decreased when combined with Crizotinib.Approved, Investigational
SpiramycinThe metabolism of Spiramycin can be decreased when combined with Crizotinib.Approved
St. John's WortThe serum concentration of Crizotinib can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Crizotinib can be increased when it is combined with Stiripentol.Approved
SufentanilThe metabolism of Sufentanil can be decreased when combined with Crizotinib.Approved, Investigational
SulfadiazineThe metabolism of Sulfadiazine can be decreased when combined with Crizotinib.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Sulfamethoxazole can be decreased when combined with Crizotinib.Approved
SulfinpyrazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Crizotinib.Approved
SulfisoxazoleThe metabolism of Crizotinib can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SunitinibThe metabolism of Sunitinib can be decreased when combined with Crizotinib.Approved, Investigational
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Crizotinib.Approved
Synthetic Conjugated Estrogens, AThe metabolism of Synthetic Conjugated Estrogens, A can be decreased when combined with Crizotinib.Approved
Synthetic Conjugated Estrogens, BThe metabolism of Synthetic Conjugated Estrogens, B can be decreased when combined with Crizotinib.Approved
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Crizotinib.Approved, Investigational
TadalafilThe metabolism of Tadalafil can be decreased when combined with Crizotinib.Approved, Investigational
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Crizotinib.Approved
TamsulosinThe metabolism of Tamsulosin can be decreased when combined with Crizotinib.Approved, Investigational
TasosartanThe metabolism of Tasosartan can be decreased when combined with Crizotinib.Approved
Taurochenodeoxycholic acidThe metabolism of Taurochenodeoxycholic acid can be decreased when combined with Crizotinib.Experimental
TelaprevirThe serum concentration of Crizotinib can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelithromycinThe serum concentration of Crizotinib can be increased when it is combined with Telithromycin.Approved
TemazepamThe metabolism of Temazepam can be decreased when combined with Crizotinib.Approved
TemsirolimusThe metabolism of Temsirolimus can be decreased when combined with Crizotinib.Approved
TeniposideThe metabolism of Teniposide can be decreased when combined with Crizotinib.Approved
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Crizotinib.Approved, Investigational, Vet Approved
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Crizotinib.Withdrawn
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Crizotinib.Experimental
TesmilifeneThe metabolism of Tesmilifene can be decreased when combined with Crizotinib.Investigational
TestosteroneThe metabolism of Testosterone can be decreased when combined with Crizotinib.Approved, Investigational
Testosterone CypionateThe metabolism of Testosterone Cypionate can be decreased when combined with Crizotinib.Approved, Investigational
Testosterone EnanthateThe metabolism of Testosterone Enanthate can be decreased when combined with Crizotinib.Approved, Investigational
Testosterone UndecanoateThe metabolism of Testosterone Undecanoate can be decreased when combined with Crizotinib.Approved, Investigational
TetracyclineThe metabolism of Tetracycline can be decreased when combined with Crizotinib.Approved, Vet Approved
TheophyllineThe metabolism of Theophylline can be decreased when combined with Crizotinib.Approved
ThiotepaThe metabolism of Thiotepa can be decreased when combined with Crizotinib.Approved
TiagabineThe metabolism of Tiagabine can be decreased when combined with Crizotinib.Approved
TicagrelorThe metabolism of Ticagrelor can be decreased when combined with Crizotinib.Approved
TiclopidineThe metabolism of Crizotinib can be decreased when combined with Ticlopidine.Approved
TinidazoleThe metabolism of Tinidazole can be decreased when combined with Crizotinib.Approved, Investigational
TiotropiumThe metabolism of Tiotropium can be decreased when combined with Crizotinib.Approved
TipranavirThe metabolism of Tipranavir can be decreased when combined with Crizotinib.Approved, Investigational
TocilizumabThe serum concentration of Crizotinib can be decreased when it is combined with Tocilizumab.Approved
TofacitinibThe metabolism of Tofacitinib can be decreased when combined with Crizotinib.Approved, Investigational
TolterodineThe metabolism of Tolterodine can be decreased when combined with Crizotinib.Approved, Investigational
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Crizotinib.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Crizotinib.Approved, Investigational
ToremifeneThe metabolism of Toremifene can be decreased when combined with Crizotinib.Approved, Investigational
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Crizotinib.Approved, Investigational
TramadolThe metabolism of Tramadol can be decreased when combined with Crizotinib.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Crizotinib.Approved, Investigational
Trastuzumab emtansineThe metabolism of Trastuzumab emtansine can be decreased when combined with Crizotinib.Approved
TrazodoneThe metabolism of Trazodone can be decreased when combined with Crizotinib.Approved, Investigational
TretinoinThe metabolism of Tretinoin can be decreased when combined with Crizotinib.Approved, Investigational, Nutraceutical
TriamcinoloneThe metabolism of Triamcinolone can be decreased when combined with Crizotinib.Approved, Vet Approved
TriazolamThe metabolism of Triazolam can be decreased when combined with Crizotinib.Approved
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Crizotinib.Approved
TrimethoprimThe metabolism of Trimethoprim can be decreased when combined with Crizotinib.Approved, Vet Approved
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Crizotinib.Approved
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Crizotinib.Investigational, Withdrawn
TroleandomycinThe metabolism of Troleandomycin can be decreased when combined with Crizotinib.Approved
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Crizotinib.Approved, Investigational, Nutraceutical
UdenafilThe metabolism of Udenafil can be decreased when combined with Crizotinib.Approved, Investigational
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Crizotinib.Approved
ValbenazineThe metabolism of Valbenazine can be decreased when combined with Crizotinib.Approved, Investigational
ValdecoxibThe metabolism of Valdecoxib can be decreased when combined with Crizotinib.Investigational, Withdrawn
Valproic AcidThe metabolism of Valproic Acid can be decreased when combined with Crizotinib.Approved, Investigational
VandetanibThe metabolism of Vandetanib can be decreased when combined with Crizotinib.Approved
VanoxerineThe metabolism of Vanoxerine can be decreased when combined with Crizotinib.Investigational
VardenafilThe metabolism of Vardenafil can be decreased when combined with Crizotinib.Approved
VelpatasvirThe metabolism of Velpatasvir can be decreased when combined with Crizotinib.Approved
VemurafenibThe serum concentration of Crizotinib can be increased when it is combined with Vemurafenib.Approved
VenetoclaxThe metabolism of Venetoclax can be decreased when combined with Crizotinib.Approved
VenlafaxineThe metabolism of Crizotinib can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Crizotinib can be decreased when combined with Verapamil.Approved
VicrivirocThe metabolism of Vicriviroc can be decreased when combined with Crizotinib.Investigational
VilanterolThe metabolism of Vilanterol can be decreased when combined with Crizotinib.Approved
VilazodoneThe serum concentration of Vilazodone can be increased when it is combined with Crizotinib.Approved
VinblastineThe metabolism of Vinblastine can be decreased when combined with Crizotinib.Approved
VincristineThe metabolism of Vincristine can be decreased when combined with Crizotinib.Approved, Investigational
VindesineThe serum concentration of Vindesine can be increased when it is combined with Crizotinib.Approved, Investigational
VinorelbineThe metabolism of Vinorelbine can be decreased when combined with Crizotinib.Approved, Investigational
VismodegibThe metabolism of Vismodegib can be decreased when combined with Crizotinib.Approved
VoriconazoleThe serum concentration of Crizotinib can be increased when it is combined with Voriconazole.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Crizotinib.Approved
VoxilaprevirThe metabolism of Voxilaprevir can be decreased when combined with Crizotinib.Approved
WarfarinThe metabolism of Warfarin can be decreased when combined with Crizotinib.Approved
YohimbineThe metabolism of Yohimbine can be decreased when combined with Crizotinib.Approved, Vet Approved
ZafirlukastThe metabolism of Zafirlukast can be decreased when combined with Crizotinib.Approved, Investigational
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Crizotinib.Approved, Investigational
ZaleplonThe metabolism of Zaleplon can be decreased when combined with Crizotinib.Approved, Illicit, Investigational
ZidovudineThe metabolism of Zidovudine can be decreased when combined with Crizotinib.Approved
ZileutonThe metabolism of Zileuton can be decreased when combined with Crizotinib.Approved, Investigational, Withdrawn
ZiprasidoneThe metabolism of Crizotinib can be decreased when combined with Ziprasidone.Approved
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Crizotinib.Approved
ZomepiracThe metabolism of Zomepirac can be decreased when combined with Crizotinib.Withdrawn
ZonisamideThe metabolism of Zonisamide can be decreased when combined with Crizotinib.Approved, Investigational
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Crizotinib.Approved
ZuclopenthixolThe serum concentration of Zuclopenthixol can be increased when it is combined with Crizotinib.Approved, Investigational
Food Interactions
  • When given with a high-fat meal, AUC and Cmax were reduced by 14%. Despite this, crizotinib may be given with or without food.

References

General References
  1. Timm A, Kolesar JM: Crizotinib for the treatment of non-small-cell lung cancer. Am J Health Syst Pharm. 2013 Jun 1;70(11):943-7. doi: 10.2146/ajhp120261. [PubMed:23686600]
  2. Forde PM, Rudin CM: Crizotinib in the treatment of non-small-cell lung cancer. Expert Opin Pharmacother. 2012 Jun;13(8):1195-201. doi: 10.1517/14656566.2012.688029. [PubMed:22594847]
External Links
KEGG Drug
D09731
PubChem Compound
11626560
PubChem Substance
310264901
ChemSpider
9801307
BindingDB
50306682
ChEBI
64310
ChEMBL
CHEMBL601719
PharmGKB
PA165946122
HET
VGH
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Crizotinib
ATC Codes
L01XE16 — Crizotinib
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
PDB Entries
2wgj / 2xp2 / 2yfx / 3zbf / 4anq / 4ans / 4c9w / 5aaa / 5aab / 5aac
FDA label
Download (279 KB)
MSDS
Download (105 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0WithdrawnTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1Active Not RecruitingTreatmentAdvanced Cancers2
1Active Not RecruitingTreatmentAdvanced Lung Cancer1
1Active Not RecruitingTreatmentAdvanced Solid Tumors1
1Active Not RecruitingTreatmentCastration-Resistant Prostate Cancer (CRPC)1
1Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1Active Not RecruitingTreatmentNeoplasms Malignant1
1Active Not RecruitingTreatmentRecurrent Childhood Anaplastic Large Cell Lymphoma / Recurrent Neuroblastoma / Unspecified Childhood Solid Tumor, Protocol Specific1
1CompletedNot AvailableHealthy Volunteers6
1CompletedBasic ScienceCancer, Advanced1
1CompletedBasic ScienceHealthy Volunteers6
1CompletedBasic ScienceImpaired Renal Function1
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
1RecruitingTreatmentALK-positive Advanced NSCLC1
1RecruitingTreatmentAdvanced Cancers1
1RecruitingTreatmentAdvanced Malignancies (Except Leukemia) / Advanced Malignancies Except Leukemia / Non-Small Cell Lung Cancer (ALK-positive) / Non-Small Cell Lung Cancer (c-Met Dependent) / Non-Small Cell Lung Cancer (ROS Marker Positive) / Non-Small Cell Lung Cancer ALK-positive / Non-Small Cell Lung Cancer c-Met Dependent / Non-Small Cell Lung Cancer ROS Marker Positive / Systemic Anaplastic Large-Cell Lymphoma1
1RecruitingTreatmentColorectal Cancers / Tumors, Solid1
1RecruitingTreatmentDiffuse Intrinsic Pontine Glioma (DIPG) / High-Grade Gliomas1
1RecruitingTreatmentGlioblastoma Multiforme (Grade IV) of Cerebellum1
1RecruitingTreatmentNeuroblastomas1
1TerminatedTreatmentAdenocarcinomas / Carcinoma, Large Cell / Non-Small Cell Lung Carcinoma (NSCLC) / Squamous Cell Carcinoma (SCC)1
1TerminatedTreatmentCancer, Breast1
1, 2Active Not RecruitingTreatmentBrain and Central Nervous System Tumors / Malignant Lymphomas / Neuroblastomas / Unspecified Childhood Solid Tumor, Protocol Specific1
1, 2Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1, 2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2Active Not RecruitingTreatmentALK-positive Non Small Cell Lung Cancer (NSCLC) and ROS1-positive NSCLC1
2Active Not RecruitingTreatmentAdenocarcinomas / Lung Cancer Non-Small Cell Cancer (NSCLC) / Lung Cancers1
2Active Not RecruitingTreatmentCrizotinib / Lung Cancer Non-Small Cell Cancer (NSCLC) / ROS1 Proto Oncogene1
2Active Not RecruitingTreatmentLocally Advanced and/or Metastatic Alveolar Rhabdomyosarcoma / Locally Advanced and/or Metastatic Alveolar Soft Part Sarcoma / Locally Advanced and/or Metastatic Anaplastic Large Cell Lymphoma / Locally Advanced and/or Metastatic Clear Cell Sarcoma / Locally Advanced and/or Metastatic Inflammatory Myofibroblastic Tumor / Locally Advanced and/or Metastatic Papillary Renal Cell Carcinoma Type 11
2Active Not RecruitingTreatmentMetastatic Cancers1
2Active Not RecruitingTreatmentStage III Non-Small Cell Lung Cancer AJCC v7 / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIA Non-Small Cell Lung Cancer AJCC v7 / Stage IIIb Non-small Cell Lung Cancer / Stage IIIB Non-Small Cell Lung Cancer AJCC v71
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentC-MET Positive Gastric Cancer1
2Not Yet RecruitingTreatmentAdvanced Solid Tumors / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)1
2Not Yet RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2RecruitingTreatmentAdenocarcinomas / Lung Cancer Non-Small Cell Cancer (NSCLC) / Squamous Cell Carcinoma (SCC)1
2RecruitingTreatmentAdvanced Malignant Neoplasm / Advanced Malignant Solid Neoplasm / Bladder Carcinoma / Carcinoma, Breast / Carcinoma, Colorectal / Carcinoma, Pancreatic / Cervical Carcinoma / Colon Carcinoma / Endometrial Carcinoma / Gastric Carcinoma / Gliomas / Head and Neck Carcinoma / Liver and Intrahepatic Bile Duct Carcinoma / Lung, Carcinoma / Malignant Lymphomas / Malignant Uterine Neoplasm / Melanoma / Oesophageal Carcinoma / Ovarian Carcinoma / Plasma Cell Myeloma / Prostate Cancer / Rectal Carcinoma / Recurrent Bladder Carcinoma / Recurrent Breast Carcinoma / Recurrent Cervical Carcinoma / Recurrent Colon Carcinoma / Recurrent Colorectal Carcinoma / Recurrent Esophageal Carcinoma / Recurrent Gastric Carcinoma / Recurrent Gliomas / Recurrent Head and Neck Carcinoma / Recurrent Liver Carcinoma / Recurrent Lung Carcinoma / Recurrent Lymphoma / Recurrent Malignant Solid Neoplasm / Recurrent Melanoma / Recurrent Ovarian Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Plasma Cell Myeloma / Recurrent Prostate Carcinoma / Recurrent Rectal Carcinoma / Recurrent Skin Carcinoma / Recurrent Solid Neoplasm / Recurrent Thyroid Gland Carcinoma / Recurrent Uterine Corpus Carcinoma / Refractory Lymphomas / Refractory Malignant Neoplasm / Refractory Malignant Solid Neoplasm / Refractory Plasma Cell Myeloma / Renal Carcinoma / Skin Carcinoma / Solid Neoplasms / Thyroid Gland Carcinoma / Uterine Corpus Cancer1
2RecruitingTreatmentAdvanced Solid Tumors / Multiple Myeloma (MM) / Non-Hodgkin's Lymphoma (NHL)1
2RecruitingTreatmentAnaplastic Large Cell Lymphoma, ALK-Positive / Lymphoma ALK+1
2RecruitingTreatmentCholangiocarcinoma of the Extrahepatic Bile Duct / Gallbladder Cancer1
2RecruitingTreatmentHematologic Cancers / Metastatic Cancers / Tumors, Solid1
2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
2RecruitingTreatmentLung adenocarcinoma metastatic1
2RecruitingTreatmentRefractory Pediatric AML / Refractory Pediatric Solid Tumors / Relapsed Pediatric AML / Relapsed Pediatric Solid Tumors1
2RecruitingTreatmentRenal Cell Carcinoma Recurrent / Stage III Renal Cell Cancer / Stage III Renal Cell Cancer AJCC v7 / Stage IV Renal Cell Cancer / Stage IV Renal Cell Cancer AJCC V7 / Type 1 Papillary Renal Cell Carcinoma / Type 2 Papillary Renal Cell Carcinoma1
2RecruitingTreatmentUreteral Neoplasms / Urethral Neoplasms / Urinary Bladder Neoplasms1
2RecruitingTreatmentUveal Melanoma1
2SuspendedTreatmentAdenocarcinoma of the Lung / Large Cell Lung Cancer / Recurrent Non-small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer1
2SuspendedTreatmentAnaplastic Large Cell Lymphoma, ALK-Positive / Ann Arbor Stage II Childhood Anaplastic Large Cell Lymphoma / Ann Arbor Stage II Noncutaneous Childhood Anaplastic Large Cell Lymphoma / Ann Arbor Stage III Childhood Anaplastic Large Cell Lymphoma / Ann Arbor Stage III Noncutaneous Childhood Anaplastic Large Cell Lymphoma / Ann Arbor Stage IV Childhood Anaplastic Large Cell Lymphoma / Ann Arbor Stage IV Noncutaneous Childhood Anaplastic Large Cell Lymphoma / CD30-Positive Neoplastic Cells Present / Stage II Childhood Anaplastic Large Cell Lymphoma / Stage III Childhood Anaplastic Large Cell Lymphoma / Stage IV Childhood Anaplastic Large Cell Lymphoma1
2WithdrawnTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3Active Not RecruitingTreatmentAdvanced Malignancies / Carcinoma NOS / Lung Cancer Non-Small Cell Cancer (NSCLC) / Lung Cancers1
3Active Not RecruitingTreatmentAnaplastic Lymphoma Kinase-positive Non-small Cell Lung Cancer1
3Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
3CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3Not Yet RecruitingTreatmentChildhood Ganglioneuroblastoma / Childhood Neuroblastoma / NMYC Gene Amplification / Recurrent Neuroblastoma1
3RecruitingTreatmentALK Gene Rearrangement / ALK Gene Translocation / ALK positive / Stage IB Non-Small Cell Lung Carcinoma / Stage IB Non-Small Cell Lung Carcinoma AJCC v7 / Stage II Non-Small Cell Lung Cancer AJCC v7 / Stage IIA Non-Small Cell Lung Carcinoma / Stage IIA Non-Small Cell Lung Carcinoma AJCC v7 / Stage IIB Non-Small Cell Lung Carcinoma / Stage IIB Non-Small Cell Lung Carcinoma AJCC v7 / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIA Non-Small Cell Lung Cancer AJCC v71
3RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
3RecruitingTreatmentNeoplasms1
4WithdrawnTreatmentSystemic Anaplastic Large-Cell Lymphoma1
Not AvailableActive Not RecruitingNot AvailableLung Cancer Non-Small Cell Cancer (NSCLC)1
Not AvailableAvailableNot AvailableNeoplasms1
Not AvailableNo Longer AvailableNot AvailableInflammatory Myofibroblastic Tumors1
Not AvailableNo Longer AvailableNot AvailableLung Cancer Non-Small Cell Cancer (NSCLC) / Neoplasms1
Not AvailableRecruitingNot AvailableLung Cancer Non-Small Cell Cancer (NSCLC)2

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
CapsuleOral200 mg
CapsuleOral200 mg/1
CapsuleOral250 mg
CapsuleOral250 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2517256No2013-04-302024-02-26Canada
CA2577937No2010-12-212025-08-15Canada
CA2578066No2011-10-112025-08-15Canada
CA2632286No2011-11-152026-11-23Canada
US7825137No2007-05-122027-05-12Us
US7858643No2009-10-082029-10-08Us
US7230098No2005-08-262025-08-26Us
US8217057No2009-11-062029-11-06Us
US8785632No2005-03-012025-03-01Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP1.83 MSDS
Predicted Properties
PropertyValueSource
Water Solubility0.00611 mg/mLALOGPS
logP3.82ALOGPS
logP3.57ChemAxon
logS-4.9ALOGPS
pKa (Strongest Basic)10.12ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area77.99 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity128.43 m3·mol-1ChemAxon
Polarizability45.44 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9721
Caco-2 permeable-0.5672
P-glycoprotein substrateSubstrate0.6938
P-glycoprotein inhibitor INon-inhibitor0.6713
P-glycoprotein inhibitor IIInhibitor0.7105
Renal organic cation transporterInhibitor0.5464
CYP450 2C9 substrateNon-substrate0.7545
CYP450 2D6 substrateNon-substrate0.7023
CYP450 3A4 substrateSubstrate0.6029
CYP450 1A2 substrateInhibitor0.6676
CYP450 2C9 inhibitorInhibitor0.5
CYP450 2D6 inhibitorNon-inhibitor0.8662
CYP450 2C19 inhibitorInhibitor0.6237
CYP450 3A4 inhibitorNon-inhibitor0.6301
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8676
Ames testNon AMES toxic0.5981
CarcinogenicityNon-carcinogens0.8018
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6581 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.643
hERG inhibition (predictor II)Inhibitor0.7877
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
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-1693800000-fc52c38f3359a378554a

Taxonomy

Description
This compound belongs to the class of organic compounds known as pyrazolylpyridines. These are compounds containing a pyrazolylpyridine skeleton, which consists of a pyrazole linked (not fused) to a pyridine by a bond.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyridines and derivatives
Sub Class
Pyrazolylpyridines
Direct Parent
Pyrazolylpyridines
Alternative Parents
Dichlorobenzenes / Alkyl aryl ethers / Aminopyridines and derivatives / Fluorobenzenes / Piperidines / Aryl chlorides / Aryl fluorides / Imidolactams / Pyrazoles / Heteroaromatic compounds
show 7 more
Substituents
3-pyrazolylpyridine / 1,3-dichlorobenzene / Alkyl aryl ether / Aminopyridine / Halobenzene / Fluorobenzene / Chlorobenzene / Aryl chloride / Aryl fluoride / Aryl halide
show 23 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
3-[1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(piperidin-4-yl)pyrazol-4-yl]pyridin-2-amine (CHEBI:64310)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Transmembrane receptor protein tyrosine kinase activity
Specific Function
Neuronal orphan receptor tyrosine kinase that is essentially and transiently expressed in specific regions of the central and peripheral nervous systems and plays an important role in the genesis a...
Gene Name
ALK
Uniprot ID
Q9UM73
Uniprot Name
ALK tyrosine kinase receptor
Molecular Weight
176440.535 Da
References
  1. Forde PM, Rudin CM: Crizotinib in the treatment of non-small-cell lung cancer. Expert Opin Pharmacother. 2012 Jun;13(8):1195-201. doi: 10.1517/14656566.2012.688029. [PubMed:22594847]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Protein tyrosine kinase activity
Specific Function
Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to hepatocyte growth factor/HGF ligand. Regulates many physiological processes including...
Gene Name
MET
Uniprot ID
P08581
Uniprot Name
Hepatocyte growth factor receptor
Molecular Weight
155540.035 Da
References
  1. Forde PM, Rudin CM: Crizotinib in the treatment of non-small-cell lung cancer. Expert Opin Pharmacother. 2012 Jun;13(8):1195-201. doi: 10.1517/14656566.2012.688029. [PubMed:22594847]
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Timm A, Kolesar JM: Crizotinib for the treatment of non-small-cell lung cancer. Am J Health Syst Pharm. 2013 Jun 1;70(11):943-7. doi: 10.2146/ajhp120261. [PubMed:23686600]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Timm A, Kolesar JM: Crizotinib for the treatment of non-small-cell lung cancer. Am J Health Syst Pharm. 2013 Jun 1;70(11):943-7. doi: 10.2146/ajhp120261. [PubMed:23686600]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Timm A, Kolesar JM: Crizotinib for the treatment of non-small-cell lung cancer. Am J Health Syst Pharm. 2013 Jun 1;70(11):943-7. doi: 10.2146/ajhp120261. [PubMed:23686600]

Drug created on March 28, 2013 11:22 / Updated on January 15, 2018 08:57