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Identification
NameCrizotinib
Accession NumberDB08865
TypeSmall Molecule
GroupsApproved
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
C-Met/Hepatocyte Growth Factor Receptor Tyrosine Kinase Inhibitor PF-02341066
C-Met/HGFR Tyrosine Kinase Inhibitor PF-02341066
Crizotinibum
MET Tyrosine Kinase Inhibitor PF-02341066
PF 2341066
PF-2341066
External Identifiers
  • PF-02341066
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Xalkoricapsule250 mg/1oralPfizer Laboratories Div Pfizer Inc2011-08-26Not applicableUs
Xalkoricapsule250 mgoralPfizer Canada Inc2012-05-10Not applicableCanada
Xalkoricapsule200 mgoralPfizer Canada Inc2012-05-10Not applicableCanada
Xalkoricapsule200 mg/1oralPfizer Laboratories Div Pfizer Inc2011-08-26Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII53AH36668S
CAS number877399-52-5
WeightAverage: 450.337
Monoisotopic: 449.11854397
Chemical FormulaC21H22Cl2FN5O
InChI KeyInChIKey=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[C@@H](OC1=CC(=CN=C1N)C1=CN(N=C1)C1CCNCC1)C1=C(Cl)C=CC(F)=C1Cl
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassPyridines and derivatives
Sub ClassPyrazolylpyridines
Direct ParentPyrazolylpyridines
Alternative Parents
Substituents
  • 3-pyrazolylpyridine
  • 1,3-dichlorobenzene
  • Halobenzene
  • Fluorobenzene
  • Chlorobenzene
  • Aminopyridine
  • 4-aminopiperidine
  • Alkyl aryl ether
  • Imidolactam
  • Benzenoid
  • Primary aromatic amine
  • Piperidine
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • Aryl chloride
  • Heteroaromatic compound
  • Pyrazole
  • Azole
  • Azacycle
  • Secondary amine
  • Ether
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organochloride
  • Organohalogen compound
  • Amine
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic 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 )
Pharmacology
IndicationCrizotinib 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.
PharmacodynamicsNot Available
Mechanism of actionCrizotinib 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.
Related Articles
AbsorptionThe 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 bindingCrizotinib 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 eliminationFollowing 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 lifePlasma 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.

ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9721
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 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Capsuleoral200 mg
Capsuleoral200 mg/1
Capsuleoral250 mg/1
Capsuleoral250 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2517256 No2013-04-302024-02-26Canada
CA2577937 No2010-12-212025-08-15Canada
CA2578066 No2011-10-112025-08-15Canada
CA2632286 No2011-11-152026-11-23Canada
US7230098 No2005-08-262025-08-26Us
US7825137 No2007-05-122027-05-12Us
US7858643 No2009-10-082029-10-08Us
US8217057 No2009-11-062029-11-06Us
US8785632 No2005-03-012025-03-01Us
Properties
StateSolid
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 RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
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
ATC CodesL01XE16
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (279 KB)
MSDSDownload (105 KB)
Interactions
Drug Interactions
Drug
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Crizotinib.
AlfentanilThe serum concentration of Alfentanil can be increased when it is combined with Crizotinib.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Crizotinib.
AprepitantThe serum concentration of Crizotinib can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Crizotinib.
AtazanavirThe serum concentration of Crizotinib can be increased when it is combined with Atazanavir.
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Crizotinib.
BexaroteneThe serum concentration of Crizotinib can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Crizotinib can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Crizotinib can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Crizotinib.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Crizotinib.
BretyliumBretylium may increase the bradycardic activities of Crizotinib.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Crizotinib.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Crizotinib.
BupropionThe serum concentration of Bupropion can be increased when it is combined with Crizotinib.
CarbamazepineThe serum concentration of Crizotinib can be decreased when it is combined with Carbamazepine.
CeritinibCrizotinib may increase the bradycardic activities of Ceritinib.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Crizotinib.
CitalopramCrizotinib may increase the QTc-prolonging activities of Citalopram.
ClarithromycinThe serum concentration of Crizotinib can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Crizotinib can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Crizotinib.
ConivaptanThe serum concentration of Crizotinib can be increased when it is combined with Conivaptan.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Crizotinib.
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Crizotinib.
DabrafenibThe serum concentration of Crizotinib can be decreased when it is combined with Dabrafenib.
DapoxetineThe serum concentration of Dapoxetine can be increased when it is combined with Crizotinib.
DarunavirThe serum concentration of Crizotinib can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Crizotinib can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Crizotinib can be decreased when it is combined with Deferasirox.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Crizotinib.
DofetilideCrizotinib may increase the QTc-prolonging activities of Dofetilide.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Crizotinib.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Crizotinib.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Crizotinib.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Crizotinib.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Crizotinib.
EnzalutamideThe serum concentration of Crizotinib can be decreased when it is combined with Enzalutamide.
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Crizotinib.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Crizotinib.
EsmololEsmolol may increase the bradycardic activities of Crizotinib.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Crizotinib.
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Crizotinib.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Crizotinib.
FluconazoleThe metabolism of Crizotinib can be decreased when combined with Fluconazole.
FlunisolideThe metabolism of Flunisolide can be decreased when combined with Crizotinib.
FosaprepitantThe serum concentration of Crizotinib can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Crizotinib can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Crizotinib can be increased when it is combined with Fusidic Acid.
GoserelinGoserelin may increase the QTc-prolonging activities of Crizotinib.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Crizotinib.
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Crizotinib.
IdelalisibThe serum concentration of Crizotinib can be increased when it is combined with Idelalisib.
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.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Crizotinib.
IndinavirThe serum concentration of Crizotinib can be increased when it is combined with Indinavir.
ItraconazoleThe serum concentration of Crizotinib can be increased when it is combined with Itraconazole.
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Crizotinib.
IvacaftorThe serum concentration of Ivacaftor can be increased when it is combined with Crizotinib.
KetoconazoleThe serum concentration of Crizotinib can be increased when it is combined with Ketoconazole.
LacosamideCrizotinib may increase the atrioventricular blocking (AV block) activities of Lacosamide.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Crizotinib.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Crizotinib.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Crizotinib.
LuliconazoleThe serum concentration of Crizotinib can be increased when it is combined with Luliconazole.
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Crizotinib.
MethadoneThe metabolism of Methadone can be decreased when combined with Crizotinib.
MifepristoneMifepristone may increase the QTc-prolonging activities of Crizotinib.
MitotaneThe serum concentration of Crizotinib can be decreased when it is combined with Mitotane.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Crizotinib.
NefazodoneThe serum concentration of Crizotinib can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Crizotinib can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Crizotinib can be increased when it is combined with Netupitant.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Crizotinib.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Crizotinib.
OctreotideOctreotide may increase the bradycardic activities of Crizotinib.
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Crizotinib.
OxycodoneThe risk or severity of adverse effects can be increased when Crizotinib is combined with Oxycodone.
PalbociclibThe serum concentration of Crizotinib can be increased when it is combined with Palbociclib.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Crizotinib.
PhenobarbitalThe serum concentration of Crizotinib can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Crizotinib can be decreased when it is combined with Phenytoin.
PimecrolimusThe metabolism of Pimecrolimus can be decreased when combined with Crizotinib.
PimozideCrizotinib may increase the QTc-prolonging activities of Pimozide.
PosaconazoleThe serum concentration of Crizotinib can be increased when it is combined with Posaconazole.
PrimidoneThe serum concentration of Crizotinib can be decreased when it is combined with Primidone.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Crizotinib.
QuinidineCrizotinib may increase the QTc-prolonging activities of Quinidine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Crizotinib.
RifabutinThe serum concentration of Crizotinib can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Crizotinib can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Crizotinib can be decreased when it is combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Crizotinib.
RitonavirThe serum concentration of Crizotinib can be increased when it is combined with Ritonavir.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Crizotinib.
RuxolitinibRuxolitinib may increase the bradycardic activities of Crizotinib.
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Crizotinib.
SaquinavirThe serum concentration of Crizotinib can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Crizotinib.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Crizotinib.
SiltuximabThe serum concentration of Crizotinib can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Crizotinib.
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Crizotinib.
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Crizotinib.
St. John's WortThe serum concentration of Crizotinib can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Crizotinib can be increased when it is combined with Stiripentol.
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Crizotinib.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Crizotinib.
TelaprevirThe serum concentration of Crizotinib can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Crizotinib can be increased when it is combined with Telithromycin.
TesmilifeneThe serum concentration of Crizotinib can be decreased when it is combined with Tesmilifene.
TocilizumabThe serum concentration of Crizotinib can be decreased when it is combined with Tocilizumab.
TofacitinibTofacitinib may increase the bradycardic activities of Crizotinib.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Crizotinib.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Crizotinib.
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Crizotinib.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Crizotinib.
VerapamilThe serum concentration of Crizotinib can be increased when it is combined with Verapamil.
VilazodoneThe serum concentration of Vilazodone can be increased when it is combined with Crizotinib.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Crizotinib.
VindesineThe serum concentration of Vindesine can be increased when it is combined with Crizotinib.
VoriconazoleThe serum concentration of Crizotinib can be increased when it is combined with Voriconazole.
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Crizotinib.
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.

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 and differentiation of the nervous system. Transduces signals from ligands at the cell surface, through specific activation of the mitogen-activated protein kinase (MAPK) pathway. Phosphorylates almost...
Gene Name:
ALK
Uniprot ID:
Q9UM73
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 proliferation, scattering, morphogenesis and survival. Ligand binding at the cell surface induces autophosphorylation of MET on its intracellular domain that provides docking sites for downstream sig...
Gene Name:
MET
Uniprot ID:
P08581
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 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. 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
substrateinhibitor
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. 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 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. 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 ]
Comments
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Drug created on March 28, 2013 11:22 / Updated on August 24, 2016 01:52