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Details

Stereochemistry ABSOLUTE
Molecular Formula C21H22Cl2FN5O
Molecular Weight 450.3373
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of CRIZOTINIB

SMILES

C[C@]([H])(c1c(ccc(c1Cl)F)Cl)Oc2cc(cnc2N)-c3cnn(c3)C4CCNCC4

InChI

InChIKey=KTEIFNKAUNYNJU-GFCCVEGCSA-N
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

HIDE SMILES / InChI

Molecular Formula C21H22Cl2FN5O
Molecular Weight 450.3373
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment:: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/202570s006lbl.pdf; https://www.mskcc.org/cancer-care/clinical-trials/14-063

Crizotinib (trade name Xalkori, Pfizer, Inc.) is an anti cancer drug approved for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test. Crizotinib is an inhibitor of receptor tyrosine kinases including ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), ROS1 (c-ros), and Recepteur d’Origine Nantais (RON). Common adverse reactions in clinical trials with crizotinib, occurring at an incidence of 25% or higher, included visual disorders, nausea, diarrhea, vomiting, constipation, edema, elevated transaminases, and fatigue. Crizotinib is currently under investigational study for use in treatment of Uveal Melanoma.

CNS Activity

Curator's Comment:: The CNS is frequently a site of disease progression, where up to 60% of patients develop metastases during treatment with crizotinib.The most likely reason for such isolated CNS failure is incomplete penetration of the blood-brain barrier by crizotinib.

Originator

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
24.0 nM [IC50]
11.0 nM [IC50]
Target ID: P36639
Gene ID: 4521.0
Gene Symbol: NUDT1
Target Organism: Homo sapiens (Human)
72.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
XALKORI

Approved Use

Indicated for the treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test.

Launch Date

1.31431675E12
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
475 ng/mL
300 mg 2 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CRIZOTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
99.6 ng/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CRIZOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
328 ng/mL
250 mg 2 times / day steady-state, oral
dose: 250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CRIZOTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
327 ng/mL
250 mg 2 times / day multiple, oral
dose: 250 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CRIZOTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
87 ng/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CRIZOTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
3240 ng × h/mL
300 mg 2 times / day steady-state, oral
dose: 300 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CRIZOTINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
2321 ng × h/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CRIZOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
3054 ng × h/mL
250 mg 2 times / day steady-state, oral
dose: 250 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
CRIZOTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3084 ng × h/mL
250 mg 2 times / day multiple, oral
dose: 250 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
CRIZOTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
1817 ng × h/mL
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CRIZOTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
29 h
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CRIZOTINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
47.1 h
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CRIZOTINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
9.3%
CRIZOTINIB plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
300 mg 2 times / day steady, oral
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy, 49 years
n = 6
Health Status: unhealthy
Age Group: 49 years
Sex: M+F
Population Size: 6
Sources:
Disc. AE: Fatigue...
AEs leading to
discontinuation/dose reduction:
Fatigue (grade 3, 1 patient)
Sources:
250 mg 2 times / day steady, oral
Recommended|MTD
Dose: 250 mg, 2 times / day
Route: oral
Route: steady
Dose: 250 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21-79 years)
n = 119
Health Status: unhealthy
Condition: Adenocarcinoma | Squamous Cell Carcinoma |Non-small Cell Lung Cancer
Age Group: 51 years (range: 21-79 years)
Sex: M+F
Population Size: 119
Sources:
Disc. AE: Autoimmune thyroiditis...
AEs leading to
discontinuation/dose reduction:
Autoimmune thyroiditis (1 patient)
Sources:
250 mg 2 times / day steady, oral
Recommended|MTD
Dose: 250 mg, 2 times / day
Route: oral
Route: steady
Dose: 250 mg, 2 times / day
Sources:
unhealthy, 52 years (range: 29-82 years)
n = 136
Health Status: unhealthy
Condition: Adenocarcinoma | Adenosquamous Carcinoma|Non-small Cell Lung Cancer
Age Group: 52 years (range: 29-82 years)
Sex: M+F
Population Size: 136
Sources:
Disc. AE: ALT increased, Pneumonitis...
AEs leading to
discontinuation/dose reduction:
ALT increased (2.2%)
Pneumonitis (1.5%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Fatigue grade 3, 1 patient
Disc. AE
300 mg 2 times / day steady, oral
Dose: 300 mg, 2 times / day
Route: oral
Route: steady
Dose: 300 mg, 2 times / day
Sources:
unhealthy, 49 years
n = 6
Health Status: unhealthy
Age Group: 49 years
Sex: M+F
Population Size: 6
Sources:
Autoimmune thyroiditis 1 patient
Disc. AE
250 mg 2 times / day steady, oral
Recommended|MTD
Dose: 250 mg, 2 times / day
Route: oral
Route: steady
Dose: 250 mg, 2 times / day
Sources:
unhealthy, 51 years (range: 21-79 years)
n = 119
Health Status: unhealthy
Condition: Adenocarcinoma | Squamous Cell Carcinoma |Non-small Cell Lung Cancer
Age Group: 51 years (range: 21-79 years)
Sex: M+F
Population Size: 119
Sources:
Pneumonitis 1.5%
Disc. AE
250 mg 2 times / day steady, oral
Recommended|MTD
Dose: 250 mg, 2 times / day
Route: oral
Route: steady
Dose: 250 mg, 2 times / day
Sources:
unhealthy, 52 years (range: 29-82 years)
n = 136
Health Status: unhealthy
Condition: Adenocarcinoma | Adenosquamous Carcinoma|Non-small Cell Lung Cancer
Age Group: 52 years (range: 29-82 years)
Sex: M+F
Population Size: 136
Sources:
ALT increased 2.2%
Disc. AE
250 mg 2 times / day steady, oral
Recommended|MTD
Dose: 250 mg, 2 times / day
Route: oral
Route: steady
Dose: 250 mg, 2 times / day
Sources:
unhealthy, 52 years (range: 29-82 years)
n = 136
Health Status: unhealthy
Condition: Adenocarcinoma | Adenosquamous Carcinoma|Non-small Cell Lung Cancer
Age Group: 52 years (range: 29-82 years)
Sex: M+F
Population Size: 136
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
weak [IC50 44 uM]
weak [IC50 48 uM]
weak [Inhibition 30 uM]
yes [IC50 0.83 uM]
yes [IC50 14.6 uM]
yes [IC50 22 uM]
yes [IC50 23 uM]
yes [IC50 5.79 uM]
yes [IC50 7.3 uM]
yes (co-administration study)
Comment: crizotinib increased AUC of midazolam by 3.7x
yes [IC50 >30 uM]
yes [IC50 >30 uM]
yes [IC50 >30 uM]
yes [IC50 >30 uM]
yes
no (co-administration study)
Drug as victimTox targets
PubMed

PubMed

TitleDatePubMed
[Following communications made at American Society of Clinical Oncology 2010, what will change our practice? The point of view of the editorial board of Bulletin du Cancer].
2010 Dec
Crizotinib, a small-molecule dual inhibitor of the c-Met and ALK receptor tyrosine kinases.
2010 Dec
New drugs in advanced non-small-cell lung cancer: searching for the correct clinical development.
2010 Dec
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.
2010 Nov 24
Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.
2011 Apr 14
Favorable response to crizotinib in three patients with echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase fusion-type oncogene-positive non-small cell lung cancer.
2011 Aug
Differential (18)F-FDG and 3'-deoxy-3'-(18)F-fluorothymidine PET responses to pharmacologic inhibition of the c-MET receptor in preclinical tumor models.
2011 Aug
Activating ALK mutations found in neuroblastoma are inhibited by Crizotinib and NVP-TAE684.
2011 Dec 15
MET amplification identifies a small and aggressive subgroup of esophagogastric adenocarcinoma with evidence of responsiveness to crizotinib.
2011 Dec 20
Genotype-driven therapies for non-small cell lung cancer: focus on EGFR, KRAS and ALK gene abnormalities.
2011 May
Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK.
2011 May 3
MET tyrosine kinase inhibitor crizotinib (PF-02341066) shows differential antitumor effects in non-small cell lung cancer according to MET alterations.
2011 Oct
Comprehensive analysis of kinase inhibitor selectivity.
2011 Oct 30
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.
2011 Sep 22
Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).
2011 Sep 22
Echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase-targeted therapy for advanced non-small cell lung cancer: molecular and clinical aspects.
2012 Aug
Adenocarcinoma of the lung with miliary brain and pulmonary metastases with echinoderm microtubule-associated protein like 4-anaplastic lymphoma kinase translocation treated with crizotinib: a case report.
2012 Dec
Isolated central nervous system progression on Crizotinib: an Achilles heel of non-small cell lung cancer with EML4-ALK translocation?
2012 Dec
Antitumor action of the MET tyrosine kinase inhibitor crizotinib (PF-02341066) in gastric cancer positive for MET amplification.
2012 Jul
Autocrine activation of the MET receptor tyrosine kinase in acute myeloid leukemia.
2012 Jul
Preclinical rationale for use of the clinically available multitargeted tyrosine kinase inhibitor crizotinib in ROS1-translocated lung cancer.
2012 Jul
Crizotinib (PF-02341066) reverses multidrug resistance in cancer cells by inhibiting the function of P-glycoprotein.
2012 Jul
Paracrine receptor activation by microenvironment triggers bypass survival signals and ALK inhibitor resistance in EML4-ALK lung cancer cells.
2012 Jul 1
The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma.
2012 Jul 10
[Management of crizotinib, a new individualized treatment].
2012 Jul-Aug
Crizotinib in the treatment of non-small-cell lung cancer.
2012 Jun
Development of treatment strategies for advanced neuroblastoma.
2012 Jun
Remarkable tumor response to crizotinib in a 14-year-old girl with ALK-positive non-small-cell lung cancer.
2012 Jun 1
A molecular dynamics investigation on the crizotinib resistance mechanism of C1156Y mutation in ALK.
2012 Jun 29
Mechanisms of resistance to crizotinib in patients with ALK gene rearranged non-small cell lung cancer.
2012 Mar 1
ROS1 rearrangements define a unique molecular class of lung cancers.
2012 Mar 10
Targeted therapy for lung cancer.
2012 Nov
Antibody targeting of anaplastic lymphoma kinase induces cytotoxicity of human neuroblastoma.
2012 Nov 15
Treatment of ALK-positive non-small cell lung cancer.
2012 Oct
Activity and safety of crizotinib in patients with ALK-positive non-small-cell lung cancer: updated results from a phase 1 study.
2012 Oct
[Cavitating nodules in a 40-year-old non-smoking woman: a very particular tumour].
2012 Sep
Targeting ALK: a promising strategy for the treatment of non-small cell lung cancer, non-Hodgkin's lymphoma, and neuroblastoma.
2012 Sep
Identifying and targeting ROS1 gene fusions in non-small cell lung cancer.
2012 Sep 1
Differential protein stability and ALK inhibitor sensitivity of EML4-ALK fusion variants.
2012 Sep 1
Enhancement of the antiproliferative activity of gemcitabine by modulation of c-Met pathway in pancreatic cancer.
2013
Development and validation of a high-throughput intrinsic ATPase activity assay for the discovery of MEKK2 inhibitors.
2013 Apr
Prediction of crizotinib-midazolam interaction using the Simcyp population-based simulator: comparison of CYP3A time-dependent inhibition between human liver microsomes versus hepatocytes.
2013 Feb
Overcoming erlotinib resistance with tailored treatment regimen in patient-derived xenografts from naïve Asian NSCLC patients.
2013 Jan 15
Crizotinib for the treatment of non-small-cell lung cancer.
2013 Jun 1
Cell culture and Drosophila model systems define three classes of anaplastic lymphoma kinase mutations in neuroblastoma.
2013 Mar
Targeted agents in the third-/fourth-line treatment of patients with advanced (stage III/IV) non-small cell lung cancer (NSCLC).
2013 May
Multi-parameter in vitro toxicity testing of crizotinib, sunitinib, erlotinib, and nilotinib in human cardiomyocytes.
2013 Oct 1
Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy.
2014 Apr 10
Elucidating mechanisms of toxicity using phenotypic data from primary human cell systems--a chemical biology approach for thrombosis-related side effects.
2015 Jan 5
Patents

Sample Use Guides

mouse xenograft: (S)-crizotinib 50mg/kg p.o., q.d (1 tablet by mouth once a day) was administered for 26 days
Route of Administration: Oral
(S)-crizotinib (in concentrations: 500 nM, 2 uM and 5 uM) efficiently inhibited colony formation of SW480 and KRAS mutated PANC1 (human pancreatic carcinoma) cells. In vitro Kd measurements indicated that (S)-crizotinib was considerably less potent than the (R)-enantiomer against the established targets ALK, MET and ROS1.
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:49:17 UTC 2021
Edited
by admin
on Fri Jun 25 21:49:17 UTC 2021
Record UNII
53AH36668S
Record Status Validated (UNII)
Record Version
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Name Type Language
CRIZOTINIB
DASH   INN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
INN   USAN  
Official Name English
CRIZOTINIB [USAN]
Common Name English
CRIZOTINIB [JAN]
Common Name English
CRIZOTINIB [ORANGE BOOK]
Common Name English
CRIZOTINIB [MI]
Common Name English
(R)-3-(1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY)-5-(1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL)PYRIDIN-2-AMINE
Systematic Name English
PF-02341066
Code English
CRIZOTINIB [WHO-DD]
Common Name English
2-PYRIDINAMINE, 3-((1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY)-5-(1-(4-PIPERIDINYL)-1H-PYRAZOL-4-YL)-
Systematic Name English
NSC-756645
Code English
3-((1R)-1-(2,6-DICHLORO-3-FLUOROPHENYL)ETHOXY)-5-(1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL)PYRIDIN-2-AMINE
Systematic Name English
CRIZOTINIB [MART.]
Common Name English
CRIZOTINIB [VANDF]
Common Name English
1066
Code English
PF-2341066
Common Name English
XALKORI
Brand Name English
CRIZOTINIB [INN]
Common Name English
Classification Tree Code System Code
WHO-VATC QL01XE16
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
FDA ORPHAN DRUG 379812
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
WHO-ATC L01XE16
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
FDA ORPHAN DRUG 310610
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
FDA ORPHAN DRUG 379712
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
NDF-RT N0000175605
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
NCI_THESAURUS C141136
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
LIVERTOX 241
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
NCI_THESAURUS C129825
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
Code System Code Type Description
MERCK INDEX
M3847
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY Merck Index
DRUG BANK
DB08865
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
ChEMBL
CHEMBL601719
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
NDF-RT
N0000182139
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY Cytochrome P450 2B6 Inhibitors [MoA]
IUPHAR
4903
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
CAS
877399-52-5
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
NDF-RT
N0000185503
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY P-Glycoprotein Inhibitors [MoA]
LACTMED
Crizotinib
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
EVMPD
SUB32267
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
NDF-RT
N0000190114
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY Cytochrome P450 3A Inhibitors [MoA]
JAPANESE REVIEW
XALKORI
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY APPROVED MARCH 2012
INN
9301
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
NDF-RT
N0000191265
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY Organic Cation Transporter 1 Inhibitors [MoA]
NDF-RT
N0000187061
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY Organic Cation Transporter 2 Inhibitors [MoA]
NCI_THESAURUS
C74061
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
MESH
C551994
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
NDF-RT
N0000020000
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY Receptor Tyrosine Kinase Inhibitors [MoA]
PUBCHEM
11626560
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
RXCUI
1148495
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY RxNorm
DRUG CENTRAL
4187
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
FDA UNII
53AH36668S
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
WIKIPEDIA
CRIZOTINIB
Created by admin on Fri Jun 25 21:49:17 UTC 2021 , Edited by admin on Fri Jun 25 21:49:17 UTC 2021
PRIMARY
Related Record Type Details
TRANSPORTER -> INHIBITOR
TRANSPORTER -> SUBSTRATE
EXCRETED UNCHANGED
URINE
EXCRETED UNCHANGED
FECAL
TRANSPORTER -> SUBSTRATE
Crizotinib is a substrate for P-glycoprotein in vitro.
TARGET -> INHIBITOR
In vitro studies in human liver microsomes demonstrated that crizotinib is a time-dependent inhibitor of CYP3A.
INHIBITOR
IC50
BINDER->LIGAND
Binding of crizotinib to human plasma proteins in vitro is 91% and is independent of drug concentration.
TARGET -> INHIBITOR
INHIBITOR
IC50
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
ORAL BIOAVAILABILITY PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC DOSE

INTRAVENOUS ADMINISTRATION

Biological Half-life PHARMACOKINETIC SINGLE-DOSE ADMINISTRATION

Tmax PHARMACOKINETIC ORAL SINGLE-DOSE ADMINISTRATION

CSF/PLASMA RATIO PHARMACOKINETIC COMMENT
PHARMACOKINETIC