U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C22H18N4OS
Molecular Weight 386.4714
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of AXITINIB

SMILES

CN=C(c1ccccc1Sc2ccc3c(/C(/[H])=C(\[H])/c4ccccn4)[nH]nc3c2)O

InChI

InChIKey=RITAVMQDGBJQJZ-FMIVXFBMSA-N
InChI=1S/C22H18N4OS/c1-23-22(27)18-7-2-3-8-21(18)28-16-10-11-17-19(25-26-20(17)14-16)12-9-15-6-4-5-13-24-15/h2-14H,1H3,(H,23,27)(H,25,26)/b12-9+

HIDE SMILES / InChI

Molecular Formula C22H18N4OS
Molecular Weight 386.4714
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Description
Curator's Comment:: http://www.drugdevelopment-technology.com/projects/axitinib-carcinoma/; http://www.ncbi.nlm.nih.gov/pubmed/18541897; https://www.ncbi.nlm.nih.gov/pubmed/?term=19010843

Axitinib (trade name Inlyta) is a small molecule tyrosine kinase inhibitor developed by Pfizer. It has been shown to significantly inhibit growth of breast cancer in animal (xenograft) models and has shown partial responses in clinical trials with renal cell carcinoma (RCC) and several other tumour types. Axitinib has been shown to inhibit receptor tyrosine kinases including vascular endothelial growth factor receptors (VEGFR)-1, VEGFR-2, and VEGFR-3 at therapeutic plasma concentrations. These receptors are implicated in pathologic angiogenesis, tumor growth, and cancer progression. VEGF-mediated endothelial cell proliferation and survival were inhibited by axitinib in vitro and in mouse models. It was approved by the U.S. Food and Drug Administration.

CNS Activity

Curator's Comment:: Mouse whole-body autoradiography revealed that [(14)C]axitinib-equivalents showed rapid absorption and distribution to all tissues except the brain. This suggests that efflux transport of axitinib may occur at the mouse blood-brain barrier

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P17948|||B3FR89
Gene ID: 2321
Gene Symbol: FLT1
Target Organism: Homo sapiens (Human)
0.100000000000000006 nM [IC50]
Target ID: P35968
Gene ID: 3791
Gene Symbol: KDR
Target Organism: Homo sapiens (Human)
0.200000000000000011 nM [IC50]
Target ID: P35916
Gene ID: 2324
Gene Symbol: FLT4
Target Organism: Homo sapiens (Human)
0.299999999999999989 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
INLYTA

Approved Use

Indicated for the treatment of advanced renal cell carcinoma (RCC) after failure of one prior systemic therapy.

Launch Date

1327622400000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
32.2 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
28.8 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: HIGH-FAT
52.7 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
51.1 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
162 ng/mL
20 mg 2 times / day steady-state, oral
dose: 20 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AXITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
27.8 ng/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
82 ng/mL
15 mg 1 times / day steady-state, oral
dose: 15 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AXITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
27.8 ng/mL
5 mg 2 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AXITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
160.3 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
162 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: HIGH-FAT
206.8 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
187 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
2171 ng × h/mL
20 mg 2 times / day steady-state, oral
dose: 20 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AXITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
265 ng × h/mL
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
717 μg × h/mL
15 mg 1 times / day steady-state, oral
dose: 15 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AXITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
265 ng × h/mL
5 mg 2 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AXITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.4 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FED
3 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: HIGH-FAT
7 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB blood
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
9.4 h
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
4.8 h
20 mg 2 times / day steady-state, oral
dose: 20 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AXITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
4.6 h
15 mg 1 times / day steady-state, oral
dose: 15 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AXITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
5 mg single, oral
dose: 5 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
AXITINIB plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
1%
5 mg 2 times / day steady-state, oral
dose: 5 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
AXITINIB unknown
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FED
Doses

Doses

DosePopulationAdverse events​
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Disc. AE: Disease progression, Fatigue...
AEs leading to
discontinuation/dose reduction:
Disease progression (11 patient)
Fatigue (4 patients)
Transient ischemic attack (3 patients)
Asthenia (2 patients)
Pleural effusion (2 patients)
Decreased appetite (2 patients)
Palmar-plantar erythrodysaesthesia syndrome (1 patient)
Dyspnea (1 patient)
Anemia (1 patient)
Vomiting (1 patient)
Retinal vein thrombosis (1 patient)
Ascites (1 patient)
Blood creatinine increased (1 patient)
Hypoglycemia (1 patient)
Altered state of consciousness (1 patient)
Cerebral hemorrhage (1 patient)
Dyspnea exertional (1 patient)
Pneumothorax (1 patient)
Hypertension (1 patient)
Sources:
30 mg 2 times / day steady, oral
Highest studied dose
Dose: 30 mg, 2 times / day
Route: oral
Route: steady
Dose: 30 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
5 mg 2 times / day steady, oral
MTD
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
DLT: Stomatitis...
Dose limiting toxicities:
Stomatitis (1 patient)
Sources:
15 mg 1 times / day steady, oral
Dose: 15 mg, 1 times / day
Route: oral
Route: steady
Dose: 15 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
DLT: Hypertension, Stomatitis...
Dose limiting toxicities:
Hypertension (1 patient)
Stomatitis (1 patient)
Pancreatitis (1 patient)
Bowel ischemia (1 patient)
Thromboembolism (1 patient)
Sources:
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
DLT: Hypertension, Hemoptysis...
Dose limiting toxicities:
Hypertension (2 patients)
Hemoptysis (1 patient)
Stomatitis (1 patient)
Sources:
AEs

AEs

AESignificanceDosePopulation
Altered state of consciousness 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Anemia 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Ascites 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Blood creatinine increased 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Cerebral hemorrhage 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Dyspnea exertional 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Dyspnea 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Hypertension 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Hypoglycemia 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Palmar-plantar erythrodysaesthesia syndrome 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Pneumothorax 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Retinal vein thrombosis 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Vomiting 1 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Disease progression 11 patient
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Asthenia 2 patients
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Decreased appetite 2 patients
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Pleural effusion 2 patients
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Transient ischemic attack 3 patients
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Fatigue 4 patients
Disc. AE
5 mg 2 times / day steady, oral
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy, 62 years (range: 20-82 years)
Health Status: unhealthy
Age Group: 62 years (range: 20-82 years)
Sex: M+F
Sources:
Stomatitis 1 patient
DLT
5 mg 2 times / day steady, oral
MTD
Dose: 5 mg, 2 times / day
Route: oral
Route: steady
Dose: 5 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Bowel ischemia 1 patient
DLT
15 mg 1 times / day steady, oral
Dose: 15 mg, 1 times / day
Route: oral
Route: steady
Dose: 15 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Hypertension 1 patient
DLT
15 mg 1 times / day steady, oral
Dose: 15 mg, 1 times / day
Route: oral
Route: steady
Dose: 15 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Pancreatitis 1 patient
DLT
15 mg 1 times / day steady, oral
Dose: 15 mg, 1 times / day
Route: oral
Route: steady
Dose: 15 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Stomatitis 1 patient
DLT
15 mg 1 times / day steady, oral
Dose: 15 mg, 1 times / day
Route: oral
Route: steady
Dose: 15 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Thromboembolism 1 patient
DLT
15 mg 1 times / day steady, oral
Dose: 15 mg, 1 times / day
Route: oral
Route: steady
Dose: 15 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Hemoptysis 1 patient
DLT
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Stomatitis 1 patient
DLT
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Hypertension 2 patients
DLT
20 mg 2 times / day steady, oral
Dose: 20 mg, 2 times / day
Route: oral
Route: steady
Dose: 20 mg, 2 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
yes [IC50 4.5 uM]
yes [Ki 0.5 uM]
no (co-administration study)
Comment: axitinib has no effect on exposure of paclitaxel
yes [Ki 0.7 uM]
yes [Ki 52.2 uM]
yes [Ki 8.3 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
yes (co-administration study)
Comment: ketoconazole increased cmax of axitinib by by 50%, auc by 106%
major
yes (co-administration study)
Comment: ketoconazole increased cmax of axitinib by by 50%, auc by 106%
minor
minor
no (pharmacogenomic study)
Comment: no clinical effect was observed in genotyping study
minor
no (pharmacogenomic study)
Comment: no clinical effect was observed in genotyping study
no
no
no
no
no
no
no
no
no
no
no
yes
yes
yes
yes
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Phase II study of axitinib in sorafenib-refractory metastatic renal cell carcinoma.
2009 Sep 20
Comprehensive analysis of kinase inhibitor selectivity.
2011 Oct 30
Evaluation of drugs with specific organ toxicities in organ-specific cell lines.
2012 Mar
Patents

Sample Use Guides

5 mg orally twice daily
Route of Administration: Oral
Transfected or endogenous RTK-expressing cells were treated by axitinib with range of concentration from 0.01 nM to 10 uM. In transfected or endogenous RTK-expressing cells, axitinib potently blocked growth factor-stimulated phosphorylation of VEGFR-2 and VEGFR-3 with average IC50 values of 0.2 and 0.1 to 0.3 nmol/L, respectively. Cellular activity against VEGFR-1 was 1.2 nmol/L.
Substance Class Chemical
Created
by admin
on Fri Jun 25 22:12:45 UTC 2021
Edited
by admin
on Fri Jun 25 22:12:45 UTC 2021
Record UNII
C9LVQ0YUXG
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
AXITINIB
DASH   INN   JAN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
N-METHYL-2-(3-((E)-2-PYRIDIN-2-YL-VINYL)-1H-INDAZOL-6-YLSULFANYL)-BENZAMIDE
Systematic Name English
AXITINIB [VANDF]
Common Name English
AG-013736
Code English
AXITINIB [ORANGE BOOK]
Common Name English
AXITINIB [MI]
Common Name English
AXITINIB [INN]
Common Name English
NSC-757441
Code English
AG-13736
Code English
AXITINIB [MART.]
Common Name English
BENZAMIDE, N-METHYL-2-((3-((1E)-2-(2-PYRIDINYL)ETHENYL)-1H-INDAZOL-6-YL)THIO)-
Systematic Name English
AXITINIB [WHO-DD]
Common Name English
AXITINIB [JAN]
Common Name English
INLYTA
Brand Name English
N-METHYL-2((3-((1E0-2-(PYRIDIN-2-YL)ETHENYL)-1H-INAZOL-6-YLSUFANYL)BENZAMIDE
Common Name English
AXITINIB [USAN]
Common Name English
Classification Tree Code System Code
WHO-ATC L01XE17
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
NCI_THESAURUS C1742
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
EMA ASSESSMENT REPORTS INLYTA (AUTHORIZED: CARCINOMA, CANCER CELL)
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
FDA ORPHAN DRUG 730120
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
WHO-VATC QL01XE17
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
NCI_THESAURUS C93259
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
NDF-RT N0000175605
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
NCI_THESAURUS C129825
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
FDA ORPHAN DRUG 230706
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
EU-Orphan Drug EU/3/10/844
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
LIVERTOX 79
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
FDA ORPHAN DRUG 240607
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
Code System Code Type Description
DRUG CENTRAL
4225
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
RXCUI
1242999
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY RxNorm
EPA CompTox
319460-85-0
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
MESH
C503983
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
LACTMED
Axitinib
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
PUBCHEM
6450551
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
MERCK INDEX
M2153
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY Merck Index
FDA UNII
C9LVQ0YUXG
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
EVMPD
SUB25427
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
ChEMBL
CHEMBL1289926
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
NDF-RT
N0000020000
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY Receptor Tyrosine Kinase Inhibitors [MoA]
IUPHAR
5659
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
INN
8720
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
DRUG BANK
DB06626
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
NCI_THESAURUS
C38718
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
CAS
319460-85-0
Created by admin on Fri Jun 25 22:12:45 UTC 2021 , Edited by admin on Fri Jun 25 22:12:45 UTC 2021
PRIMARY
Related Record Type Details
BINDER->LIGAND
BINDING
TARGET -> INHIBITOR
TARGET -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TARGET -> INHIBITOR
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TARGET -> INHIBITOR
Related Record Type Details
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
URINE
METABOLITE INACTIVE -> PARENT
MAJOR
PLASMA
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC