AXITINIB

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H18N4OS
Molecular Weight	386.47
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(\C=C\C4=CC=CC=N4)=NN3

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	386.47
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202324lbl.pdf
Curator's Comment: description was created based on several sources, including 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

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Vascular endothelial growth factor receptor 1 39 Target ID: P17948\|\|\|B3FR89 Gene ID: 2321.0 Gene Symbol: FLT1 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=19010843	Inhibitor 8146	0.1 nM [IC50]
Vascular endothelial growth factor receptor 2 100 Target ID: P35968 Gene ID: 3791.0 Gene Symbol: KDR Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=19010843	Inhibitor 8146	0.2 nM [IC50]
Vascular endothelial growth factor receptor 3 39 Target ID: P35916 Gene ID: 2324.0 Gene Symbol: FLT4 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=19010843	Inhibitor 8146	0.3 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Renal cell carcinoma 27 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202324lbl.pdf	Secondary		Approved 8307	INLYTA Approved Use Indicated for the treatment of advanced renal cell carcinoma (RCC) after failure of one prior systemic therapy. Launch Date 1.32762239E12

C_max

Value	Dose	Analyte	Population
32.2 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22644797	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22644797	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22644797	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/19603168	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16027439	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202324lbl.pdf	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16027439	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202324lbl.pdf	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

Value	Dose	Analyte	Population
160.3 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22644797	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22644797	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22644797	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/19603168	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16027439	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202324lbl.pdf	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16027439	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 DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202324lbl.pdf	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

T_1/2

Value	Dose	Analyte	Population
5.4 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22644797	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22644797	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22644797	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 EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/19603168	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16027439	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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/16027439	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

F_unbound

Value	Dose	Co-administered	Analyte	Population
1% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202324lbl.pdf	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% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202324lbl.pdf	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

Dose	Population	Adverse events
5 mg 2 times / day steady, oral (starting) Dose: 5 mg, 2 times / day Route: oral Route: steady Dose: 5 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000MedR.pdf	unhealthy, 62 years (range: 20-82 years) n = 359 Health Status: unhealthy Age Group: 62 years (range: 20-82 years) Sex: M+F Population Size: 359 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000MedR.pdf	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: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000MedR.pdf
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: https://pubmed.ncbi.nlm.nih.gov/16027439	unhealthy n = 2 Health Status: unhealthy Condition: advanced solid malignancies Population Size: 2 Sources: https://pubmed.ncbi.nlm.nih.gov/16027439	Sources: https://pubmed.ncbi.nlm.nih.gov/16027439
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: https://pubmed.ncbi.nlm.nih.gov/16027439	unhealthy n = 8 Health Status: unhealthy Condition: advanced solid malignancies Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/16027439	DLT: Stomatitis... Dose limiting toxicities: Stomatitis (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16027439
15 mg 1 times / day steady, oral Dose: 15 mg, 1 times / day Route: oral Route: steady Dose: 15 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16027439	unhealthy n = 6 Health Status: unhealthy Condition: advanced solid malignancies Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/16027439	DLT: Hypertension, Stomatitis... Dose limiting toxicities: Hypertension (1 patient) Stomatitis (1 patient) Pancreatitis (1 patient) Bowel ischemia (1 patient) Thromboembolism (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16027439
20 mg 2 times / day steady, oral Dose: 20 mg, 2 times / day Route: oral Route: steady Dose: 20 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16027439	unhealthy n = 4 Health Status: unhealthy Condition: advanced solid malignancies Population Size: 4 Sources: https://pubmed.ncbi.nlm.nih.gov/16027439	DLT: Hypertension, Hemoptysis... Dose limiting toxicities: Hypertension (2 patients) Hemoptysis (1 patient) Stomatitis (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16027439

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1670 inhibitor 1532 inducer 753	inhibitor 1695	inhibitor 1789	inhibitor 1570

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1463 CYP2A6 670 CYP2C8 869 CYP2C19 1410 CYP2E1 846 P-gp 1401 UGT1A1 200	CYP3A5 383 CYP1A2 1013 CYP2C19 955 UGT1A1 417 P-gp 1491 UGT1A3 421 UGT1A4 345 UGT1A6 306 UGT1A7 235 UGT1A8 282 UGT1A9 378 UGT1A10 289 UGT2B4 248 UGT2B7 387 UGT2B15 202 UGT2B17 212 BCRP 545 OATP1B1 389 OATP1B3 333	CYP1A 55

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A 119	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
CYP2A6 702	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
CYP2C19 1484	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
CYP2D6 1826	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
CYP2E1 929	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
CYP3A4 1857	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A1 249	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
P-gp 1588	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes [IC50 4.5 uM]
CYP2C8 923	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes [Ki 0.5 uM]	no (co-administration study) Comment: axitinib has no effect on exposure of paclitaxel Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf
CYP1A2 1620	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes [Ki 0.7 uM]
CYP2C9 1747	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes [Ki 52.2 uM]
CYP3A4 1857	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes [Ki 8.3 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1670	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	major	yes (co-administration study) Comment: ketoconazole increased cmax of axitinib by by 50%, auc by 106% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf
CYP3A5 383	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	major	yes (co-administration study) Comment: ketoconazole increased cmax of axitinib by by 50%, auc by 106% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf
CYP1A2 1013	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	minor
CYP2C19 955	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	minor	no (pharmacogenomic study) Comment: no clinical effect was observed in genotyping study Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf
UGT1A1 417	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	minor	no (pharmacogenomic study) Comment: no clinical effect was observed in genotyping study Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf
UGT1A10 289	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A3 421	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A4 345	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A6 306	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A7 235	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A8 282	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A9 378	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT2B15 202	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT2B17 212	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT2B4 248	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT2B7 387	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
BCRP 545	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes
OATP1B1 389	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes
OATP1B3 333	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes
P-gp 1491	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1603	inhibitor 1584 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000PharmR.pdf

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:66910	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:66910
ChemicalBook	CB81011728	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB81011728
MolPort	MolPort-006-392-413	https://www.molport.com/shop/molecule-link/MolPort-006-392-413
Selleck Chemicals	Axitinib	http://www.selleckchem.com/products/Axitinib.html
ZINC	ZINC000003816287	http://zinc15.docking.org/substances/ZINC000003816287
eMolecules	26951384	https://www.emolecules.com/cgi-bin/more?vid=26951384

PubMed

Title	Date	PubMed
Pharmacophore modeling and virtual screening studies for new VEGFR-2 kinase inhibitors.	2010 Nov	20869793
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.	2010 Nov 24	21095574
Comprehensive analysis of kinase inhibitor selectivity.	2011 Oct 30	22037378
Evaluation of drugs with specific organ toxicities in organ-specific cell lines.	2012 Mar	22166485

Patents

Sample Use Guides

In Vivo Use Guide

5 mg orally twice daily

Route of Administration: Oral

In Vitro Use Guide

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 Dec 16 19:52:12 UTC 2022` Edited by `admin` on `Fri Dec 16 19:52:12 UTC 2022`
Record UNII	C9LVQ0YUXG
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

AXITINIB

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 [WHO-DD]

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 [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