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 41 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 8297	0.1 nM [IC50]
Vascular endothelial growth factor receptor 2 104 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 8297	0.2 nM [IC50]
Vascular endothelial growth factor receptor 3 41 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 8297	0.3 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Renal cell carcinoma 31 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/202324lbl.pdf	Secondary		Approved 8429	INLYTA Approved Use Indicated for the treatment of advanced renal cell carcinoma (RCC) after failure of one prior systemic therapy. Launch Date 2012

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 1737 inhibitor 1587 inducer 781	inhibitor 1767	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2A6 707 CYP2C8 911 CYP2C19 1478 CYP2E1 882 P-gp 1461 UGT1A1 204	CYP3A5 395 CYP1A2 1054 CYP2C19 991 UGT1A1 418 P-gp 1537 UGT1A3 422 UGT1A4 347 UGT1A6 307 UGT1A7 236 UGT1A8 283 UGT1A9 380 UGT1A10 291 UGT2B4 249 UGT2B7 389 UGT2B15 203 UGT2B17 213 BCRP 561 OATP1B1 406 OATP1B3 350	CYP1A 56

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A 121	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
CYP2A6 739	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A1 254	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes [IC50 4.5 uM]
CYP2C8 965	inhibitor 3277 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 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes [Ki 0.7 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes [Ki 52.2 uM]
CYP3A4 1925	inhibitor 3277 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 1737	substrate 3367 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 395	substrate 3367 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 1054	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	minor
CYP2C19 991	substrate 3367 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 418	substrate 3367 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 291	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A3 422	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A4 347	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A6 307	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A7 236	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A8 283	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT1A9 380	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT2B15 203	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT2B17 213	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT2B4 249	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
UGT2B7 389	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	no
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/202324Orig1s000ClinPharmR.pdf	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 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
		252160124
Modulation of the antitumor activity of metronomic cyclophosphamide by the angiogenesis inhibitor axitinib.	2008 Jan	18202011
Comprehensive analysis of kinase inhibitor selectivity.	2011 Oct 30	22037378
The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents.	2013 Aug 8	23829549
Bridging Functional and Structural Cardiotoxicity Assays Using Human Embryonic Stem Cell-Derived Cardiomyocytes for a More Comprehensive Risk Assessment.	2015 Nov	26259608

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 15 16:19:06 GMT 2023` Edited by `admin` on `Fri Dec 15 16:19:06 GMT 2023`
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

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

NCI_THESAURUS

C1742

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

EMA ASSESSMENT REPORTS

INLYTA (AUTHORIZED: CARCINOMA, CANCER CELL)

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

FDA ORPHAN DRUG

730120

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

WHO-VATC

QL01XE17

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

NCI_THESAURUS

C93259

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

NDF-RT

N0000175605

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

NCI_THESAURUS

C129825

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

FDA ORPHAN DRUG

230706

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

EU-Orphan Drug

EU/3/10/844

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

LIVERTOX

NBK548139

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

FDA ORPHAN DRUG

240607

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

Code System Code Type Description

DRUG CENTRAL

4225

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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WIKIPEDIA

Axitinib

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

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RXCUI

1242999

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

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RxNorm

EPA CompTox

DTXSID3049049

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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MESH

C503983

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

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LACTMED

Axitinib

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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PUBCHEM

6450551

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

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MERCK INDEX

m2153

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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Merck Index

FDA UNII

C9LVQ0YUXG

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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SMS_ID

100000089442

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

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EVMPD

SUB25427

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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ChEMBL

CHEMBL1289926

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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NDF-RT

N0000020000

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

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Receptor Tyrosine Kinase Inhibitors [MoA]

NSC

757441

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

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IUPHAR

5659

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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USAN

RR-15

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

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INN

8720

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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DRUG BANK

DB06626

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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DAILYMED

C9LVQ0YUXG

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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CHEBI

66910

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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NCI_THESAURUS

C38718

Created by admin on Fri Dec 15 16:19:07 GMT 2023 , Edited by admin on Fri Dec 15 16:19:07 GMT 2023

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CAS

319460-85-0

Created by admin on Fri Dec 15 16:19:06 GMT 2023 , Edited by admin on Fri Dec 15 16:19:06 GMT 2023

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VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 3

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AXITINIB

ACTIVE MOIETY

Amount:

Name	Property Type	Amount	Referenced Substance	Defining	Parameters	References
Biological Half-life	PHARMACOKINETIC

Volume of Distribution	PHARMACOKINETIC

AE	Significance	Dose	Population
Altered state of consciousness	1 patient Disc. AE	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
Anemia	1 patient Disc. AE	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
Ascites	1 patient Disc. AE	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
Blood creatinine increased	1 patient Disc. AE	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
Cerebral hemorrhage	1 patient Disc. AE	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
Dyspnea exertional	1 patient Disc. AE	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
Dyspnea	1 patient Disc. AE	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
Hypertension	1 patient Disc. AE	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
Hypoglycemia	1 patient Disc. AE	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
Palmar-plantar erythrodysaesthesia syndrome	1 patient Disc. AE	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
Pneumothorax	1 patient Disc. AE	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
Retinal vein thrombosis	1 patient Disc. AE	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
Vomiting	1 patient Disc. AE	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
Disease progression	11 patient Disc. AE	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
Asthenia	2 patients Disc. AE	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
Decreased appetite	2 patients Disc. AE	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
Pleural effusion	2 patients Disc. AE	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
Transient ischemic attack	3 patients Disc. AE	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
Fatigue	4 patients Disc. AE	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
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: 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
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: 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
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: 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
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: 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
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: 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
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: 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
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: 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
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: 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
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: 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

Details

SMILES

InChI

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

C_max

T_1/2

F_unbound

Drug as perpetrator