MITOTOX

Drug

D0486 | axitinib

Properties

Molecular Formula	C22H18N4OS
Molecular Weight	386.5
Structure
State	solid
Clearance	The average clearance of axitinib is 38 L/h.
Volume of distribution	The volume of distribution is 160 L.
Route of elimination	Axitinib is mainly eliminated unchanged in the feces (41%) with 12% of the original dose as unchanged axitinib. There is also 23% eliminated in the urine, most of which are metabolites.
Protein binding	Plasma protein binding for axitinib is high at over 99% with most protein binding to albumin followed by alpha1-acid glycoprotein.
Half life	Axitinib has a half life of 2.5 to 6.1 hours.
Absorption	After one 5 mg dose of axitinib, it takes about 2.5 to 4.1 hours to reach maximum plasma concentration.

Therapeutic Classification Source: DrugBank

L01XE17 Axitinib

[L01XE] Protein kinase inhibitors

[L01X] OTHER ANTINEOPLASTIC AGENTS

[L01] ANTINEOPLASTIC AGENTS

[L] Antineoplastic and immunomodulating agents

Mitochondrial Toxicity Evaulation

Toxicity	Dose	Species	Model	Method	Action	Positive criterion	Reference
MEMBRANE POTENTIAL	3.76±2.80	human	qHTS-HepG2	MMP assay	decrease	IC50	163
MEMBRANE POTENTIAL	1.09	human	HepG2	MMP assay	decrease	IC50	163
MEMBRANE POTENTIAL		rat	hepatocytes	MMP assay	Negative	IC50	163
ELECTRON TRANSPORT CHAIN		rat	isolated liver mitochondria	measurements of mitochondrial respiration; RST inhibition assay, RST uncoupling assay; IC 50ratio of glucose/galactose assay	decrease		53

GHS Hazard Tables Source: PubChem

Pictogram	Signal	Statements	Precautionary Statement Codes
	Warning	Aggregated GHS information provided by 68 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies. H302 (55.88%): Harmful if swallowed [Warning Acute toxicity, oral] H341 (42.65%): Suspected of causing genetic defects [Warning Germ cell mutagenicity] H361 (44.12%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity] H373 (44.12%): Causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure] H400 (57.35%): Very toxic to aquatic life [Warning Hazardous to the aquatic environment, acute hazard] Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.	P201, P202, P260, P264, P270, P273, P281, P301+P312, P308+P313, P314, P330, P391, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

Pictogram

Signal

Statements

Precautionary Statement Codes

Warning

Aggregated GHS information provided by 68 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

H302 (55.88%): Harmful if swallowed [Warning Acute toxicity, oral]

H341 (42.65%): Suspected of causing genetic defects [Warning Germ cell mutagenicity]

H361 (44.12%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]

H373 (44.12%): Causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure]

H400 (57.35%): Very toxic to aquatic life [Warning Hazardous to the aquatic environment, acute hazard]

Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.

P201, P202, P260, P264, P270, P273, P281, P301+P312, P308+P313, P314, P330, P391, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)

Indications Source: SIDER

Synonyms Source: PubChem

(E)-N-Methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)benzamide	(E)-N-methyl-2-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-ylthio)benzamide	319460-85-0
460A850	4CA-0215	4ag8
4agc	A10103	AB0008632
AB01274739-01	AB01274739_02	ABP000115
AC-1539	AG 013736	AG-013736
AG-013736;Axitinib	AG-13736	AG013736
AG13736	AKOS015902898	AM20090673
AOB87786	Axitinib	Axitinib (AG 013736)
Axitinib (JAN/USAN)	Axitinib [USAN:INN:JAN]	Axitinib, >=98% (HPLC)
Axitinib,AG-013736	Axitinib/AG013736	BCP01371
BCP9000345	BCPP000372	BDBM25117
BRD-K29905972-001-01-4	BRD-K29905972-001-02-2	Benzamide, N-methyl-2-((3-((1E)-2-(2-pyridinyl)ethenyl)-1H-indazo)-6-yl)thio)-
Benzamide, N-methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-	C22H18N4OS	C9LVQ0YUXG
CAS-319460-85-0	CHEBI:66910	CHEBI:94568
CHEMBL1289926	CS-0116	D03218
DB06626	DSSTox_CID_28975	DSSTox_GSID_49049
DSSTox_RID_83240	DTXSID3049049	EX-A337
GTPL5659	HY-10065	Inlyta
Inlyta (TN)	J-502064	KS-1448
MFCD09837898	MLS006010164	N-METHYL-2-(3-((E)-2-PYRIDIN-2-YL-VINYL)-1H-INDAZOL-6-YLSULFANYL)-BENZAMIDE;
N-Methyl-[[3[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide	N-methyl-2-((3-((1E)-2-(pyridin-2-yl)ethenyl)-1H-indazol-6-yl)sulfanyl)benzamide	N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-1H-indazol-6-yl}sulfanyl)benzamide
N-methyl-2-({3-[(E)-2-(pyridin-2-yl)vinyl]-1H-indazol-6-yl}sulfanyl)benzamide	N-methyl-2-({3-[(E)-2-pyridin-2-ylethenyl]-2H-indazol-6-yl}sulfanyl)benzamide	N-methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide
NCGC00241108-01	NCGC00241108-04	NCGC00241108-06
NSC-757441	NSC757441	Q-200662
Q-3279	Q4830631	QCR-109
S1005	SB20061	SC-22491
SCHEMBL172918	SMR002530046	SR-01000941566
SR-01000941566-1	SW219464-1	SYN1014
TR-013491	Tox21_113597	Tox21_113597_1
UNII-C9LVQ0YUXG	ZINC3816287	axitinibum
cc-356

External IDs

DrugBank Name	axitinib
DrugBank	DB06626
CAS Number	319460-85-0, 319463-51-9
PubChem Compound	6450551
KEGG Drug	D03218
ChEBI	66910
PharmGKB	PA164924493