D0486 | axitinib

Molecular Formula C22H18N4OS
Molecular Weight 386.5
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.


L01XE17 Axitinib

[L01XE] Protein kinase inhibitors



[L] Antineoplastic and immunomodulating agents

Toxicity Dose Time 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

Pictogram Signal Statements Precautionary Statement Codes

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.)

  • (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
    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

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