KEGG   DRUG: Axitinib
Entry
D03218                      Drug                                   

Name
Axitinib (JAN/USAN);
Inlyta (TN)
Product
Formula
C22H18N4OS
Exact mass
386.1201
Mol weight
386.4695
Structure
Class
Antineoplastic
 DG01918  Tyrosine kinase inhibitor
  DG01917  Receptor tyrosine kinase inhibitor
Metabolizing enzyme substrate
 DG01633  CYP3A/CYP3A4 substrate
  DG02913  CYP3A4 substrate
 DG02925  CYP3A5 substrate
Remark
Therapeutic category: 4291
ATC code: L01EK01
Product: D03218<JP/US>
Efficacy
Antineoplastic, Receptor tyrosine kinase inhibitor
  Disease
Renal cell carcinoma [DS:H00021]
Target
VEGFR1 (FLT1) [HSA:2321] [KO:K05096]
VEGFR2 (KDR) [HSA:3791] [KO:K05098]
VEGFR3 (FLT4) [HSA:2324] [KO:K05097]
  Pathway
hsa04010  MAPK signaling pathway
hsa04370  VEGF signaling pathway
hsa05200  Pathways in cancer
Metabolism
Enzyme: CYP3A4 [HSA:1576], CYP3A5 [HSA:1577]
Interaction
Structure map
map07045  Antineoplastics - protein kinase inhibitors
Brite
Anatomical Therapeutic Chemical (ATC) classification [BR:br08303]
 L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
  L01 ANTINEOPLASTIC AGENTS
   L01E PROTEIN KINASE INHIBITORS
    L01EK Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors
     L01EK01 Axitinib
      D03218  Axitinib (JAN/USAN) <JP/US>
USP drug classification [BR:br08302]
 Antineoplastics
  Molecular Target Inhibitors
   Axitinib
    D03218  Axitinib (JAN/USAN)
Therapeutic category of drugs in Japan [BR:br08301]
 4  Agents affecting cellular function
  42  Antineoplastics
   429  Miscellaneous
    4291  Other Antitumors
     D03218  Axitinib (JAN/USAN)
Target-based classification of drugs [BR:br08310]
 Protein kinases
  Receptor tyrosine kinases (RTK)
   VEGFR family
    VEGFR1 (FLT1)
     D03218  Axitinib (JAN/USAN) <JP/US>
    VEGFR2 (KDR)
     D03218  Axitinib (JAN/USAN) <JP/US>
    VEGFR3 (FLT4)
     D03218  Axitinib (JAN/USAN) <JP/US>
New drug approvals in the USA [br08319.html]
 New molecular entities and new therapeutic biological products
  D03218
New drug approvals in Europe [br08329.html]
 European public assessment reports (EPAR) authorised medicine
  D03218
New drug approvals in Japan [br08318.html]
 Drugs with new active ingredients
  D03218
New drug approvals in the USA, Europe and Japan [br08328.html]
 Approval dates by FDA, EMA and PMDA
  D03218
Drug metabolizing enzymes and transporters [br08309.html]
 Drug metabolizing enzymes
  D03218
Other DBs
CAS: 319460-85-0
PubChem: 17397371
ChEBI: 66910
ChEMBL: CHEMBL1289926
PDB-CCD: AXI[PDBj]
LigandBox: D03218
NIKKAJI: J2.302.956A
LinkDB
KCF data

ATOM        28
            1   C8y C    13.1600  -21.9100
            2   C8x C    13.1600  -23.3100
            3   C8x C    14.4200  -24.0100
            4   C8y C    15.6100  -23.3100
            5   C8y C    15.6100  -21.9100
            6   C8x C    14.4200  -21.2100
            7   C8y C    16.9400  -23.7300
            8   N5x N    17.7800  -22.6100
            9   N4x N    16.9400  -21.4900
            10  S2a S    11.9700  -21.2100
            11  C8y C    10.7800  -21.9100
            12  C8y C     9.5900  -21.2100
            13  C8x C     8.3300  -21.9100
            14  C8x C     8.3300  -23.3100
            15  C8x C     9.5200  -24.0100
            16  C8x C    10.7800  -23.3100
            17  C5a C     9.5900  -19.8100
            18  N1b N     8.3300  -19.1100
            19  O5a O    10.7800  -19.1100
            20  C1a C     7.1400  -19.8100
            21  C2b C    16.9400  -25.2000
            22  C2b C    18.2000  -25.9000
            23  C8y C    18.2172  -27.2999
            24  N5x N    17.0008  -28.0224
            25  C8x C    17.0181  -29.4223
            26  C8x C    18.2391  -30.1073
            27  C8x C    19.4556  -29.3847
            28  C8x C    19.4382  -27.9848
BOND        31
            1     1   2 2
            2     2   3 1
            3     3   4 2
            4     4   5 1
            5     5   6 2
            6     1   6 1
            7     4   7 1
            8     7   8 2
            9     8   9 1
            10    5   9 1
            11    1  10 1
            12   10  11 1
            13   11  12 2
            14   12  13 1
            15   13  14 2
            16   14  15 1
            17   15  16 2
            18   11  16 1
            19   12  17 1
            20   17  18 1
            21   17  19 2
            22   18  20 1
            23    7  21 1
            24   21  22 2
            25   22  23 1
            26   23  24 2
            27   24  25 1
            28   25  26 2
            29   26  27 1
            30   27  28 2
            31   23  28 1

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