KEGG   DRUG: Axitinib
Entry
D03218                      Drug                                   
Name
Axitinib (JAN/USAN);
Inlyta (TN)
Product
INLYTA (Pfizer Laboratories Div Pfizer), INLYTA (U.S. Pharmaceuticals)
Formula
C22H18N4OS
Exact mass
386.1201
Mol weight
386.4695
Structure
Class
Antineoplastic
 DG01918  Tyrosine kinase inhibitor
  DG01917  Receptor tyrosine kinase inhibitor
   DG03203  VEGFR 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)
Drug groups [BR:br08330]
 Antineoplastic
  DG01918  Tyrosine kinase inhibitor
   DG01917  Receptor tyrosine kinase inhibitor
    DG03203  VEGFR inhibitor
     D03218  Axitinib
 Metabolizing enzyme substrate
  DG01633  CYP3A/CYP3A4 substrate
   DG02913  CYP3A4 substrate
    D03218  Axitinib
  DG02925  CYP3A5 substrate
   D03218  Axitinib
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
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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