KEGG   DRUG: Erdafitinib
Entry
D10927                      Drug                                   
Name
Erdafitinib (JAN/USAN/INN);
Balversa (TN)
Product
BALVERSA (Janssen Products LP)
Formula
C25H30N6O2
Exact mass
446.2430
Mol weight
446.54
Structure
Class
Antineoplastic
 DG01918  Tyrosine kinase inhibitor
  DG01917  Receptor tyrosine kinase inhibitor
   DG03208  FGFR inhibitor
Metabolizing enzyme substrate
 DG01642  CYP2C9 substrate
 DG01633  CYP3A/CYP3A4 substrate
  DG02913  CYP3A4 substrate
Transporter substrate
 DG01665  ABCB1 substrate
Transporter inhibitor
 DG01622  ABCB1 inhibitor
 DG02863  SLC22A2 inhibitor
Remark
Therapeutic category: 4291
ATC code: L01EN01
Product: D10927<JP/US>
Efficacy
Antineoplastic, Receptor tyrosine kinase inhibitor
  Disease
Urothelial carcinoma (FGFR3 or FGFR2 genetic alterations) [DS:H00022]
Comment
Treatment of cancer
Target
FGFR3* (CD333) [HSA_VAR:2261v2] [HSA:2261] [KO:K05094]
FGFR2* (CD332) [HSA_VAR:2263v2] [HSA:2263] [KO:K05093]
  Pathway
hsa04151  PI3K-Akt signaling pathway
hsa05200  Pathways in cancer
hsa05219  Bladder cancer
  Network
nt06265  Bladder cancer
Metabolism
Enzyme: CYP2C9 [HSA:1559], CYP3A4 [HSA:1576]
Transporter: ABCB1 [HSA:5243]
Interaction
Transporter inhibition: ABCB1 [HSA:5243], SLC22A2 [HSA:6582]
Brite
Anatomical Therapeutic Chemical (ATC) classification [BR:br08303]
 L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
  L01 ANTINEOPLASTIC AGENTS
   L01E PROTEIN KINASE INHIBITORS
    L01EN Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors
     L01EN01 Erdafitinib
      D10927  Erdafitinib (JAN/USAN/INN) <JP/US>
USP drug classification [BR:br08302]
 Antineoplastics
  Molecular Target Inhibitors
   Fibroblast Growth Factor Receptor (FGFR) Inhibitors
    Erdafitinib
     D10927  Erdafitinib (JAN/USAN/INN)
Therapeutic category of drugs in Japan [BR:br08301]
 4  Agents affecting cellular function
  42  Antineoplastics
   429  Miscellaneous
    4291  Other Antitumors
     D10927  Erdafitinib (JAN/USAN/INN)
Drug groups [BR:br08330]
 Antineoplastic
  DG01918  Tyrosine kinase inhibitor
   DG01917  Receptor tyrosine kinase inhibitor
    DG03208  FGFR inhibitor
     D10927  Erdafitinib
 Metabolizing enzyme substrate
  DG01642  CYP2C9 substrate
   D10927  Erdafitinib
  DG01633  CYP3A/CYP3A4 substrate
   DG02913  CYP3A4 substrate
    D10927  Erdafitinib
 Transporter substrate
  DG01665  ABCB1 substrate
   D10927  Erdafitinib
 Transporter inhibitor
  DG01622  ABCB1 inhibitor
   D10927  Erdafitinib
  DG02863  SLC22A2 inhibitor
   D10927  Erdafitinib
Target-based classification of drugs [BR:br08310]
 Protein kinases
  Receptor tyrosine kinases (RTK)
   FGFR family
    FGFR2* (CD332) [HSA_VAR:2263v2]
     D10927  Erdafitinib (JAN/USAN/INN) <JP/US>
    FGFR3* (CD333) [HSA_VAR:2261v2]
     D10927  Erdafitinib (JAN/USAN/INN) <JP/US>
New drug approvals in the USA [br08319.html]
 New molecular entities and new therapeutic biological products
  D10927
New drug approvals in Europe [br08329.html]
 European public assessment reports (EPAR) authorised medicine
  D10927
New drug approvals in Japan [br08318.html]
 Drugs with new active ingredients
  D10927
New drug approvals in the USA, Europe and Japan [br08328.html]
 Approval dates by FDA, EMA and PMDA
  D10927
Drug metabolizing enzymes and transporters [br08309.html]
 Drug metabolizing enzymes
  D10927
 Drug transporters
  D10927
Pharmacogenomic biomarkers [br08341.html]
 Somatic variations in targeted cancer therapies
  D10927
Other DBs
CAS: 1346242-81-6
PubChem: 342581784
PDB-CCD: 5SF[PDBj]
LinkDB
KCF data

ATOM        33
            1   C8y C     9.7300  -15.3300
            2   C8y C     9.7300  -16.7300
            3   C8x C    10.9200  -17.4300
            4   C8x C    12.1800  -16.7300
            5   C8y C    12.1800  -15.3300
            6   C8x C    10.9200  -14.6300
            7   N5x N     8.5400  -14.6300
            8   C8y C     7.2800  -15.3300
            9   C8x C     7.2800  -16.7300
            10  N5x N     8.5400  -17.4300
            11  C8y C     6.0900  -14.6300
            12  C8x C     5.9500  -13.2300
            13  N5x N     4.5500  -12.9500
            14  N4y N     3.8500  -14.1400
            15  C8x C     4.8300  -15.1900
            16  C1a C     2.4500  -14.2800
            17  N1c N    13.3700  -14.6300
            18  C1b C    14.6300  -15.3300
            19  C1b C    15.8200  -14.6300
            20  N1b N    17.0100  -15.3300
            21  C1c C    18.2700  -14.6300
            22  C1a C    19.4600  -15.3300
            23  C8y C    13.3700  -13.2300
            24  C8y C    12.1800  -11.1300
            25  C8x C    12.1800  -12.5300
            26  C8x C    14.6300  -12.5300
            27  C8y C    14.6300  -11.1300
            28  C8x C    13.3700  -10.4300
            29  O2a O    10.9647  -10.4349
            30  O2a O    15.8366  -10.4200
            31  C1a C    17.0463  -11.1053
            32  C1a C     9.7763  -11.1277
            33  C1a C    18.2872  -13.2301
BOND        36
            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     1   7 1
            8     7   8 2
            9     8   9 1
            10    9  10 2
            11    2  10 1
            12    8  11 1
            13   11  12 1
            14   12  13 2
            15   13  14 1
            16   14  15 1
            17   11  15 2
            18   14  16 1
            19    5  17 1
            20   17  18 1
            21   18  19 1
            22   19  20 1
            23   20  21 1
            24   21  22 1
            25   17  23 1
            26   24  25 2
            27   25  23 1
            28   26  27 1
            29   27  28 2
            30   24  28 1
            31   26  23 2
            32   24  29 1
            33   27  30 1
            34   30  31 1
            35   29  32 1
            36   21  33 1

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