KEGG   DRUG: Pemigatinib
Entry
D11417                      Drug                                   

Name
Pemigatinib (JAN/USAN/INN);
Pemazyre (TN)
Product
Formula
C24H27F2N5O4
Exact mass
487.2031
Mol weight
487.4991
Structure
Class
Antineoplastic
 DG01918  Tyrosine kinase inhibitor
  DG01917  Receptor tyrosine kinase inhibitor
Metabolizing enzyme substrate
 DG01633  CYP3A/CYP3A4 substrate
  DG02913  CYP3A4 substrate
Remark
Therapeutic category: 4291
ATC code: L01EX20
Product: D11417<JP/US>
Efficacy
Antineoplastic, Receptor tyrosine kinase inhibitor
  Disease
Cholangiocarcinoma (FGFR2 fusion positive) [DS:H00046]
Target
FGFR2* (CD332) [HSA_VAR:2263v2] [HSA:2263] [KO:K05093]
FGFR1 (CD331) [HSA:2260] [KO:K04362]
FGFR3 (CD333) [HSA:2261] [KO:K05094]
  Pathway
hsa01521  EGFR tyrosine kinase inhibitor resistance
hsa04151  PI3K-Akt signaling pathway
hsa05200  Pathways in cancer
Metabolism
Enzyme: CYP3A4 [HSA:1576]
Interaction
Brite
Anatomical Therapeutic Chemical (ATC) classification [BR:br08303]
 L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
  L01 ANTINEOPLASTIC AGENTS
   L01E PROTEIN KINASE INHIBITORS
    L01EX Other protein kinase inhibitors
     L01EX20 Pemigatinib
      D11417  Pemigatinib (JAN/USAN/INN) <JP/US>
Therapeutic category of drugs in Japan [BR:br08301]
 4  Agents affecting cellular function
  42  Antineoplastics
   429  Miscellaneous
    4291  Other Antitumors
     D11417  Pemigatinib (JAN/USAN/INN)
Target-based classification of drugs [BR:br08310]
 Protein kinases
  Receptor tyrosine kinases (RTK)
   FGFR family
    FGFR1 (CD331)
     D11417  Pemigatinib (JAN/USAN/INN) <JP/US>
    FGFR2* (CD332) [HSA_VAR:2263v2]
     D11417  Pemigatinib (JAN/USAN/INN) <JP/US>
    FGFR3 (CD333)
     D11417  Pemigatinib (JAN/USAN/INN) <JP/US>
New drug approvals in the USA [br08319.html]
 New molecular entities and new therapeutic biological products
  D11417
New drug approvals in Europe [br08329.html]
 European public assessment reports (EPAR) authorised medicine
  D11417
New drug approvals in Japan [br08318.html]
 Drugs with new active ingredients
  D11417
New drug approvals in the USA, Europe and Japan [br08328.html]
 Approval dates by FDA, EMA and PMDA
  D11417
Drug metabolizing enzymes and transporters [br08309.html]
 Drug metabolizing enzymes
  D11417
Pharmacogenomic biomarkers [br08341.html]
 Somatic variations in targeted cancer therapies
  D11417
Other DBs
CAS: 1513857-77-6
PubChem: 384585394
ChEMBL: CHEMBL4297522
LinkDB
KCF data

ATOM        35
            1   C8y C    18.2000  -16.5900
            2   C8x C    18.2000  -17.9900
            3   N5x N    17.0100  -18.6900
            4   C8y C    15.7500  -17.9900
            5   C8y C    15.7500  -16.5900
            6   C8y C    17.0100  -15.8900
            7   C8x C    14.4200  -16.1700
            8   C8y C    13.5800  -17.2900
            9   N4x N    14.4200  -18.4100
            10  C1b C    12.1800  -17.2900
            11  N1y N    11.4800  -16.1000
            12  C1x C    12.1800  -14.9100
            13  C1x C    11.4800  -13.6500
            14  O2x O    10.0800  -13.6500
            15  C1x C     9.3800  -14.8400
            16  C1x C    10.0800  -16.1000
            17  C1x C    19.4600  -15.8900
            18  N1y N    19.4600  -14.4900
            19  C5x C    18.2700  -13.7900
            20  N1y N    17.0100  -14.4900
            21  C1b C    15.8200  -13.7900
            22  C1a C    14.5600  -14.4900
            23  O5x O    18.2700  -12.3900
            24  C8y C    20.6500  -13.7900
            25  C8y C    21.9100  -14.4200
            26  C8y C    23.0300  -13.7200
            27  C8x C    23.0300  -12.3200
            28  C8y C    21.8400  -11.6200
            29  C8y C    20.6500  -12.3900
            30  O2a O    24.2200  -14.4200
            31  C1a C    25.4100  -13.7200
            32  O2a O    21.8400  -10.2200
            33  C1a C    20.5800   -9.5200
            34  X   F    21.9100  -15.8200
            35  X   F    19.4600  -11.6900
BOND        39
            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     5   7 1
            8     7   8 2
            9     8   9 1
            10    4   9 1
            11    8  10 1
            12   10  11 1
            13   11  12 1
            14   12  13 1
            15   13  14 1
            16   14  15 1
            17   15  16 1
            18   11  16 1
            19    1  17 1
            20   17  18 1
            21   18  19 1
            22   19  20 1
            23    6  20 1
            24   20  21 1
            25   21  22 1
            26   19  23 2
            27   18  24 1
            28   24  25 2
            29   25  26 1
            30   26  27 2
            31   27  28 1
            32   28  29 2
            33   24  29 1
            34   26  30 1
            35   30  31 1
            36   28  32 1
            37   32  33 1
            38   25  34 1
            39   29  35 1

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