Tucatinib


Entry
D11141                      Drug                                   
Name
Tucatinib (USAN/INN);
Tukysa (TN)
Product
TUKYSA (SEAGEN)
Formula
C26H24N8O2
Exact mass
480.2022
Mol weight
480.5212
Structure
Class
Antineoplastic
 DG01918  Tyrosine kinase inhibitor
  DG01917  Receptor tyrosine kinase inhibitor
   DG03158  HER2 inhibitor
Metabolizing enzyme substrate
 DG02918  CYP2C8 substrate
 DG01633  CYP3A/CYP3A4 substrate
Remark
ATC code: L01EH03
Product: D11141<US>
Efficacy
Antineoplastic, Receptor tyrosine kinase inhibitor
  Disease
Breast cancer (HER2 positive) [DS:H00031]
Target
ERBB2* (HER2, CD340) [HSA_VAR:2064v1] [HSA:2064] [KO:K05083]
ERBB3 (HER3) [HSA:2065] [KO:K05084]
  Network
N10009  Tyrosine kinase inhibitor to HER2 overexpression/amplification
  Pathway
hsa04010  MAPK signaling pathway
hsa04012  ErbB signaling pathway
hsa04151  PI3K-Akt signaling pathway
hsa05200  Pathways in cancer
hsa05224  Breast cancer
Metabolism
Enzyme: CYP2C8 [HSA:1558]; CYP3A [HSA:1576 1577 1551]
Interaction
Brite
Anatomical Therapeutic Chemical (ATC) classification [BR:br08303]
 L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
  L01 ANTINEOPLASTIC AGENTS
   L01E PROTEIN KINASE INHIBITORS
    L01EH Human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitors
     L01EH03 Tucatinib
      D11141  Tucatinib (USAN/INN) <US>
USP drug classification [BR:br08302]
 Antineoplastics
  Molecular Target Inhibitors
   Tucatinib
    D11141  Tucatinib (USAN/INN)
Drug groups [BR:br08330]
 Antineoplastic
  DG01918  Tyrosine kinase inhibitor
   DG01917  Receptor tyrosine kinase inhibitor
    DG03158  HER2 inhibitor
     D11141  Tucatinib
 Metabolizing enzyme substrate
  DG02918  CYP2C8 substrate
   D11141  Tucatinib
  DG01633  CYP3A/CYP3A4 substrate
   D11141  Tucatinib
Drug classes [BR:br08332]
 Antineoplastic
  DG03158  HER2 inhibitor
   D11141  Tucatinib
Target-based classification of drugs [BR:br08310]
 Protein kinases
  Receptor tyrosine kinases (RTK)
   EGFR family
    ERBB2* (HER2, CD340) [HSA_VAR:2064v1]
     D11141  Tucatinib (USAN/INN) <US>
    ERBB3 (HER3)
     D11141  Tucatinib (USAN/INN) <US>
New drug approvals in the USA [br08319.html]
 New molecular entities and new therapeutic biological products
  D11141
New drug approvals in Europe [br08329.html]
 European public assessment reports (EPAR) authorised medicine
  D11141
New drug approvals in the USA, Europe and Japan [br08328.html]
 Approval dates by FDA, EMA and PMDA
  D11141
Drug metabolizing enzymes and transporters [br08309.html]
 Drug metabolizing enzymes
  D11141
Pharmacogenomic biomarkers [br08341.html]
 Somatic variations in targeted cancer therapies
  D11141
Other DBs
CAS: 937263-43-9
PubChem: 376219065
KCF data

ATOM        36
            1   C8y C    24.3600  -13.7900
            2   C8y C    24.3600  -15.1900
            3   C8y C    23.1700  -15.8900
            4   N5x N    21.9100  -15.1900
            5   C8x C    21.9100  -13.7900
            6   N5x N    23.1700  -13.0900
            7   C8x C    25.5500  -13.0900
            8   C8x C    26.8100  -13.7900
            9   C8y C    26.8100  -15.1900
            10  C8x C    25.5500  -15.8900
            11  N1b N    28.0000  -15.8900
            12  C2y C    29.1900  -15.1900
            13  O2x O    29.1900  -13.7900
            14  C1x C    30.5200  -13.3000
            15  C1z C    31.3600  -14.4200
            16  N2x N    30.5900  -15.6100
            17  N1b N    23.1700  -17.2900
            18  C1a C    32.0600  -13.2300
            19  C1a C    32.3400  -15.4000
            20  C8y C    24.3853  -17.9851
            21  C8x C    24.3911  -19.3897
            22  C8x C    25.6064  -20.0847
            23  C8y C    26.8159  -19.3797
            24  C8y C    26.8101  -17.9751
            25  C8x C    25.5948  -17.2801
            26  C1a C    28.0131  -17.2740
            27  O2a O    28.0312  -20.0746
            28  C8y C    27.9674  -21.4906
            29  C8x C    26.7728  -22.1638
            30  C8x C    26.7582  -23.5637
            31  N4y N    27.9632  -24.2763
            32  C8y C    29.1578  -23.6032
            33  C8x C    29.1724  -22.2033
            34  N5x N    28.2343  -25.6205
            35  C8x C    29.5964  -25.7781
            36  N5x N    30.1671  -24.5313
BOND        41
            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    9  11 1
            13   11  12 1
            14   12  13 1
            15   13  14 1
            16   14  15 1
            17   15  16 1
            18   12  16 2
            19    3  17 1
            20   15  18 1
            21   15  19 1
            22   17  20 1
            23   20  21 2
            24   21  22 1
            25   22  23 2
            26   23  24 1
            27   24  25 2
            28   20  25 1
            29   24  26 1
            30   23  27 1
            31   27  28 1
            32   28  29 1
            33   29  30 2
            34   30  31 1
            35   31  32 1
            36   32  33 1
            37   28  33 2
            38   31  34 1
            39   34  35 2
            40   35  36 1
            41   32  36 2