Tazemetostat hydrobromide


Entry
D11485                      Drug                                   
Name
Tazemetostat hydrobromide (JAN/USAN);
Tazverik (TN)
Product
TAZVERIK (Epizyme)
Formula
C34H44N4O4. HBr
Exact mass
652.2624
Mol weight
653.6495
Structure
Simcomp
Class
Transporter substrate
 DG01665  ABCB1 substrate
Transporter inhibitor
 DG02864  SLC47A1 inhibitor
 DG03110  SLC47A2 inhibitor
Remark
Therapeutic category: 4291
ATC code: L01XX72
Chemical structure group: DG03020
Product (DG03020): D11485<JP/US>
Efficacy
Antineoplastic, histone methyltransferase inhibitor
  Disease
Epithelioid sarcoma [DS:H02427]
Follicular Lymphoma (EZH2 mutation positive) [DS:H01613]
Comment
Treatment of epithelioid sarcoma
Target
EZH2* [HSA_VAR:2146v1] [HSA:2146] [KO:K11430]
  Pathway
hsa00310  Lysine degradation
hsa05206  MicroRNAs in cancer
Metabolism
Transporter: ABCB1 [HSA:5243]
Interaction
Transporter inhibition: SLC47A1 [HSA:55244], SLC47A2 [HSA:146802]
Brite
Anatomical Therapeutic Chemical (ATC) classification [BR:br08303]
 L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
  L01 ANTINEOPLASTIC AGENTS
   L01X OTHER ANTINEOPLASTIC AGENTS
    L01XX Other antineoplastic agents
     L01XX72 Tazemetostat
      D11485  Tazemetostat hydrobromide (JAN/USAN) <JP/US>
USP drug classification [BR:br08302]
 Antineoplastics
  Antineoplastics, Other
   Tazemetostat
    D11485  Tazemetostat hydrobromide (JAN/USAN)
Therapeutic category of drugs in Japan [BR:br08301]
 4  Agents affecting cellular function
  42  Antineoplastics
   429  Miscellaneous
    4291  Other Antitumors
     D11485  Tazemetostat hydrobromide (JAN/USAN)
Drug groups [BR:br08330]
 Transporter substrate
  DG01665  ABCB1 substrate
   DG03020  Tazemetostat
    D11485  Tazemetostat hydrobromide
 Transporter inhibitor
  DG02864  SLC47A1 inhibitor
   DG03020  Tazemetostat
    D11485  Tazemetostat hydrobromide
  DG03110  SLC47A2 inhibitor
   DG03020  Tazemetostat
    D11485  Tazemetostat hydrobromide
Target-based classification of drugs [BR:br08310]
 Enzymes
  Transferases (EC2)
   Methyltransferases
    EZH2* [HSA_VAR:2146v1]
     D11485  Tazemetostat hydrobromide (JAN/USAN) <JP/US>
New drug approvals in the USA [br08319.html]
 New molecular entities and new therapeutic biological products
  D11485
New drug approvals in Japan [br08318.html]
 Drugs with new active ingredients
  D11485
New drug approvals in the USA, Europe and Japan [br08328.html]
 Approval dates by FDA, EMA and PMDA
  D11485
Drug metabolizing enzymes and transporters [br08309.html]
 Drug transporters
  D11485
Pharmacogenomic biomarkers [br08341.html]
 Somatic variations in targeted cancer therapies
  D11485
Drug groups [BR:br08330]
 Transporter substrate
  DG01665  ABCB1 substrate
   DG03020  Tazemetostat
 Transporter inhibitor
  DG02864  SLC47A1 inhibitor
   DG03020  Tazemetostat
  DG03110  SLC47A2 inhibitor
   DG03020  Tazemetostat
Other DBs
CAS: 1467052-75-0
PubChem: 384585461
KCF data

ATOM        43
            1   C1x C     8.9644  -12.3261
            2   O2x O     8.9644  -13.7268
            3   C1x C    10.1550  -14.4272
            4   C1x C    11.4157  -13.7268
            5   N1y N    11.4157  -12.3261
            6   C1x C    10.1550  -11.6258
            7   C1b C    12.6063  -11.6258
            8   C8y C    13.8669  -12.3261
            9   C8x C    13.8669  -13.7268
            10  C8x C    15.0575  -14.4272
            11  C8y C    16.2481  -13.7268
            12  C8x C    16.2481  -12.3261
            13  C8x C    15.0575  -11.6258
            14  C8y C    17.5087  -14.4272
            15  C8x C    17.5087  -15.8279
            16  C8y C    18.6993  -16.5282
            17  C8y C    19.8899  -15.8279
            18  C8y C    19.8899  -14.4272
            19  C8x C    18.6993  -13.7268
            20  C5a C    21.0805  -13.7268
            21  N1b N    22.3411  -14.4272
            22  O5a O    21.0805  -12.3261
            23  C1b C    23.5317  -13.7268
            24  C8y C    24.7223  -14.4272
            25  C8y C    24.7223  -15.8279
            26  N4x N    25.9129  -16.5282
            27  C8y C    27.1034  -15.8279
            28  C8x C    27.1034  -14.4272
            29  C8y C    25.9129  -13.7268
            30  C1a C    25.9129  -12.3261
            31  C1a C    28.3641  -16.5282
            32  O5x O    23.4616  -16.5282
            33  C1a C    21.1505  -16.5282
            34  N1c N    18.6993  -17.9289
            35  C1y C    19.8899  -18.6292
            36  C1b C    17.5087  -18.6292
            37  C1x C    19.8899  -20.0299
            38  C1x C    21.1505  -20.7303
            39  O2x O    22.3411  -20.0299
            40  C1x C    22.3411  -18.6292
            41  C1x C    21.1505  -17.9289
            42  C1a C    16.3181  -17.9289
            43  X   Br   28.2100  -20.3700
BOND        46
            1     1   2 1
            2     2   3 1
            3     3   4 1
            4     4   5 1
            5     5   6 1
            6     1   6 1
            7     5   7 1
            8     7   8 1
            9     8   9 2
            10    9  10 1
            11   10  11 2
            12   11  12 1
            13   12  13 2
            14    8  13 1
            15   11  14 1
            16   14  15 2
            17   15  16 1
            18   16  17 2
            19   17  18 1
            20   18  19 2
            21   14  19 1
            22   18  20 1
            23   20  21 1
            24   20  22 2
            25   21  23 1
            26   23  24 1
            27   24  25 1
            28   25  26 1
            29   26  27 1
            30   27  28 2
            31   28  29 1
            32   24  29 2
            33   29  30 1
            34   27  31 1
            35   25  32 2
            36   17  33 1
            37   16  34 1
            38   34  35 1
            39   34  36 1
            40   35  37 1
            41   37  38 1
            42   38  39 1
            43   39  40 1
            44   40  41 1
            45   35  41 1
            46   36  42 1