Belzutifan


Entry
D11954                      Drug                                   
Name
Belzutifan (JAN/USAN/INN);
Welireg (TN)
Product
WELIREG (Merck Sharp & Dohme LLC)
Formula
C17H12F3NO4S
Exact mass
383.0439
Mol weight
383.3417
Structure
Class
Metabolizing enzyme substrate
 DG01639  CYP2C19 substrate
 DG01633  CYP3A/CYP3A4 substrate
  DG02913  CYP3A4 substrate
 DG02924  UGT substrate
  DG03181  UGT2B17 substrate
Remark
ATC code: L01XX74
Product: D11954<US>
Efficacy
Antineoplastic, Hypoxia-inducible factor-2 alpha inhibitor
  Disease
von Hippel-Lindau disease-associated tumors [DS:H00559]
Target
HIF2A [HSA:2034] [KO:K09095]
  Pathway
hsa05200  Pathways in cancer
hsa05211  Renal cell carcinoma
Metabolism
Enzyme: UGT2B17 [HSA:7367], CYP2C19 [HSA:1557]; CYP3A4 [HSA:1576]
Interaction
Brite
Anatomical Therapeutic Chemical (ATC) classification [BR:br08303]
 L ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
  L01 ANTINEOPLASTIC AGENTS
   L01X OTHER ANTINEOPLASTIC AGENTS
    L01XX Other antineoplastic agents
     L01XX74 Belzutifan
      D11954  Belzutifan (JAN/USAN/INN) <US>
USP drug classification [BR:br08302]
 Antineoplastics
  Antineoplastics, Other
   Belzutifan
    D11954  Belzutifan (JAN/USAN/INN)
Drug groups [BR:br08330]
 Metabolizing enzyme substrate
  DG01639  CYP2C19 substrate
   D11954  Belzutifan
  DG01633  CYP3A/CYP3A4 substrate
   DG02913  CYP3A4 substrate
    D11954  Belzutifan
  DG02924  UGT substrate
   DG03181  UGT2B17 substrate
    D11954  Belzutifan
Target-based classification of drugs [BR:br08310]
 Not elsewhere classified
  Signaling molecules
   Transcription factor
    HIF2A
     D11954  Belzutifan (JAN/USAN/INN) <US>
New drug approvals in the USA [br08319.html]
 New molecular entities and new therapeutic biological products
  D11954
New drug approvals in the USA, Europe and Japan [br08328.html]
 Approval dates by FDA, EMA and PMDA
  D11954
Drug metabolizing enzymes and transporters [br08309.html]
 Drug metabolizing enzymes
  D11954
Pharmacogenomic biomarkers [br08341.html]
 Polymorphisms and mutations affecting drug response
  D11954
Other DBs
CAS: 1672668-24-4
PDB-CCD: 72Q[PDBj]
KCF data

ATOM        26
            1   C8x C    18.1393  -14.0809
            2   C8x C    18.1393  -15.4819
            3   C8y C    19.3526  -16.1824
            4   C8y C    20.5659  -15.4819
            5   C8y C    20.5659  -14.0809
            6   C8y C    19.3526  -13.3804
            7   C1y C    21.8984  -15.9148
            8   C1y C    22.7218  -14.7814
            9   C1y C    21.8984  -13.6480
            10  X   F    22.3298  -17.2426
            11  X   F    24.0935  -14.7814
            12  O1a O    22.3298  -12.3203
            13  S4a S    19.3526  -11.9796
            14  O3c O    17.9516  -11.9796
            15  O3c O    20.7536  -11.9796
            16  C1a C    19.3526  -10.5787
            17  O2a O    19.3526  -17.5832
            18  C8y C    18.1225  -18.2936
            19  C8x C    16.9176  -17.5980
            20  C8y C    15.7044  -18.2985
            21  C8x C    15.7045  -19.6995
            22  C8y C    16.9092  -20.3951
            23  C8x C    18.1225  -19.6946
            24  X   F    16.9090  -21.7861
            25  C3b C    14.4721  -17.5872
            26  N3a N    13.2587  -16.8867
BOND        28
            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 1
            9     8   9 1
            10    5   9 1
            11    7  10 1 #Down
            12    8  11 1 #Down
            13    9  12 1 #Down
            14    6  13 1
            15   13  14 2
            16   13  15 2
            17   13  16 1
            18    3  17 1
            19   17  18 1
            20   18  19 2
            21   19  20 1
            22   20  21 2
            23   21  22 1
            24   22  23 2
            25   18  23 1
            26   22  24 1
            27   20  25 1
            28   25  26 3