KEGG   DRUG: Ezetimibe
Entry
D01966                      Drug                                   
Name
Ezetimibe (JAN/USP/INN);
Zetia (TN)
Product
ZETIA (Organon LLC)
  Generic
EZETIMIBE (A-S Medication Solutions), EZETIMIBE (A-S Medication Solutions), EZETIMIBE (A-S Medication Solutions), EZETIMIBE (A-S Medication Solutions), EZETIMIBE (A-S Medication Solutions), EZETIMIBE (Accord Healthcare), EZETIMIBE (Actavis Pharma), EZETIMIBE (American Health Packaging), EZETIMIBE (Amneal Pharmaceuticals NY LLC), EZETIMIBE (Ascend Laboratories), EZETIMIBE (Aurobindo Pharma Limited), EZETIMIBE (AvPAK), EZETIMIBE (Bryant Ranch Prepack), EZETIMIBE (Bryant Ranch Prepack), EZETIMIBE (Bryant Ranch Prepack), EZETIMIBE (Bryant Ranch Prepack), EZETIMIBE (Camber Pharmaceuticals), EZETIMIBE (Glenmark Pharmaceuticals), EZETIMIBE (Golden State Medical Supply), EZETIMIBE (Major Pharmaceuticals), EZETIMIBE (Marlex Pharmaceuticals), EZETIMIBE (NCS HealthCare of KY), EZETIMIBE (NorthStar Rx LLC), EZETIMIBE (Ohm Laboratories), EZETIMIBE (Orient Pharma), EZETIMIBE (Preferred Pharmaceuticals), EZETIMIBE (Proficient Rx LP), EZETIMIBE (Proficient Rx LP), EZETIMIBE (Proficient Rx LP), EZETIMIBE (Quallent Pharmaceuticals Health LLC), EZETIMIBE (REMEDYREPACK), EZETIMIBE (REMEDYREPACK), EZETIMIBE (REMEDYREPACK), EZETIMIBE (Sandoz), EZETIMIBE (ScieGen Pharmaceuticals), EZETIMIBE (Zydus Lifesciences Limited), EZETIMIBE (Zydus Pharmaceuticals USA)
Formula
C24H21F2NO3
Exact mass
409.149
Mol weight
409.4252
Structure
Class
Hypolipidemic agent
 DG01946  Hypolipidemic agent
Metabolizing enzyme substrate
 DG02924  UGT substrate
Transporter substrate
 DG02856  SLCO1B1 substrate
 DG02965  MRP2 substrate
Remark
Therapeutic category: 2189
ATC code: C10AX09
Product: D01966<JP/US>
Product (mixture): D10257<US> D10385<JP/US> D11520<JP/US> D12438<JP>
Efficacy
Antihyperlipidemic, Cholesterol absorption inhibitor
  Disease
Hyperlipidemia [DS:H01635]
Homozygous familial hypercholesterolemia [DS:H00155]
Homozygous sitosterolemia [DS:H00152]
Comment
Intestinal cholesterol absorption inhibitor
Target
NPC1L1 [HSA:29881] [KO:K14461]
  Pathway
hsa04975  Fat digestion and absorption
Metabolism
Enzyme: UGT [KO:K00699]
Transporter: SLCO1B1 [HSA:10599], MRP2 [HSA:1244]
Interaction
Structure map
map07052  Antidyslipidemic agents
Brite
Anatomical Therapeutic Chemical (ATC) classification [BR:br08303]
 C CARDIOVASCULAR SYSTEM
  C10 LIPID MODIFYING AGENTS
   C10A LIPID MODIFYING AGENTS, PLAIN
    C10AX Other lipid modifying agents
     C10AX09 Ezetimibe
      D01966  Ezetimibe (JAN/USP/INN) <JP/US>
USP drug classification [BR:br08302]
 Cardiovascular Agents
  Dyslipidemics, Other
   Ezetimibe
    D01966  Ezetimibe (JAN/USP/INN)
Therapeutic category of drugs in Japan [BR:br08301]
 2  Agents affecting individual organs
  21  Cardiovascular agents
   218  Hyperlipidemia agents
    2189  Others
     D01966  Ezetimibe (JAN/USP/INN)
Drug groups [BR:br08330]
 Hypolipidemic agent
  DG01946  Hypolipidemic agent
   D01966  Ezetimibe
 Metabolizing enzyme substrate
  DG02924  UGT substrate
   D01966  Ezetimibe
 Transporter substrate
  DG02856  SLCO1B1 substrate
   D01966  Ezetimibe
  DG02965  MRP2 substrate
   D01966  Ezetimibe
Drug classes [BR:br08332]
 Cardiovascular agent
  DG01946  Hypolipidemic agent
   D01966  Ezetimibe
Target-based classification of drugs [BR:br08310]
 Transporters
  Other transporters
   Others
    NPC1L1
     D01966  Ezetimibe (JAN/USP/INN) <JP/US>
New drug approvals in the USA [br08319.html]
 New molecular entities and new therapeutic biological products
  D01966
New drug approvals in Japan [br08318.html]
 Drugs with new active ingredients
  D01966
New drug approvals in the USA, Europe and Japan [br08328.html]
 Approval dates by FDA, EMA and PMDA
  D01966
Drug metabolizing enzymes and transporters [br08309.html]
 Drug metabolizing enzymes
  D01966
 Drug transporters
  D01966
Other DBs
CAS: 163222-33-1
PubChem: 7849028
ChEBI: 49040
PDB-CCD: H56[PDBj]
LigandBox: D01966
KCF data

ATOM        30
            1   C1y C    13.5100  -21.2800
            2   C5x C    13.5100  -22.6800
            3   N1y N    14.9100  -22.6800
            4   C1y C    14.9100  -21.2800
            5   O5x O    12.3200  -23.3800
            6   C8y C    16.1000  -23.3800
            7   C8x C    16.1000  -24.7800
            8   C8x C    17.3600  -25.4800
            9   C8y C    18.5500  -24.7800
            10  C8x C    18.5500  -23.3800
            11  C8x C    17.3600  -22.6800
            12  X   F    19.7400  -25.4800
            13  C8y C    16.1000  -20.5800
            14  C8x C    17.2900  -21.2800
            15  C8x C    18.5500  -20.5800
            16  C8y C    18.5500  -19.1800
            17  C8x C    17.3600  -18.4800
            18  C8x C    16.1000  -19.1800
            19  O1a O    19.7400  -18.4800
            20  C1b C    12.3200  -20.5800
            21  C1b C    11.1300  -21.2800
            22  C1c C     9.9400  -20.5800
            23  C8y C     8.7500  -21.2800
            24  O1a O     9.9400  -19.1800
            25  C8x C     7.5600  -20.5800
            26  C8x C     6.3000  -21.2800
            27  C8y C     6.3000  -22.6800
            28  C8x C     7.4900  -23.3800
            29  C8x C     8.7500  -22.6800
            30  X   F     5.1100  -23.3800
BOND        33
            1     1   2 1
            2     2   3 1
            3     3   4 1
            4     1   4 1
            5     5   2 2
            6     3   6 1
            7     6   7 2
            8     7   8 1
            9     8   9 2
            10    9  10 1
            11   10  11 2
            12    6  11 1
            13    9  12 1
            14    4  13 1 #Up
            15   13  14 2
            16   14  15 1
            17   15  16 2
            18   16  17 1
            19   17  18 2
            20   13  18 1
            21   16  19 1
            22    1  20 1 #Down
            23   20  21 1
            24   21  22 1
            25   22  23 1
            26   22  24 1 #Up
            27   23  25 2
            28   25  26 1
            29   26  27 2
            30   27  28 1
            31   28  29 2
            32   23  29 1
            33   27  30 1

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Disease (3)   
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