Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTMH124)

• DTT Name: Cytochrome P450 2B6 (CYP2B6)
• Synonyms: Cytochrome P450 IIB1; CYPIIB6; 1,4-cineole 2-exo-monooxygenase
• Gene Name: CYP2B6
• DTT Type: Literature-reported target; [1]
• BioChemical Class: Paired donor oxygen oxidoreductase
• UniProt ID: CP2B6_HUMAN
• TTD ID: T11793
• EC Number: EC 1.14.13.-
• Sequence:
  MELSVLLFLALLTGLLLLLVQRHPNTHDRLPPGPRPLPLLGNLLQMDRRGLLKSFLRFRE
  KYGDVFTVHLGPRPVVMLCGVEAIREALVDKAEAFSGRGKIAMVDPFFRGYGVIFANGNR
  WKVLRRFSVTTMRDFGMGKRSVEERIQEEAQCLIEELRKSKGALMDPTFLFQSITANIIC
  SIVFGKRFHYQDQEFLKMLNLFYQTFSLISSVFGQLFELFSGFLKYFPGAHRQVYKNLQE
  INAYIGHSVEKHRETLDPSAPKDLIDTYLLHMEKEKSNAHSEFSHQNLNLNTLSLFFAGT
  ETTSTTLRYGFLLMLKYPHVAERVYREIEQVIGPHRPPELHDRAKMPYTEAVIYEIQRFS
  DLLPMGVPHIVTQHTSFRGYIIPKDTEVFLILSTALHDPHYFEKPDAFNPDHFLDANGAL
  KKTEAFIPFSLGKRICLGEGIARAELFLFFTTILQNFSMASPVAPEDIDLTPQECGVGKI
  PPTYQIRFLPR
• Function: In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase. Cytochromes P450 are a group of heme-thiolate monooxygenases.
• KEGG Pathway:
  Arachidonic acid metabolism (hsa00590)
  Retinol metabolism (hsa00830)
  Metabolism of xenobiotics by cytochrome P450 (hsa00980)
  Drug metabolism - cytochrome P450 (hsa00982)
  Metabolic pathways (hsa01100)
  Chemical carcinogenesis - receptor activation (hsa05207)
  Lipid and atherosclerosis (hsa05417)
• Reactome Pathway:
  Xenobiotics (R-HSA-211981)
  CYP2E1 reactions (R-HSA-211999)
  Fatty acids (R-HSA-211935)
• BioCyc Pathway: MetaCyc:HS09587-MON

The Drug-Metabolizing Enzyme (DME) Role of This DTT

• DTT DME Name: Cytochrome P450 2B6 (CYP2B6) DME Info
• Gene Name: CYP2B6

86 Approved Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Amitriptyline	DMK7F9S	Depression	6A70-6A7Z	Approved	[2]
Artemether	DM48QOT	Malaria	1F40-1F45	Approved	[3]
Artemisinin	DMOY7W3	Malaria	1F40-1F45	Approved	[4]
Benzphetamine	DMIJATC	Obesity	5B81	Approved	[5]
Brivaracetam	DMSEPK8	Complex partial seizure	8A68.0	Approved	[6]
Bupropion	DM5PCS7	Depression	6A70-6A7Z	Approved	[7]
Capsaicin	DMGMF6V	Back pain	ME84.Z	Approved	[8]
Carbamazepine	DMZOLBI	Epilepsy	8A60-8A68	Approved	[9]
Cenobamate	DM8KLU9	Complex partial seizure	8A68.0	Approved	[10]
Cinnarizine	DM7U5QJ	Meniere disease	AB31.0	Approved	[11]
Cisapride	DMY7PED	Gastroesophageal reflux disease	DA22.Z	Approved	[12]
Clobazam - Lundbeck	DMW1OQ0	Anxiety disorder	6B00-6B0Z	Approved	[13]
Clofibrate	DMPC1J7	Dysbetalipoproteinemia	5C80.2	Approved	[14]
Clopidogrel	DMOL54H	Acute coronary syndrome	BA41	Approved	[15]
Clotiazepam	DM59AZT	Anxiety disorder	6B00-6B0Z	Approved	[16]
Cyclophosphamide	DM4O2Z7	Advanced cancer	2A00-2F9Z	Approved	[17]
Desipramine	DMT2FDC	Attention deficit hyperactivity disorder	6A05.Z	Approved	[18]
Dextromethorphan	DMUDJZM	Allergic rhinitis	CA08.0	Approved	[19]
Diazepam	DM08E9O	Alcohol withdrawal		Approved	[20]
Diclofenac	DMPIHLS	Chronic renal failure	GB61.Z	Approved	[21]
Domperidone	DMBDPY0	Gastrointestinal disease	DE2Z	Approved	[22]
Efavirenz	DMC0GSJ	Human immunodeficiency virus infection	1C62	Approved	[23]
Enasidenib	DM8QXOC	N. A.	N. A.	Approved	[24]
Epinastine	DMX0K3Q	Allergic conjunctivitis	9A60.02	Approved	[25]
Estrone	DM5T6US	Acne vulgaris	ED80	Approved	[26]
Fexinidazole	DMOYE70	African trypanosomiasis	1F51	Approved	[27]
Flunitrazepam	DMGR5Z3	Insomnia	7A00-7A0Z	Approved	[28]
Fluoxetine	DM3PD2C	Bipolar depression		Approved	[29]
Halothane	DM80OZ5	Anaesthesia	9A78.6	Approved	[30]
Hydrocodone bitartrate	DMIAPBE	N. A.	N. A.	Approved	[31]
Ifosfamide	DMCT3I8	Adult central nervous system germ cell tumor		Approved	[32]
Imipramine	DM2NUH3	Depression	6A70-6A7Z	Approved	[33]
Irinotecan	DMP6SC2	Adenocarcinoma	2D40	Approved	[18]
Isoflurane	DMY6T31	Anaesthesia	9A78.6	Approved	[34]
Istradefylline	DM20VSK	Parkinson disease	8A00.0	Approved	[35]
Ketamine	DMT5HA4	Anaesthesia	9A78.6	Approved	[36]
Ketobemidone	DMM3L6Z	Pain	MG30-MG3Z	Approved	[37]
Lidocaine	DML4ZOT	Anaesthesia	9A78.6	Approved	[3]
Loperamide	DMOJZQ9	Diarrhea	ME05.1	Approved	[38]
Loratadine	DMF3AN7	Allergy	4A80-4A85	Approved	[39]
Lorcaserin	DMG6OYJ	Obesity	5B81	Approved	[40]
Malathion	DMXZ84M	Pediculus capitis infestation	1G00.0	Approved	[41]
Meperidine	DMX4GND	Pain	MG30-MG3Z	Approved	[3]
Mephenytoin	DM5UGDK	Epilepsy	8A60-8A68	Approved	[11]
Methadone	DMTW6IU	Advanced cancer	2A00-2F9Z	Approved	[42]
Methoxyflurane	DML0RAE	Anaesthesia	9A78.6	Approved	[43]
Methylphenobarbital	DMDSWAG	Anxiety		Approved	[44]
Methyltestosterone	DMWLFGO	Advanced cancer	2A00-2F9Z	Approved	[45]
Mexiletine	DMCTE9R	Ventricular tachycardia	BC71	Approved	[46]
Mianserin	DMVKA4O	Depression	6A70-6A7Z	Approved	[30]
Midazolam	DMXOELT	Agitation	6A70.3	Approved	[47]
MLN9708	DMCMETN	Amyloidosis	5D00	Approved	[48]
Nevirapine	DM6HX9B	Human immunodeficiency virus infection	1C62	Approved	[49]
Nicotine	DMWX5CO	Lung cancer	2C25.0	Approved	[50]
Ospemifene	DMC4GEI	Dyspareunia	GA12	Approved	[51]
Perhexiline	DMINO7Z	Angina pectoris	BA40	Approved	[52]
Permethrin	DMZ0Q1G	Pediculus capitis infestation	1G00.0	Approved	[53]
Phenobarbital	DMXZOCG	Cluster headache	8A81.0	Approved	[9]
Phenytoin	DMNOKBV	Epilepsy	8A60-8A68	Approved	[54]
Prasugrel	DM7MT6E	Acute coronary syndrome	BA41	Approved	[55]
Promethazine	DM6I5GR	Hyperemesis gravidarum		Approved	[30]
Propofol	DMB4OLE	Anaesthesia	9A78.6	Approved	[56]
Rifampicin	DM5DSFZ	Non-insulin dependent diabetes	5A11	Approved	[57]
Ritonavir	DMU764S	Human immunodeficiency virus infection	1C62	Approved	[23]
Romidepsin	DMT5GNL	Cutaneous T-cell lymphoma	2B01	Approved	[58]
Ropivacaine	DMSPJG2	Anaesthesia	9A78.6	Approved	[34]
Selegiline Hydrochloride	DM3VR1L	Parkinson disease	8A00.0	Approved	[59]
Sertraline	DM0FB1J	Coronary heart disease	BA80.Z	Approved	[60]
Sevoflurane	DMC9O43	Anaesthesia	9A78.6	Approved	[34]
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[61]
Temazepam	DM02A65	Insomnia	7A00-7A0Z	Approved	[62]
Testosterone cypionate	DMC1TEV	N. A.	N. A.	Approved	[3]
Testosterone enanthate	DMB6871	N. A.	N. A.	Approved	[3]
Testosterone undecanoate	DMZO10Y	Hypogonadism	5A61.0	Approved	[3]
Thalidomide	DM70BU5	Adult T-cell leukemia/lymphoma		Approved	[63]
Tramadol	DMRQD04	Osteoarthritis	FA00-FA05	Approved	[64]
Tretinoin	DM49DUI	Acne vulgaris	ED80	Approved	[34]
Trifarotene	DMOL793	Acne vulgaris	ED80	Approved	[65]
Trofosfamide	DMHB2C3	Non-hodgkin lymphoma	2B33.5	Approved	[66]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[3]
Velpatasvir	DMGF8ZQ	N. A.	N. A.	Approved	[67]
Verapamil	DMA7PEW	Angina pectoris	BA40	Approved	[34]
Vonoprazan	DMO6315	Helicobacter infection	DA42-DA63	Approved	[68]
Vortioxetine	DM6F1PU	Major depressive disorder	6A70.3	Approved	[69]
Voxelotor	DMCS6M5	Sickle-cell disorder	3A51	Approved	[70]
ZOTEPINE	DMF3VXA	Anxiety disorder	6B00-6B0Z	Approved	[71]

6 Clinical Trial Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Clomethiazole	DMSPN58	Stroke	8B20	Phase 3	[34]
Esketamine	DMVU687	Depression	6A70-6A7Z	Phase 3	[36]
BMS 650032	DMQI43G	Hepatitis C virus infection	1E51.1	Phase 2	[72]
Dexloxiglumide	DM52HUD	Pancreatic malfunction	DC30-DC3Z	Phase 2	[73]
R-roscovitine	DMSH108	Non-small-cell lung cancer	2C25.Y	Phase 2	[74]
H3B-6545	DMIFCY2	Breast cancer	2C60-2C65	Phase 1/2	[75]

3 Discontinued Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Seratrodast	DMPNTDL	Allergic asthma	CA23.0	Discontinued in Phase 3	[11]
FCP-3P1	DMTQLIJ	Arteriosclerosis	BD40	Discontinued in Phase 2	[76]
Banoxantrone	DMK5I07	Acute lymphoblastic leukaemia	2A85	Discontinued in Phase 1	[77]

3 Investigative Drug(s) Metabolized by This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ethylmorphine	DM0YROF	Discovery agent	N.A.	Investigative	[20]
Levoverbenone	DMV3P89	N. A.	N. A.	Investigative	[78]
Phenazone	DMCE985	Discovery agent	N.A.	Investigative	[79]

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