General Information of Drug (ID: DMARQE0)

Drug Name
Radafaxine Drug Info
Synonyms Hydroxybupropion
Indication
Disease Entry ICD 11 Status REF
Major depressive disorder 6A70.3 Discontinued in Phase 2 [1]
Cross-matching ID
PubChem CID
9795056
CAS Number
CAS 192374-14-4
TTD Drug ID
DMARQE0
VARIDT Drug ID
DR01455

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [4]
Amitriptyline DMK7F9S Depression 6A70-6A7Z Approved [5]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [6]
Desipramine DMT2FDC Attention deficit hyperactivity disorder 6A05.Z Approved [4]
Cocaine DMSOX7I Anaesthesia 9A78.6 Approved [7]
Bupropion DM5PCS7 Depression 6A70-6A7Z Approved [8]
Tapentadol hydrochloride DMXLSH3 Acute pain MG31 Approved [9]
Venlafaxine DMR6QH0 Anxiety disorder 6B00-6B0Z Approved [8]
Trimipramine DM1SC8M Major depressive disorder 6A70.3 Approved [10]
Duloxetine DM9BI7M Depression 6A70-6A7Z Approved [11]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Dopamine transporter (DAT)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cocaine DMSOX7I Anaesthesia 9A78.6 Approved [7]
Dasotraline DMLDQFV Attention deficit hyperactivity disorder 6A05.Z Approved [12]
Methylphenidate DM7SJD6 Attention deficit hyperactivity disorder 6A05.Z Approved [13]
Modafinil DMYILBE Malignant glioma 2A00.0 Approved [14]
Phenmetrazine DMXYTN9 Obesity 5B81 Approved [15]
Ioflupane i-123 DMNARJT Parkinson disease 8A00.0 Approved [16]
DEXMETHYLPHENIDATE HYDROCHLORIDE DM8WBAH Attention deficit hyperactivity disorder 6A05.Z Approved [17]
Altropane DMO9WDS Attention deficit hyperactivity disorder 6A05.Z Approved [18]
Amitifadine DMS1X67 Obesity 5B81 Phase 3 [19]
NAV5001 DMRSI1M Dementia 6D80-6D86 Phase 3 [18]
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Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [20]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [21]
Methotrexate DM2TEOL Anterior urethra cancer Approved [22]
Folic Acid DMEMBJC Colorectal carcinoma Approved [23]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [22]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [22]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [24]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [22]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [25]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [26]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Cytochrome P450 2B6 (CYP2B6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [27]
Ritonavir DMU764S Human immunodeficiency virus infection 1C62 Approved [28]
Rifampicin DM5DSFZ Non-insulin dependent diabetes 5A11 Approved [29]
Thalidomide DM70BU5 Adult T-cell leukemia/lymphoma Approved [30]
Phenytoin DMNOKBV Epilepsy 8A60-8A68 Approved [31]
Clopidogrel DMOL54H Acute coronary syndrome BA41 Approved [32]
Artemisinin DMOY7W3 Malaria 1F40-1F45 Approved [33]
Malathion DMXZ84M Pediculus capitis infestation 1G00.0 Approved [34]
Phenobarbital DMXZOCG Cluster headache 8A81.0 Approved [35]
Permethrin DMZ0Q1G Pediculus capitis infestation 1G00.0 Approved [36]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Dopamine transporter (DAT) TTVBI8W SC6A3_HUMAN Inhibitor [1]
Norepinephrine transporter (NET) TTAWNKZ SC6A2_HUMAN Inhibitor [1]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Cytochrome P450 2B6 (CYP2B6) OTOYO4S7 CP2B6_HUMAN Biotransformations [3]

References

1 Emerging drugs for bipolar disorder. Expert Opin Emerg Drugs. 2006 Nov;11(4):621-34.
2 Sertraline and its metabolite desmethylsertraline, but not bupropion or its three major metabolites, have high affinity for P-glycoprotein. Biol Pharm Bull. 2008 Feb;31(2):231-4.
3 Validated assays for human cytochrome P450 activities. Drug Metab Dispos. 2004 Jun;32(6):647-60.
4 Augmentation effect of combination therapy of aripiprazole and antidepressants on forced swimming test in mice. Psychopharmacology (Berl). 2009 Sep;206(1):97-107.
5 Treatment of comorbid pain with serotonin norepinephrine reuptake inhibitors. CNS Spectr. 2008 Jul;13(7 Suppl 11):22-6.
6 Invivo antioxidant status: a putative target of antidepressant action. Prog Neuropsychopharmacol Biol Psychiatry. 2009 Mar 17;33(2):220-8.
7 Differential involvement of the norepinephrine, serotonin and dopamine reuptake transporter proteins in cocaine-induced taste aversion. Pharmacol Biochem Behav. 2009 Jul;93(1):75-81.
8 Clinically relevant drug interactions with new generation antidepressants and antipsychotics. Ther Umsch. 2009 Jun;66(6):485-92.
9 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
10 Antidepressants suppress production of the Th1 cytokine interferon-gamma, independent of monoamine transporter blockade. Eur Neuropsychopharmacol. 2006 Oct;16(7):481-90.
11 Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42.
12 Dasotraline for the Treatment of Attention-Deficit/Hyperactivity Disorder: A Randomized, Double-Blind, Placebo-Controlled, Proof-of-Concept Trial in Adults. Neuropsychopharmacology. 2015 Nov;40(12):2745-52.
13 Imaging the effects of methylphenidate on brain dopamine: new model on its therapeutic actions for attention-deficit/hyperactivity disorder. Biol Psychiatry. 2005 Jun 1;57(11):1410-5.
14 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
15 Interaction of the anorectic medication, phendimetrazine, and its metabolites with monoamine transporters in rat brain. Eur J Pharmacol. 2002 Jun 28;447(1):51-7.
16 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
17 Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate. J Med Chem. 2007 May 31;50(11):2718-31.
18 Rapid detection of Parkinson's disease by SPECT with altropane: a selective ligand for dopamine transporters. Synapse. 1998 Jun;29(2):128-41.
19 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 927).
20 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
21 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
22 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
23 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
24 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
25 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
26 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
27 Cytochrome P450 inhibition potential of new psychoactive substances of the tryptamine class. Toxicol Lett. 2016 Jan 22;241:82-94.
28 Transcriptional profiling suggests that Nevirapine and Ritonavir cause drug induced liver injury through distinct mechanisms in primary human hepatocytes. Chem Biol Interact. 2016 Aug 5;255:31-44.
29 Evaluation of gene induction of drug-metabolizing enzymes and transporters in primary culture of human hepatocytes using high-sensitivity real-time reverse transcription PCR. Yakugaku Zasshi. 2002 May;122(5):339-61.
30 Thalidomide increases human hepatic cytochrome P450 3A enzymes by direct activation of the pregnane X receptor. Chem Res Toxicol. 2014 Feb 17;27(2):304-308.
31 Human constitutive androstane receptor mediates induction of CYP2B6 gene expression by phenytoin. J Biol Chem. 2004 Jul 9;279(28):29295-301. doi: 10.1074/jbc.M400580200. Epub 2004 Apr 28.
32 Identification of novel agonists by high-throughput screening and molecular modelling of human constitutive androstane receptor isoform 3. Arch Toxicol. 2019 Aug;93(8):2247-2264. doi: 10.1007/s00204-019-02495-6. Epub 2019 Jul 16.
33 Antimalarial artemisinin drugs induce cytochrome P450 and MDR1 expression by activation of xenosensors pregnane X receptor and constitutive androstane receptor. Mol Pharmacol. 2005 Jun;67(6):1954-65.
34 Characterization of human cytochrome P450 induction by pesticides. Toxicology. 2012 Mar 29;294(1):17-26.
35 Species-specific mechanisms for cholesterol 7alpha-hydroxylase (CYP7A1) regulation by drugs and bile acids. Arch Biochem Biophys. 2005 Feb 1;434(1):75-85.
36 Pyrethroids: cytotoxicity and induction of CYP isoforms in human hepatocytes. Drug Metabol Drug Interact. 2008;23(3-4):211-36.