Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMHG57U)

Drug Name
OPC-34712 Drug Info
Synonyms Brexpiprazole
Indication
Disease Entry ICD 11 Status REF
Major depressive disorder 6A70.3 Approved [1]
Cross-matching ID
PubChem CID
11978813
ChEBI ID
CHEMBL2105760
CAS Number
CAS 913611-97-9
TTD Drug ID
DMHG57U
VARIDT Drug ID
DR01335
INTEDE Drug ID
DR0227
ACDINA Drug ID
D00076

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Download the Complete Related Drug List
Drug(s) Targeting Dopamine D2 receptor (D2R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [6]
Haloperidol DM96SE0 Delirium Approved [7]
Perphenazine DMA4MRX Schizophrenia 6A20 Approved [8]
Perazine DM2AOTZ Psychotic disorder 6A20-6A25 Approved [9]
Domperidone DMBDPY0 Gastrointestinal disease DE2Z Approved [10]
Levodopa DMN3E57 Parkinson disease 8A00.0 Approved [11]
Quetiapine DM1N62C Anorexia nervosa cachexia 6B80 Approved [12]
Pimozide DMW83TP Schizophrenia 6A20 Approved [13]
Chlorpromazine DMBGZI3 Acute intermittent hepatic porphyria 5C58.11 Approved [14]
Iloperidone DM6AUFY Schizophrenia 6A20 Approved [15]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting 5-HT 1A receptor (HTR1A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Trazodone DMK1GBJ Depression 6A70-6A7Z Approved [16]
Buspirone DMBS632 Anxiety disorder 6B00-6B0Z Approved [17]
Vilazodone DM4LECQ Major depressive disorder 6A70.3 Approved [18]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [19]
Gepirone DMGX5Q0 Major depressive disorder 6A70.3 Approved [20]
TERTATOLOL DM2L3D5 Hypertension BA00-BA04 Approved [21]
Urapidil DMD59GI Hypertension BA00-BA04 Approved [22]
Treximet DMU54QB Migraine 8A80 Approved [23]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [24]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [25]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Transported By Sodium-dependent dopamine transporter (SLC6A3)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [26]
Amphetamine DMSZQAK Attention deficit hyperactivity disorder 6A05.Z Approved [27]
Bretylium DM1FX74 Long QT syndrome BC65.0 Approved [28]
Benztropine DMGZOVN Parkinson disease 8A00.0 Approved [29]
Drug(s) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [30]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [31]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [32]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [33]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [34]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [35]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [36]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [37]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [31]
Verapamil DMA7PEW Angina pectoris BA40 Approved [38]
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Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [39]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [40]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [41]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [34]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [38]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [42]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [43]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [44]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [45]
Propranolol DM79NTF Angina pectoris BA40 Approved [46]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Stearoyl-CoA desaturase (SCD)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Clavulanate DM2FGRT Bacteremia 1A73 Approved [47]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [48]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [48]
Methotrexate DM2TEOL Anterior urethra cancer Approved [49]
Quercetin DM3NC4M Obesity 5B81 Approved [50]
Rofecoxib DM3P5DA Osteoarthritis FA00-FA05 Approved [51]
Fluoxetine DM3PD2C Bipolar depression Approved [48]
Fructose DM43AN2 Vomiting MD90 Approved [52]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [53]
Bupropion DM5PCS7 Depression 6A70-6A7Z Approved [48]
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Drug(s) Affected By Acetyl-CoA carboxylase 1 (ACACA)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [54]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [55]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [56]
Quercetin DM3NC4M Obesity 5B81 Approved [57]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [58]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [59]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [60]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [61]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [62]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [63]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas
Download the Complete Interaction Atlas for Visualization in Cytoscape

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
5-HT 1A receptor (HTR1A) TTSQIFT 5HT1A_HUMAN Modulator [2]
Dopamine D2 receptor (D2R) TTEX248 DRD2_HUMAN Modulator [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Sodium-dependent dopamine transporter (SLC6A3) DT3BA8L SC6A3_HUMAN Substrate [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [4]
Cytochrome P450 2D6 (CYP2D6) Main DME DECB0K3 CP2D6_HUMAN Substrate [4]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Acetyl-CoA carboxylase 1 (ACACA) OT5CQPZY ACACA_HUMAN Gene/Protein Processing [5]
Stearoyl-CoA desaturase (SCD) OTB1073G SCD_HUMAN Gene/Protein Processing [5]

References

1 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. (Ligand id: 7672).
2 Effects of brexpiprazole, a novel serotonin-dopamine activity modulator, on phencyclidine-induced cognitive deficits in mice: a role for serotonin 5-HT1A receptors.Pharmacol Biochem Behav.2014 Sep;124:245-9.
3 Brexpiprazole reduces hyperactivity, impulsivity, and risk-preference behavior in mice with dopamine transporter knockdown-a model of mania. Psychopharmacology (Berl). 2017 Mar;234(6):1017-1028.
4 Brexpiprazole: first global approval. Drugs. 2015 Sep;75(14):1687-97.
5 Brexpiprazole suppresses cell proliferation and de novo lipogenesis through AMPK/SREBP1 pathway in colorectal cancer. Environ Toxicol. 2023 Oct;38(10):2352-2360. doi: 10.1002/tox.23871. Epub 2023 Jun 22.
6 The Detection of Dopamine Gene Receptors (DRD1-DRD5) Expression on Human Peripheral Blood Lymphocytes by Real Time PCR. Iran J Allergy Asthma Immunol. 2004 Dec;3(4):169-74.
7 Dopaminergic synapses in the matrix of the ventrolateral striatum after chronic haloperidol treatment. Synapse. 2002 Aug;45(2):78-85.
8 CYP2D6 and DRD2 genes differentially impact pharmacodynamic sensitivity and time course of prolactin response to perphenazine. Pharmacogenet Genomics. 2007 Nov;17(11):989-93.
9 Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands. Bioorg Med Chem. 2005 Jan 3;13(1):77-87.
10 Screening of domperidone in wastewater by high performance liquid chromatography and solid phase extraction methods. Talanta. 2006 Jan 15;68(3):928-31.
11 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. (Ligand id: 3639).
12 Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors. Eur J Pharmacol. 2009 Apr 1;607(1-3):35-40.
13 [The benzamides tiapride, sulpiride, and amisulpride in treatment for Tourette's syndrome]. Nervenarzt. 2007 Mar;78(3):264, 266-8, 270-1.
14 Modulatory role of dopamine D2 receptors and fundamental role of L-type Ca2+ channels in the induction of long-term potentiation in the basolateral... Eur J Pharmacol. 2009 Mar 15;606(1-3):90-3.
15 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
16 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
17 Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
18 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
19 Radium 223 dichloride for prostate cancer treatment. Drug Des Devel Ther. 2017 Sep 6;11:2643-2651.
20 Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92.
21 Synthesis of new derivatives of 8-OH-DPAT: Influence of substitution on the aromatic ring on the pharmacological profile, Bioorg. Med. Chem. Lett. 3(10):2035-2038 (1993).
22 Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
23 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
24 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
25 Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
26 Characterization of VNTRs Within the Entire Region of SLC6A3 and Its Association with Hypertension. DNA Cell Biol. 2017 Mar;36(3):227-236.
27 Amphetamines, new psychoactive drugs and the monoamine transporter cycle. Trends Pharmacol Sci. 2015 Jan;36(1):41-50.
28 Which form of dopamine is the substrate for the human dopamine transporter: the cationic or the uncharged species? J Biol Chem. 1999 Feb 19;274(8):4876-82.
29 Pharmacological characterization of a dopamine transporter ligand that functions as a cocaine antagonist. J Pharmacol Exp Ther. 2014 Jan;348(1):106-15.
30 Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer. 2007 Mar 1;109(5):957-65.
31 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
32 Comprehensive evaluation of tamoxifen sequential biotransformation by the human cytochrome P450 system in vitro: prominent roles for CYP3A and CYP2D6. J Pharmacol Exp Ther. 2004 Sep;310(3):1062-75.
33 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
34 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
35 Potent mechanism-based inhibition of CYP3A4 by imatinib explains its liability to interact with CYP3A4 substrates. Br J Pharmacol. 2012 Apr;165(8):2787-98.
36 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
37 The metabolism of zidovudine by human liver microsomes in vitro: formation of 3'-amino-3'-deoxythymidine. Biochem Pharmacol. 1994 Jul 19;48(2):267-76.
38 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
39 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
40 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
41 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
42 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
43 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
44 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
45 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
46 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
47 Molecular mechanisms of hepatotoxic cholestasis by clavulanic acid: Role of NRF2 and FXR pathways. Food Chem Toxicol. 2021 Dec;158:112664. doi: 10.1016/j.fct.2021.112664. Epub 2021 Nov 9.
48 Antidepressant drugs activate SREBP and up-regulate cholesterol and fatty acid biosynthesis in human glial cells. Neurosci Lett. 2006 Mar 13;395(3):185-90. doi: 10.1016/j.neulet.2005.10.096. Epub 2005 Dec 1.
49 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
50 Comparison of phenotypic and transcriptomic effects of false-positive genotoxins, true genotoxins and non-genotoxins using HepG2 cells. Mutagenesis. 2011 Sep;26(5):593-604.
51 Rofecoxib modulates multiple gene expression pathways in a clinical model of acute inflammatory pain. Pain. 2007 Mar;128(1-2):136-47.
52 Effects of four-week high-fructose diet on gene expression in skeletal muscle of healthy men. Diabetes Metab. 2008 Feb;34(1):82-5. doi: 10.1016/j.diabet.2007.08.004. Epub 2007 Dec 11.
53 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
54 Antidepressant drug sertraline modulates AMPK-MTOR signaling-mediated autophagy via targeting mitochondrial VDAC1 protein. Autophagy. 2021 Oct;17(10):2783-2799. doi: 10.1080/15548627.2020.1841953. Epub 2020 Nov 9.
55 Minimal peroxide exposure of neuronal cells induces multifaceted adaptive responses. PLoS One. 2010 Dec 17;5(12):e14352. doi: 10.1371/journal.pone.0014352.
56 Drug-induced hepatic steatosis in absence of severe mitochondrial dysfunction in HepaRG cells: proof of multiple mechanism-based toxicity. Cell Biol Toxicol. 2021 Apr;37(2):151-175. doi: 10.1007/s10565-020-09537-1. Epub 2020 Jun 14.
57 Multifaceted preventive effects of single agent quercetin on a human prostate adenocarcinoma cell line (PC-3): implications for nutritional transcriptomics and multi-target therapy. Med Oncol. 2011 Dec;28(4):1395-404. doi: 10.1007/s12032-010-9603-3. Epub 2010 Jul 2.
58 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
59 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
60 Multi-parameter in vitro toxicity testing of crizotinib, sunitinib, erlotinib, and nilotinib in human cardiomyocytes. Toxicol Appl Pharmacol. 2013 Oct 1;272(1):245-55.
61 Adipocyte differentiation, mitochondrial gene expression and fat distribution: differences between zidovudine and tenofovir after 6 months. Antivir Ther. 2009;14(8):1089-100. doi: 10.3851/IMP1457.
62 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
63 Comparative effects of fructose and glucose on lipogenic gene expression and intermediary metabolism in HepG2 liver cells. PLoS One. 2011;6(11):e26583. doi: 10.1371/journal.pone.0026583. Epub 2011 Nov 11.