General Information of Drug (ID: DMGX5Q0)

Drug Name
Gepirone Drug Info
Synonyms
83928-76-1; 4,4-Dimethyl-1-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)piperidine-2,6-dione; Gepironum [Latin]; Gepirone [INN]; Gepirona [Spanish]; UNII-JW5Y7B8Z18; BMY-13805; JW5Y7B8Z18; CHEMBL284092; Gepironum; AK115965; Gepirona; Travivo; 2,6-Piperidinedione, 4,4-dimethyl-1-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-; BMY 13805; gepiron ER; MJ 13805-1; ORG-13011(Gepirone); AC1L1IK6; AC1Q6F8Q; 4,4-dimethyl-1-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-2,6-piperidinedione; 3,3-dimethyl-1-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]glutarimide; 4,4-dimethyl-1-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]piperidine-2,6-dione
Indication
Disease Entry ICD 11 Status REF
Major depressive disorder 6A70.3 Approved [1]
Depression 6A70-6A7Z Terminated [2]
Cross-matching ID
PubChem CID
55191
ChEBI ID
CHEBI:135990
CAS Number
CAS 83928-76-1
TTD Drug ID
DMGX5Q0
INTEDE Drug ID
DR0769

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Clinical Trial 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 [5]
Buspirone DMBS632 Anxiety disorder 6B00-6B0Z Approved [6]
OPC-34712 DMHG57U Major depressive disorder 6A70.3 Approved [7]
Vilazodone DM4LECQ Major depressive disorder 6A70.3 Approved [8]
Flibanserin DM70DTN Depression 6A70-6A7Z Approved [9]
TERTATOLOL DM2L3D5 Hypertension BA00-BA04 Approved [10]
Urapidil DMD59GI Hypertension BA00-BA04 Approved [11]
Treximet DMU54QB Migraine 8A80 Approved [12]
CM-2395 DMASPWR Schizophrenia 6A20 Phase 3 [13]
Eltoprazine DMW6C81 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [14]
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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 [3]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [15]
Methotrexate DM2TEOL Anterior urethra cancer Approved [16]
Folic Acid DMEMBJC Colorectal carcinoma Approved [17]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [16]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [16]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [18]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [16]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [19]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [20]
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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 [21]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [22]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [23]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [24]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [25]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [26]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [27]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [28]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [22]
Verapamil DMA7PEW Angina pectoris BA40 Approved [29]
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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 [30]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [31]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [32]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [25]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [29]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [33]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [34]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [35]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [36]
Propranolol DM79NTF Angina pectoris BA40 Approved [37]
⏷ 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
5-HT 1A receptor (HTR1A) TTSQIFT 5HT1A_HUMAN Agonist [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [3]

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

References

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6 Interactions between corticotropin-releasing hormone and serotonin: implications for the aetiology and treatment of anxiety disorders. Handb Exp Pharmacol. 2005;(169):181-204.
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11 Urapidil. A reappraisal of its use in the management of hypertension. Drugs. 1998 Nov;56(5):929-55.
12 Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
13 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031127)
14 Clinical pipeline report, company report or official report of Jazz Pharmaceuticals.
15 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
16 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.
17 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
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19 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
20 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.
21 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.
22 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
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24 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
25 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.
26 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.
27 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
28 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.
29 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.
30 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
31 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.
32 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
33 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.
34 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
35 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
36 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
37 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.