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CLOZAPINE Drug Record

  • Summary
  • Interactions
  • Claims
  • CLOZAPINE chembl:CHEMBL42 Approved

    Alternate Names:

    CLOZAPINE RESOLUTION MIXTURE
    HF-1854
    CLOZARIL
    FAZACLO
    VERSACLOZ
    ZAPONEX
    CLOZAPINE
    FAZACLO ODT
    CLOZAPIN
    CLOZAPINUM
    CLORAZIL®
    LEX123
    CLOZAPINA
    rxcui:2626
    drugbank:00363
    chembl:CHEMBL42
    chemidplus:5786-21-0
    pubchem.compound:2818

    Drug Info:

    Drug Categories gaba antagonists
    FDA Approval 1989
    Drug Class small molecule
    Drug Indications Antipsychotic Agents
    Drug Class antipsychotic agents
    Year of Approval 1989
    Drug Categories adrenergic alpha-1 receptor antagonists
    Drug Categories adrenergic alpha-antagonists
    Drug Categories adrenergic antagonists
    Drug Categories agents producing tachycardia
    Drug Categories agents that produce hypertension
    Drug Categories agents that reduce seizure threshold
    Drug Categories anticholinergic agents
    Drug Categories antidepressive agents
    Drug Categories cytochrome p-450 cyp1a2 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp2c19 inhibitors (strength unknown)
    Drug Categories cytochrome p-450 cyp2c19 inhibitors (weak)
    Drug Categories cytochrome p-450 cyp3a substrates
    Drug Categories cytochrome p-450 cyp3a4 inducers
    Drug Categories cytochrome p-450 cyp3a4 inducers (strength unknown)
    Drug Categories cytochrome p-450 cyp3a4 inhibitors
    Drug Categories cytochrome p-450 cyp3a4 inhibitors (moderate)
    Drug Categories cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
    Drug Categories cytochrome p-450 enzyme inducers
    Drug Categories cytochrome p-450 enzyme inhibitors
    Drug Categories cytochrome p-450 substrates
    Drug Categories dopamine antagonists
    Drug Categories dopamine d2 receptor antagonists
    Drug Categories drugs causing inadvertant photosensitivity
    Drug Categories drugs that are mainly renally excreted
    Drug Categories heterocyclic compounds, fused-ring
    Drug Categories histamine antagonists
    Drug Categories histamine h1 antagonists
    Drug Categories muscarinic antagonists
    Drug Categories neurotoxic agents
    Drug Categories p-glycoprotein substrates
    Drug Categories photosensitizing agents
    Drug Categories qtc prolonging agents
    Drug Categories serotonin 5-ht2 receptor antagonists
    Drug Categories serotonin receptor antagonists
    Drug Categories ugt1a4 substrates
    (7 More Sources)

    Publications:

    Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
    Li T et al., 1998, Case-control, haplotype relative risk and transmission disequilibrium analysis of a dopamine D2 receptor functional promoter polymorphism in schizophrenia., Schizophr Res
    Stonehouse et al., 2005, Bromocriptine and clozapine regulate dopamine 2 receptor gene expression in the mouse striatum., J. Mol. Neurosci.
    Müller DJ et al., 2012, Systematic analysis of dopamine receptor genes (DRD1-DRD5) in antipsychotic-induced weight gain., Pharmacogenomics J
    Wu et al., 2005, Response to chlorpromazine treatment may be associated with polymorphisms of the DRD2 gene in Chinese schizophrenic patients., Neurosci. Lett.
    Weizman et al., 2003, The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms., Eur. J. Pharmacol.
    Eum S et al., 2017, Pharmacogenetic evaluation to assess breakthrough psychosis with aripiprazole long-acting injection: a case report., BMC Psychiatry
    López-Rodríguez R et al., 2013, Pharmacodynamic genetic variants related to antipsychotic adverse reactions in healthy volunteers., Pharmacogenomics
    Bakker PR et al., 2008, Antipsychotic-induced tardive dyskinesia and polymorphic variations in COMT, DRD2, CYP1A2 and MnSOD genes: a meta-analysis of pharmacogenetic interactions., Mol Psychiatry
    Suzuki A et al., 2001, The -141C Ins/Del polymorphism in the dopamine D2 receptor gene promoter region is associated with anxiolytic and antidepressive effects during treatment with dopamine antagonists in schizophrenic patients., Pharmacogenetics
    Xing Q et al., 2007, The relationship between the therapeutic response to risperidone and the dopamine D2 receptor polymorphism in Chinese schizophrenia patients., Int J Neuropsychopharmacol
    Young et al., 2004, Prolactin levels in antipsychotic treatment of patients with schizophrenia carrying the DRD2*A1 allele., Br J Psychiatry
    Shen YC et al., 2009, Effects of DRD2/ANKK1 gene variations and clinical factors on aripiprazole efficacy in schizophrenic patients., J Psychiatr Res
    Lerman C et al., 2006, Role of functional genetic variation in the dopamine D2 receptor (DRD2) in response to bupropion and nicotine replacement therapy for tobacco dependence: results of two randomized clinical trials., Neuropsychopharmacology
    Li T et al., 2002, Allelic association analysis of the dopamine D2, D3, 5-HT2A, and GABA(A)gamma2 receptors and serotonin transporter genes with heroin abuse in Chinese subjects., Am J Med Genet
    Tresadern G et al., 2011, Molecular properties affecting fast dissociation from the D2 receptor., Bioorg Med Chem
    Batra S, 1976, Unconjugated estradiol in the myometrium of pregnancy., Endocrinology
    Yamanouchi Y et al., 2003, Effect of DRD2, 5-HT2A, and COMT genes on antipsychotic response to risperidone., Pharmacogenomics J
    Green et al., 2002, Treatment of schizophrenia and comorbid substance use disorder., Curr Drug Targets CNS Neurol Disord
    Alenius M et al., 2008, Gene polymorphism influencing treatment response in psychotic patients in a naturalistic setting., J Psychiatr Res
    Yasui-Furukori N et al., 2008, Association between dopamine-related polymorphisms and plasma concentrations of prolactin during risperidone treatment in schizophrenic patients., Prog Neuropsychopharmacol Biol Psychiatry
    Hong CJ et al., 2010, Dopamine receptor D2 gene is associated with weight gain in schizophrenic patients under long-term atypical antipsychotic treatment., Pharmacogenet Genomics
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Ohara K et al., 1998, Functional polymorphism of -141C Ins/Del in the dopamine D2 receptor gene promoter and schizophrenia., Psychiatry Res
    Hwang R et al., 2005, Association study of 12 polymorphisms spanning the dopamine D(2) receptor gene and clozapine treatment response in two treatment refractory/intolerant populations., Psychopharmacology (Berl)
    Sukasem C et al., 2016, Impact of Pharmacogenetic Markers of CYP2D6 and DRD2 on Prolactin Response in Risperidone-Treated Thai Children and Adolescents With Autism Spectrum Disorders., J Clin Psychopharmacol
    Zai CC et al., 2007, Meta-analysis of two dopamine D2 receptor gene polymorphisms with tardive dyskinesia in schizophrenia patients., Mol Psychiatry
    Lencz et al., 2006, DRD2 promoter region variation as a predictor of sustained response to antipsychotic medication in first-episode schizophrenia patients., Am J Psychiatry
    Takano et al., 2006, Time course of dopamine D2 receptor occupancy by clozapine with medium and high plasma concentrations., Prog. Neuropsychopharmacol. Biol. Psychiatry
    Roke Y et al., 2013, The effect of the Taq1A variant in the dopamine D₂ receptor gene and common CYP2D6 alleles on prolactin levels in risperidone-treated boys., Pharmacogenet Genomics
    Zhang JP et al., 2010, D2 receptor genetic variation and clinical response to antipsychotic drug treatment: a meta-analysis., Am J Psychiatry
    Arranz MJ et al., 1998, Lack of association between a polymorphism in the promoter region of the dopamine-2 receptor gene and clozapine response., Pharmacogenetics
    Lipska et al., 2003, Gene expression in dopamine and GABA systems in an animal model of schizophrenia: effects of antipsychotic drugs., Eur. J. Neurosci.
    Schmitt et al., 2003, Decreased gene expression of glial and neuronal glutamate transporters after chronic antipsychotic treatment in rat brain., Neurosci. Lett.
    Kuballa et al., Central effects of nafadotride, a dopamine D3 receptor antagonist, in rats. Comparison with haloperidol and clozapine., Pharmacol Rep
    Glatt et al., 2003, Schizophrenia is not associated with DRD4 48-base-pair-repeat length or individual alleles: results of a meta-analysis., Biol. Psychiatry
    Nakane et al., 2005, 2-[4-(3,4-Dimethylphenyl)piperazin-1-ylmethyl]-1H benzoimidazole (A-381393), a selective dopamine D4 receptor antagonist., Neuropharmacology
    Zhao et al., 2005, Dopamine D4 receptor gene exon III polymorphism and interindividual variation in response to clozapine., Int. J. Neurosci.
    Patel et al., 2003, Pharmacological and functional characterisation of dopamine D4 receptors in the rat retina., Neuropharmacology
    Hwang R et al., 2007, Association study of four dopamine D1 receptor gene polymorphisms and clozapine treatment response., J Psychopharmacol
    Tiwari AK et al., 2010, Association study of polymorphisms in cholecystokinin gene and its receptors with antipsychotic induced weight gain in schizophrenia patients., Prog Neuropsychopharmacol Biol Psychiatry
    Piatkov I et al., 2017, CYP2C19*17 protects against metabolic complications of clozapine treatment., World J Biol Psychiatry
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Roegge et al., 2007, Histamine H1 receptor involvement in prepulse inhibition and memory function: relevance for the antipsychotic actions of clozapine., Pharmacol. Biochem. Behav.
    Leysen et al., 1994, Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity., J Clin Psychiatry
    Kontkanen et al., 2002, Chronic antipsychotic drug treatment induces long-lasting expression of fos and jun family genes and activator protein 1 complex in the rat prefrontal cortex., Neuropsychopharmacology
    Houston JP et al., 2012, Pharmacogenomic associations with weight gain in olanzapine treatment of patients without schizophrenia., J Clin Psychiatry
    Ma X et al., 2014, HTR2C polymorphisms, olanzapine-induced weight gain and antipsychotic-induced metabolic syndrome in schizophrenia patients: a meta-analysis., Int J Psychiatry Clin Pract
    Mulder H et al., 2009, HTR2C gene polymorphisms and the metabolic syndrome in patients with schizophrenia: a replication study., J Clin Psychopharmacol
    Sicard MN et al., 2010, Polymorphisms of the HTR2C gene and antipsychotic-induced weight gain: an update and meta-analysis., Pharmacogenomics
    Navailles et al., 2006, Clozapine and haloperidol differentially alter the constitutive activity of central serotonin2C receptors in vivo., Biol. Psychiatry
    Sodhi et al., 2005, A rapid new assay to detect RNA editing reveals antipsychotic-induced changes in serotonin-2C transcripts., Mol. Pharmacol.
    Mulder H et al., 2007, The association between HTR2C gene polymorphisms and the metabolic syndrome in patients with schizophrenia., J Clin Psychopharmacol
    Risselada AJ et al., 2012, Association between HTR2C gene polymorphisms and the metabolic syndrome in patients using antipsychotics: a replication study., Pharmacogenomics J
    Opgen-Rhein C et al., 2010, Association of HTR2C, but not LEP or INSIG2, genes with antipsychotic-induced weight gain in a German sample., Pharmacogenomics
    Godlewska BR et al., 2009, Olanzapine-induced weight gain is associated with the -759C/T and -697G/C polymorphisms of the HTR2C gene., Pharmacogenomics J
    Mulder H et al., 2007, The association between HTR2C polymorphisms and obesity in psychiatric patients using antipsychotics: a cross-sectional study., Pharmacogenomics J
    Roth et al., 1994, Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors., J. Pharmacol. Exp. Ther.
    Lacivita E et al., 2012, Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo., J Med Chem
    Broderick et al., 2004, Clozapine and cocaine effects on dopamine and serotonin release in nucleus accumbens during psychostimulant behavior and withdrawal., Prog. Neuropsychopharmacol. Biol. Psychiatry
    McDonald et al., 2003, Enhancement of latent inhibition by two 5-HT2A receptor antagonists only when given at both pre-exposure and conditioning., Psychopharmacology (Berl.)
    Reist et al., 2004, Inter-relationships of intermediate phenotypes for serotonin function, impulsivity, and a 5-HT2A candidate allele: His452Tyr., Mol. Psychiatry
    Arranz et al., 1996, Analysis of a structural polymorphism in the 5-HT2A receptor and clinical response to clozapine., Neurosci. Lett.
    Goldstein, 1999, Quetiapine fumarate (Seroquel): a new atypical antipsychotic., Drugs Today
    Salloum NC et al., 2014, Towards the clinical implementation of pharmacogenetics in bipolar disorder., BMC Med
    Heiser et al., 2004, Effects of clozapine and its metabolites on the 5-HT2 receptor system in cortical and hippocampal cells in vitro., Prog. Neuropsychopharmacol. Biol. Psychiatry
    Travis et al., 1998, 5-HT2A receptor blockade in patients with schizophrenia treated with risperidone or clozapine. A SPET study using the novel 5-HT2A ligand 123I-5-I-R-91150., Br J Psychiatry
    Shao et al., 2006, Antipsychotic drugs cause glial cell line-derived neurotrophic factor secretion from C6 glioma cells., J Psychiatry Neurosci
    Dettling M et al., 2001, Genetic determinants of clozapine-induced agranulocytosis: recent results of HLA subtyping in a non-jewish caucasian sample., Arch Gen Psychiatry
    Hwang R et al., 2010, Effect of dopamine D3 receptor gene polymorphisms and clozapine treatment response: exploratory analysis of nine polymorphisms and meta-analysis of the Ser9Gly variant., Pharmacogenomics J
    Hwang R et al., 2011, Gene-gene interaction analyses between NMDA receptor subunit and dopamine receptor gene variants and clozapine response., Pharmacogenomics
    Smits et al., 2006, Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives., J. Med. Chem.
    Sugata et al., 2007, Histamine H4 receptor agonists have more activities than H4 agonism in antigen-specific human T-cell responses., Immunology
    Adachi et al., 2006, Suppression of ischemia/reperfusion liver injury by histamine H4 receptor stimulation in rats., Eur. J. Pharmacol.
    Hagino et al., 2002, Effects of clozapine on the efflux of serotonin and dopamine in the rat brain: the role of 5-HT1A receptors., Can. J. Physiol. Pharmacol.
    Newman-Tancredi et al., 2003, Comparison of hippocampal G protein activation by 5-HT(1A) receptor agonists and the atypical antipsychotics clozapine and S16924., Naunyn Schmiedebergs Arch. Pharmacol.
    Zahorodna et al., 2004, The influence of repeated administration of clozapine and haloperidol on the effects of the activation of 5-HT(1A), 5-HT(2) and 5-HT(4) receptors in rat frontal cortex., J. Physiol. Pharmacol.
    Bosia M et al., 2015, COMT Val158Met and 5-HT1A-R -1019 C/G polymorphisms: effects on the negative symptom response to clozapine., Pharmacogenomics
    Tomić et al., 2004, Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential., Bioorg. Med. Chem. Lett.
    Chou et al., 2003, Occupancy of 5-HT1A receptors by clozapine in the primate brain: a PET study., Psychopharmacology (Berl.)
    Valevski A et al., 1998, HLA-B38 and clozapine-induced agranulocytosis in Israeli Jewish schizophrenic patients., Eur J Immunogenet
    Saito T et al., 2016, Pharmacogenomic Study of Clozapine-Induced Agranulocytosis/Granulocytopenia in a Japanese Population., Biol Psychiatry
    Lieberman JA et al., 1990, HLA-B38, DR4, DQw3 and clozapine-induced agranulocytosis in Jewish patients with schizophrenia., Arch Gen Psychiatry
    Wittmann et al., 2005, Clozapine potentiation of N-methyl-D-aspartate receptor currents in the nucleus accumbens: role of NR2B and protein kinase A/Src kinases., J. Pharmacol. Exp. Ther.
    Mitjans M et al., 2015, Hypothalamic-pituitary-adrenal system, neurotrophic factors and clozapine response: association with FKBP5 and NTRK2 genes., Pharmacogenet Genomics
    Chetty et al., 2007, CYP-mediated clozapine interactions: how predictable are they?, Curr. Drug Metab.
    Dragovic S et al., 2013, Characterization of human cytochrome P450s involved in the bioactivation of clozapine., Drug Metab Dispos
    Nurmi EL et al., 2013, Moderation of antipsychotic-induced weight gain by energy balance gene variants in the RUPP autism network risperidone studies., Transl Psychiatry
    Tiwari AK et al., 2010, A common polymorphism in the cannabinoid receptor 1 (CNR1) gene is associated with antipsychotic-induced weight gain in Schizophrenia., Neuropsychopharmacology
    Monteleone P et al., 2010, Endocannabinoid Pro129Thr FAAH functional polymorphism but not 1359G/A CNR1 polymorphism is associated with antipsychotic-induced weight gain., J Clin Psychopharmacol
    Fernø et al., 2006, Drug-induced activation of SREBP-controlled lipogenic gene expression in CNS-related cell lines: marked differences between various antipsychotic drugs., BMC Neurosci
    Delacrétaz A et al., 2017, Association of variants in SH2B1 and RABEP1 with worsening of low-density lipoprotein and glucose parameters in patients treated with psychotropic drugs., Gene
    Brandl EJ et al., 2016, The role of the ITIH3 rs2535629 variant in antipsychotic response., Schizophr Res
    Rajkumar AP et al., 2012, Outcome definitions and clinical predictors influence pharmacogenetic associations between HTR3A gene polymorphisms and response to clozapine in patients with schizophrenia., Psychopharmacology (Berl)
    Souza RP et al., 2010, Influence of serotonin 3A and 3B receptor genes on clozapine treatment response in schizophrenia., Pharmacogenet Genomics
    Xu M et al., 2010, Pharacogenetic effects of dopamine transporter gene polymorphisms on response to chlorpromazine and clozapine and on extrapyramidal syndrome in schizophrenia., Prog Neuropsychopharmacol Biol Psychiatry
    Kang et al., 2004, The effects of clozapine on the GSK-3-mediated signaling pathway., FEBS Lett.
    Brandl EJ et al., 2014, Genetic variation in the GCG and in the GLP1R genes and antipsychotic-induced weight gain., Pharmacogenomics
    Dettling M et al., 2001, Further evidence of human leukocyte antigen-encoded susceptibility to clozapine-induced agranulocytosis independent of ancestry., Pharmacogenetics
    Szuster-Ciesielska et al., Neuroleptics modulate cytokine and reactive oxygen species production in blood leukocytes of healthy volunteers., Arch. Immunol. Ther. Exp. (Warsz.)
    Kobayashi et al., 2000, Inhibition by various antipsychotic drugs of the G-protein-activated inwardly rectifying K(+) (GIRK) channels expressed in xenopus oocytes., Br. J. Pharmacol.
    Kao AC et al., 2014, Methylenetetrahydrofolate reductase gene variants and antipsychotic-induced weight gain and metabolic disturbances., J Psychiatr Res
    Atmaca et al., 2003, Serum leptin and triglyceride levels in patients on treatment with atypical antipsychotics., J Clin Psychiatry
    Porcelli S et al., 2016, PDE7B, NMBR and EPM2A Variants and Schizophrenia: A Case-Control and Pharmacogenetics Study., Neuropsychobiology
    Malhotra AK et al., 2012, Association between common variants near the melanocortin 4 receptor gene and severe antipsychotic drug-induced weight gain., Arch Gen Psychiatry
    Czerwensky F et al., 2013, MC4R rs489693: a clinical risk factor for second generation antipsychotic-related weight gain?, Int J Neuropsychopharmacol
    Zhang JP et al., 2016, Pharmacogenetic Associations of Antipsychotic Drug-Related Weight Gain: A Systematic Review and Meta-analysis., Schizophr Bull
    Chowdhury NI et al., 2013, Genetic association study between antipsychotic-induced weight gain and the melanocortin-4 receptor gene., Pharmacogenomics J
    van der Weide K et al., 2017, Genetic risk factors for clozapine-induced neutropenia and agranulocytosis in a Dutch psychiatric population., Pharmacogenomics J
    Kohlrausch FB et al., 2010, Influence of serotonin transporter gene polymorphisms on clozapine response in Brazilian schizophrenics., J Psychiatr Res
    Lara et al., 2001, Chronic treatment with clozapine, but not haloperidol, increases striatal ecto-5'-nucleotidase activity in rats., Neuropsychobiology
    Taylor DL et al., 2016, Genetic association analysis of N-methyl-D-aspartate receptor subunit gene GRIN2B and clinical response to clozapine., Hum Psychopharmacol
    Lieberman et al., 1994, Predictors of response to clozapine., J Clin Psychiatry
    Brandl EJ et al., 2013, Exploratory study on association of genetic variation in TBC1D1 with antipsychotic-induced weight gain., Hum Psychopharmacol
    Jaquenoud Sirot E et al., 2009, ABCB1 and cytochrome P450 polymorphisms: clinical pharmacogenetics of clozapine., J Clin Psychopharmacol
    Palma BB et al., 2010, Functional characterization of eight human cytochrome P450 1A2 gene variants by recombinant protein expression., Pharmacogenomics J
    Bolla E et al., 2011, Are CYP1A2*1F and *1C associated with clozapine tolerability?: a preliminary investigation., Psychiatry Res
    Kohlrausch FB et al., 2013, The CYP1A2 -163C>A polymorphism is associated with clozapine-induced generalized tonic-clonic seizures in Brazilian schizophrenia patients., Psychiatry Res
    Lee ST et al., 2012, Association study of 27 annotated genes for clozapine pharmacogenetics: validation of preexisting studies and identification of a new candidate gene, ABCB1, for treatment response., J Clin Psychopharmacol
    Erickson-Ridout KK et al., 2012, Glucuronidation of the second-generation antipsychotic clozapine and its active metabolite N-desmethylclozapine. Potential importance of the UGT1A1 A(TA)₇TAA and UGT1A4 L48V polymorphisms., Pharmacogenet Genomics
    Zhang C et al., 2017, Complement 3 and metabolic syndrome induced by clozapine: a cross-sectional study and retrospective cohort analysis., Pharmacogenomics J
    Boerma JS et al., 2011, Application of CYP102A1M11H as a tool for the generation of protein adducts of reactive drug metabolites., Chem Res Toxicol
  • CLOZAPINE   JUND

    Interaction Score: 1.42

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12093589


    Sources:
    NCI

  • CLOZAPINE   TBC1D1

    Interaction Score: 0.71

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23364847


    Sources:
    PharmGKB

  • CLOZAPINE   HLA-DPB1

    Interaction Score: 0.71

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11266078


    Sources:
    PharmGKB

  • CLOZAPINE   ANKK1

    Interaction Score: 0.49

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20714340 23859574 18180754 18086475 18579277 26872113 17767146 23851570


    Sources:
    PharmGKB

  • CLOZAPINE   HLA-DRB3

    Interaction Score: 0.47

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11266078


    Sources:
    PharmGKB

  • CLOZAPINE   CALY

    Interaction Score: 0.47

    Interaction Types & Directionality:
    other/unknown

    Interaction Info:

    PMIDs:
    11752352


    Sources:
    DrugBank

  • CLOZAPINE   ITIH3

    Interaction Score: 0.47

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27396837


    Sources:
    PharmGKB

  • CLOZAPINE   HLA-DRB5

    Interaction Score: 0.36

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11146763


    Sources:
    PharmGKB

  • CLOZAPINE   MC4R

    Interaction Score: 0.24

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22566560 23799528 23920449 27217270 22310352


    Sources:
    PharmGKB

  • CLOZAPINE   C3

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26503818


    Sources:
    PharmGKB

  • CLOZAPINE   EPM2A

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27092952


    Sources:
    PharmGKB

  • CLOZAPINE   GDNF

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    16496033


    Sources:
    NCI

  • CLOZAPINE   DTNBP1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    PharmGKB

  • CLOZAPINE   KCNJ3

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10780978


    Sources:
    NCI

  • CLOZAPINE   SLC1A1

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12873733


    Sources:
    NCI

  • CLOZAPINE   HRH4

    Interaction Score: 0.16

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Endogenous Drug? False
    Specific Action of the Ligand Antagonist
    Trial Name -

    PMIDs:
    16854056 17346280 11752352 16860312


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology

  • CLOZAPINE   RABEP1

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28694205


    Sources:
    PharmGKB

  • CLOZAPINE   SH2B1

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28694205


    Sources:
    PharmGKB

  • CLOZAPINE   DRD2

    Interaction Score: 0.14

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Novel drug target Established target
    Trial Name -
    Specific Action of the Ligand Antagonist

    PMIDs:
    9713903 15781964 20714340 15694263 14575800 28673279 23859574 18180754 11505224 17105675 15286066 18926547 16123753 11920858 21421319 991813 14610521 12769622 18086475 18579277 20375926 11752352 9858029 15830237 26872113 17767146 16513877 16040180 23851570 20194480 9918131 12887421


    Sources:
    NCI TEND DTC PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • CLOZAPINE   GSTT1

    Interaction Score: 0.13

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27168101


    Sources:
    PharmGKB

  • CLOZAPINE   HLA-C

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11266078


    Sources:
    PharmGKB

  • CLOZAPINE   FKBP5

    Interaction Score: 0.12

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25751398


    Sources:
    PharmGKB

  • CLOZAPINE   HLA-B

    Interaction Score: 0.11

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9587740 26876947 2222133


    Sources:
    PharmGKB

  • CLOZAPINE   DRD4

    Interaction Score: 0.11

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Endogenous Drug? False
    Specific Action of the Ligand Antagonist
    Novel drug target Established target

    PMIDs:
    15886414 13129658 15992586 16223700 11752352 12763097


    Sources:
    TEND TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • CLOZAPINE   NT5E

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    11490180


    Sources:
    NCI

  • CLOZAPINE   LEP

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12755665


    Sources:
    NCI

  • CLOZAPINE   GCG

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24624910


    Sources:
    PharmGKB

  • CLOZAPINE   HTR2C

    Interaction Score: 0.09

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Specific Action of the Ligand Inverse agonist

    PMIDs:
    22967772 25152019 19142101 21121776 16182256 15917433 17632216 20680028 20504252 19434072 17016522


    Sources:
    TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

  • CLOZAPINE   HTR7

    Interaction Score: 0.08

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Endogenous Drug? False
    Specific Action of the Ligand Inverse agonist

    PMIDs:
    7908055 22738316 17848919


    Sources:
    NCI DTC DrugBank GuideToPharmacology

  • CLOZAPINE   FASN

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17052361


    Sources:
    NCI

  • CLOZAPINE   CCKBR

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20732371


    Sources:
    PharmGKB

  • CLOZAPINE   CNR1

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23799528 20107430 20631561


    Sources:
    PharmGKB

  • CLOZAPINE   FAAH

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20631561


    Sources:
    PharmGKB

  • CLOZAPINE   HTR1E

    Interaction Score: 0.06

    Interaction Types & Directionality:
    agonist (activating)
    antagonist (inhibitory)

    Interaction Info:
    Endogenous Drug? False
    Specific Action of the Ligand Full agonist

    PMIDs:
    17848919


    Sources:
    DrugBank GuideToPharmacology

  • CLOZAPINE   HTR2A

    Interaction Score: 0.06

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inverse agonist
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    14687870 14530903 15037867 8916101 7520908 12973385 24885933 14751426 9926100


    Sources:
    NCI TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology ChemblInteractions

  • CLOZAPINE   GSTM1

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27168101


    Sources:
    PharmGKB

  • CLOZAPINE   HTR3A

    Interaction Score: 0.06

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17848919 22700043 20168265


    Sources:
    PharmGKB DrugBank

  • CLOZAPINE   MTHFR

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24725652


    Sources:
    PharmGKB

  • CLOZAPINE   HTR1A

    Interaction Score: 0.05

    Interaction Types & Directionality:
    agonist (activating)
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target
    Specific Action of the Ligand Full agonist

    PMIDs:
    12564641 12923612 15213359 25560469 15261283 12589516


    Sources:
    TEND PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

  • CLOZAPINE   PRL

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    7961556


    Sources:
    NCI

  • CLOZAPINE   DRD3

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    20029384 17848919 21332319


    Sources:
    PharmGKB DrugBank GuideToPharmacology

  • CLOZAPINE   HTR5A

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CLOZAPINE   HTR6

    Interaction Score: 0.04

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inverse agonist
    Endogenous Drug? False

    PMIDs:
    17848919


    Sources:
    DrugBank GuideToPharmacology

  • CLOZAPINE   COMT

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25560469


    Sources:
    PharmGKB

  • CLOZAPINE   UGT1A1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22565219


    Sources:
    PharmGKB

  • CLOZAPINE   IL2

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15053234


    Sources:
    NCI

  • CLOZAPINE   HTR1D

    Interaction Score: 0.03

    Interaction Types & Directionality:
    agonist (activating)
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Full agonist
    Endogenous Drug? False

    PMIDs:
    17848919


    Sources:
    DrugBank GuideToPharmacology

  • CLOZAPINE   DRD1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False
    Trial Name -

    PMIDs:
    17092969 11752352


    Sources:
    TEND DTC PharmGKB TdgClinicalTrial DrugBank GuideToPharmacology

  • CLOZAPINE   NTRK2

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    25751398


    Sources:
    PharmGKB

  • CLOZAPINE   HTR1B

    Interaction Score: 0.03

    Interaction Types & Directionality:
    agonist (activating)
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Full agonist
    Endogenous Drug? False

    PMIDs:
    17848919


    Sources:
    DrugBank GuideToPharmacology

  • CLOZAPINE   HRH1

    Interaction Score: 0.03

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False
    Trial Name -

    PMIDs:
    17382376 7520908 11752352


    Sources:
    TEND TdgClinicalTrial DrugBank GuideToPharmacology

  • CLOZAPINE   GRIN2B

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26876050


    Sources:
    PharmGKB

  • CLOZAPINE   GSTP1

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    21639118


    Sources:
    DrugBank

  • CLOZAPINE   HTR1F

    Interaction Score: 0.02

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Specific Action of the Ligand Full agonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CLOZAPINE   DRD5

    Interaction Score: 0.02

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CLOZAPINE   ADRA1B

    Interaction Score: 0.02

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    17848919


    Sources:
    DrugBank GuideToPharmacology

  • CLOZAPINE   SLC6A3

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20580759


    Sources:
    PharmGKB

  • CLOZAPINE   CHRM4

    Interaction Score: 0.02

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17848919


    Sources:
    DrugBank

  • CLOZAPINE   CHRM5

    Interaction Score: 0.02

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17848919


    Sources:
    DrugBank

  • CLOZAPINE   SLC6A4

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    20452607


    Sources:
    PharmGKB

  • CLOZAPINE   ADRA2B

    Interaction Score: 0.02

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17848919


    Sources:
    DrugBank

  • CLOZAPINE   SRC

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    15659539


    Sources:
    NCI

  • CLOZAPINE   CHRM1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    allosteric modulator
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Positive
    Endogenous Drug? False

    PMIDs:
    17848919


    Sources:
    DrugBank GuideToPharmacology

  • CLOZAPINE   ADRA2C

    Interaction Score: 0.01

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17848919


    Sources:
    DrugBank

  • CLOZAPINE   PIK3CG

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    14988008


    Sources:
    NCI

  • CLOZAPINE   ADRA1A

    Interaction Score: 0.01

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    17848919


    Sources:
    DrugBank GuideToPharmacology

  • CLOZAPINE   CHRM2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17848919


    Sources:
    DrugBank

  • CLOZAPINE   ABCB1

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27168101 19593168 22722500


    Sources:
    PharmGKB

  • CLOZAPINE   ADRA2A

    Interaction Score: 0.01

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17848919


    Sources:
    DrugBank

  • CLOZAPINE   CHRM3

    Interaction Score: 0.01

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:

    PMIDs:
    17848919


    Sources:
    DrugBank

  • CLOZAPINE   ADRA1D

    Interaction Score: 0.01

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CLOZAPINE   GLP1R

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24624910


    Sources:
    PharmGKB

  • CLOZAPINE   HTR2B

    Interaction Score: 0.01

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CLOZAPINE   CYP1A2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300 19593168 20125119 21481946 23601795


    Sources:
    DTC PharmGKB

  • CLOZAPINE   CYP2C19

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28664816 22931300


    Sources:
    DTC PharmGKB

  • CLOZAPINE   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17504220 23297297 22931300


    Sources:
    NCI DTC PharmGKB

  • CLOZAPINE   CBX1

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CLOZAPINE   CYP2C9

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • CLOZAPINE   POLI

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CLOZAPINE   CYP2D6

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    FDA

  • DrugBank: DB00363

    • Version: 5.1.7

    Alternate Names:
    CLOZAPINE DrugBank Drug Name
    5786-21-0 CAS Number
    Aa-clozapine Drug Brand

    Drug Info:
    Drug Type small molecule
    Drug Groups approved
    Drug Categories adrenergic alpha-1 receptor antagonists

    Publications:
    Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
    Broderick et al., 2004, Clozapine and cocaine effects on dopamine and serotonin release in nucleus accumbens during psychostimulant behavior and withdrawal., Prog. Neuropsychopharmacol. Biol. Psychiatry
    McDonald et al., 2003, Enhancement of latent inhibition by two 5-HT2A receptor antagonists only when given at both pre-exposure and conditioning., Psychopharmacology (Berl.)

  • TEND: CLOZAPINE

    • Version: 01-August-2011

    Alternate Names:
    CLOZAPINE Primary Drug Name

    Drug Info:
    Year of Approval 1989
    Drug Class antipsychotic agents

    Publications:

  • TdgClinicalTrial: CLOZAPINE

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications Antipsychotic Agents
    Drug Class small molecule
    FDA Approval 1989

    Publications:

  • NCI: CLOZAPINE

    • Version: 14-September-2017

    Alternate Names:
    C28936 NCI drug code

    Drug Info:

    Publications:
    Lipska et al., 2003, Gene expression in dopamine and GABA systems in an animal model of schizophrenia: effects of antipsychotic drugs., Eur. J. Neurosci.
    Schmitt et al., 2003, Decreased gene expression of glial and neuronal glutamate transporters after chronic antipsychotic treatment in rat brain., Neurosci. Lett.
    Chetty et al., 2007, CYP-mediated clozapine interactions: how predictable are they?, Curr. Drug Metab.

  • DTC: CLOZAPINE

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL42 ChEMBL Drug ID

    Drug Info:

    Publications:
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Lacivita E et al., 2012, Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo., J Med Chem
    Tresadern G et al., 2011, Molecular properties affecting fast dissociation from the D2 receptor., Bioorg Med Chem

  • PharmGKB: clozapine

    • Version: 18-August-2020

    Alternate Names:

    Drug Info:

    Publications:
    Tiwari AK et al., 2010, Association study of polymorphisms in cholecystokinin gene and its receptors with antipsychotic induced weight gain in schizophrenia patients., Prog Neuropsychopharmacol Biol Psychiatry
    Li T et al., 1998, Case-control, haplotype relative risk and transmission disequilibrium analysis of a dopamine D2 receptor functional promoter polymorphism in schizophrenia., Schizophr Res
    Müller DJ et al., 2012, Systematic analysis of dopamine receptor genes (DRD1-DRD5) in antipsychotic-induced weight gain., Pharmacogenomics J

  • TTD: Clozapine

    • Version: 2020.06.01

    Alternate Names:
    D0Z1RV TTD Drug ID

    Drug Info:

    Publications:

  • GuideToPharmacology: 135650115

    • Version: 29-September-2020

    Alternate Names:
    CLOZAPINE GuideToPharmacology Ligand Name

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL42

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL42

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Clozapine

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21