General Information of Drug (ID: DM7NPJS)

Drug Name
Paliperidone Drug Info
Synonyms
Xeplion; Invega Sustenna; Paliperidone palmitate; JNS-010; Paliperidone (depot injection, NanoCrystal); Paliperidone (injectable, NanoCrystal), Elan; Paliperidone (depot injection, NanoCrystal), Johnson & Johnson
Indication
Disease Entry ICD 11 Status REF
Psychotic disorder 6A20-6A25 Approved [1]
Schizoaffective disorder 6A21 Approved [1]
Schizophrenia 6A20 Approved [2]
Cross-matching ID
PubChem CID
115237
ChEBI ID
CHEBI:83804
CAS Number
CAS 144598-75-4
TTD Drug ID
DM7NPJS
VARIDT Drug ID
DR00159
INTEDE Drug ID
DR1230
ACDINA Drug ID
D00505

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting 5-HT receptor (5HTR)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metergolin DMJFP6G Hyperprolactinaemia 5A60.1 Approved [15]
Ramosetron DMH7GN8 Diarrhea-predominant irritable bowel syndrome DD91.01 Approved [15]
Pizotyline DMV74ZH Headache 8A80-8A84 Approved [3]
Tandospirone DMPHWU6 Anxiety disorder 6B00-6B0Z Approved [15]
Nafronyl DMVMQ1L Cerebrovascular ischaemia 8B1Z Approved [3]
ITI-007 DMUQ1DO Depression 6A70-6A7Z Phase 3 [16]
Fenfluramine DM0762O Dravet syndrome 8A61.11 Phase 3 [17]
MIN-117 DMSLIW6 Major depressive disorder 6A70.3 Phase 2 [16]
Lu-AA34893 DM2ZUXK Anxiety disorder 6B00-6B0Z Phase 2 [18]
SEP--4199 DMA12HB Bipolar disorder 6A60 Phase 2 [19]
⏷ Show the Full List of 10 Drug(s)
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) Metabolized By Cytochrome P450 3A4 (CYP3A4)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [27]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [28]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [29]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [30]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [31]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [32]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [33]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [34]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [28]
Verapamil DMA7PEW Angina pectoris BA40 Approved [35]
⏷ Show the Full List of 10 Drug(s)
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 [36]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [37]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [38]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [31]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [35]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [39]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [40]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [41]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [42]
Propranolol DM79NTF Angina pectoris BA40 Approved [43]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [53]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [54]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [55]
Oxatomide DM1F42Z Hay fever CA08.00 Approved [56]
Cinacalcet DMCX0K3 Hyperparathyroidism 5A51 Approved [57]
Capsaicin DMGMF6V Back pain ME84.Z Approved [58]
Pentamidine DMHZJCG African trypanosomiasis 1F51 Approved [59]
Quinidine DMLPICK N. A. N. A. Approved [60]
Buprenorphine DMPRI8G Opioid dependence 6C43.2Z Approved [61]
Methadone DMTW6IU Advanced cancer 2A00-2F9Z Approved [62]
⏷ Show the Full List of 20 Drug(s)
Drug(s) Metabolized By Cytochrome P450 3A5 (CYP3A5)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [44]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [45]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [46]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [47]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [48]
Sulfasalazine DMICA9H Irritable bowel syndrome DD91.0 Approved [49]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [50]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [51]
Verapamil DMA7PEW Angina pectoris BA40 Approved [52]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [47]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [63]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [64]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [65]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [66]
Cepharanthine DM9Y5JB N. A. N. A. Approved [67]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [68]
Clozapine DMFC71L Schizophrenia 6A20 Approved [69]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [70]
Trifluoperazine DMKBYWI Anxiety Approved [71]
Olanzapine DMPFN6Y Bipolar depression Approved [69]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Prolactin (PRL)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [72]
Ranitidine DM0GUSX Gastric ulcer DA60 Approved [73]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [74]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [75]
Methotrexate DM2TEOL Anterior urethra cancer Approved [76]
Thioridazine DM35M8J Schizophrenia 6A20 Approved [77]
Naloxone DM3FXMA Narcotic depression 6A7Z Approved [78]
Aripiprazole DM3NUMH Bipolar I disorder Approved [79]
Fluoxetine DM3PD2C Bipolar depression Approved [80]
Penicillamine DM40EF6 Cystinuria 5C60.2 Approved [81]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Interleukin-1 alpha (IL1A)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [82]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [11]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [11]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [83]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [11]
Methotrexate DM2TEOL Anterior urethra cancer Approved [76]
Quercetin DM3NC4M Obesity 5B81 Approved [84]
Rofecoxib DM3P5DA Osteoarthritis FA00-FA05 Approved [11]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [85]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [86]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Interleukin-1 beta (IL1B)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [87]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [88]
Gefitinib DM15F0X Colon adenocarcinoma Approved [89]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [11]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [90]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [11]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [91]
Selenium DM25CGV N. A. N. A. Approved [92]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [93]
Spironolactone DM2AQ5N Chronic heart failure BD1Z Approved [94]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Interleukin-8 (CXCL8)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrocortisone DMGEMB7 Acne vulgaris ED80 Approved [95]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [96]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [97]
Pantothenic acid DM091H2 Vitamin deficiency 5B55-5B71 Approved [98]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [99]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [88]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [11]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [90]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [100]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [11]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Paclitaxel DMLB81S Breast carcinoma Approved [101]
Verapamil DMA7PEW Angina pectoris BA40 Approved [102]
Methysergide DM1EF73 Migraine 8A80 Approved [12]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [103]
Methotrexate DM2TEOL Anterior urethra cancer Approved [104]
Lapatinib DM3BH1Y Breast cancer 2C60-2C65 Approved [12]
Quercetin DM3NC4M Obesity 5B81 Approved [105]
obeticholic acid DM3Q1SM Primary biliary cholangitis DB96.1 Approved [106]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [107]
Omeprazole DM471KJ Cystic fibrosis CA25 Approved [108]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Gabapentin DM6T924 Complex partial seizure 8A68.0 Approved [109]
Fluphenazine DMIT8LX Psychotic disorder 6A20-6A25 Approved [110]
Haloperidol DM96SE0 Delirium Approved [8]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [111]
Temozolomide DMKECZD Adenocarcinoma 2D40 Approved [112]
Olanzapine DMPFN6Y Bipolar depression Approved [113]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [114]
Arsenic DMTL2Y1 N. A. N. A. Approved [115]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [116]
Ketanserin DMVLMW6 Hypertension BA00-BA04 Approved [117]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metoclopramide DMFA5MY Nausea MD90 Approved [118]
Quinidine DMLPICK N. A. N. A. Approved [119]
Verapamil DMA7PEW Angina pectoris BA40 Approved [120]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [121]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [121]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [122]
Propranolol DM79NTF Angina pectoris BA40 Approved [123]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [124]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [125]
Flecainide DMSQDLE Tachyarrhythmias BC71 Approved [121]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Interleukin-24 (IL24)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [82]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [11]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [88]
Lumiracoxib DM1S4AG Chronic renal failure GB61.Z Approved [11]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [11]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [126]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [127]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [128]
Penbutolol DM4ES8F Hypertension BA00-BA04 Approved [11]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [128]
⏷ 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 receptor (5HTR) TT85JO3 NOUNIPROTAC Antagonist [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [5]
Cytochrome P450 2D6 (CYP2D6) Main DME DECB0K3 CP2D6_HUMAN Substrate [6]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [7]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
5-hydroxytryptamine receptor 2A (HTR2A) OTWXJX0M 5HT2A_HUMAN Protein Interaction/Cellular Processes [8]
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Regulation of Drug Effects [9]
Cytochrome P450 2D6 (CYP2D6) OTZJC802 CP2D6_HUMAN Regulation of Drug Effects [10]
Interleukin-1 alpha (IL1A) OTPSGILV IL1A_HUMAN Gene/Protein Processing [11]
Interleukin-1 beta (IL1B) OT0DWXXB IL1B_HUMAN Gene/Protein Processing [11]
Interleukin-24 (IL24) OT4VUWH1 IL24_HUMAN Gene/Protein Processing [11]
Interleukin-8 (CXCL8) OTS7T5VH IL8_HUMAN Gene/Protein Processing [11]
Phosphatidylcholine translocator ABCB4 (ABCB4) OTE6PY83 MDR3_HUMAN Gene/Protein Processing [12]
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Gene/Protein Processing [13]
Prolactin (PRL) OTWFQGX7 PRL_HUMAN Gene/Protein Processing [14]

References

1 Paliperidone FDA Label
2 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: 7258).
3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
4 Invega (paliperidone) extended release tablets FDA Label
5 ABCB1 polymorphisms influence steady-state plasma levels of 9-hydroxyrisperidone and risperidone active moiety. Ther Drug Monit. 2008 Oct;30(5):628-33.
6 Interpreting serum risperidone concentrations. Pharmacotherapy. 2005 Feb;25(2):299-302.
7 Different enantioselective 9-hydroxylation of risperidone by the two human CYP2D6 and CYP3A4 enzymes. Drug Metab Dispos. 2001 Oct;29(10):1263-8.
8 Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity. J Clin Psychiatry. 1994 May;55 Suppl:5-12.
9 Blonanserin, a novel atypical antipsychotic agent not actively transported as substrate by P-glycoprotein. Prog Neuropsychopharmacol Biol Psychiatry. 2012 Oct 1;39(1):156-62. doi: 10.1016/j.pnpbp.2012.06.005. Epub 2012 Jun 9.
10 Cytochrome P450 2D6 genotype and steady state plasma levels of risperidone and 9-hydroxyrisperidone. Psychopharmacology (Berl). 1999 Dec;147(3):300-5. doi: 10.1007/s002130051171.
11 An in vitro coculture system of human peripheral blood mononuclear cells with hepatocellular carcinoma-derived cells for predicting drug-induced liver injury. Arch Toxicol. 2021 Jan;95(1):149-168. doi: 10.1007/s00204-020-02882-4. Epub 2020 Aug 20.
12 Evaluating the Role of Multidrug Resistance Protein 3 (MDR3) Inhibition in Predicting Drug-Induced Liver Injury Using 125 Pharmaceuticals. Chem Res Toxicol. 2017 May 15;30(5):1219-1229. doi: 10.1021/acs.chemrestox.7b00048. Epub 2017 May 4.
13 Prolongation of cardiac ventricular repolarization under paliperidone: how and how much?. J Cardiovasc Pharmacol. 2011 Jun;57(6):690-5. doi: 10.1097/FJC.0b013e318217d941.
14 Extended-release paliperidone: efficacy, safety and tolerability profile of a new atypical antipsychotic. Drugs Today (Barc). 2007 Apr;43(4):249-58. doi: 10.1358/dot.2007.43.4.1067342.
15 Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.
16 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
17 Pharmacotherapy for obesity. Drugs. 2005;65(10):1391-418.
18 Encyclopedia of Psychopharmacology. Ian Stolerman. 2010. Page(105).
19 ClinicalTrials.gov (NCT03543410) A Clinical Study to Test the Effectiveness of an Investigational Drug to Treat People That Have Major Depressive Episodes When They Have Bipolar 1 Depression. U.S. National Institutes of Health.
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 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.
28 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
29 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.
30 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
31 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.
32 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.
33 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
34 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.
35 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.
36 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
37 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.
38 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
39 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.
40 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
41 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
42 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
43 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
44 Drug related genetic polymorphisms affecting adverse reactions to methotrexate, vinblastine, doxorubicin and cisplatin in patients with urothelial cancer. J Urol. 2008 Dec;180(6):2389-95.
45 Human prostate CYP3A5: identification of a unique 5'-untranslated sequence and characterization of purified recombinant protein. Biochem Biophys Res Commun. 1999 Jul 14;260(3):676-81.
46 Polymorphisms in cytochrome P4503A5 (CYP3A5) may be associated with race and tumor characteristics, but not metabolism and side effects of tamoxifen in breast cancer patients. Cancer Lett. 2005 Jan 10;217(1):61-72.
47 Drug Interactions Flockhart Table
48 Induction of hepatic CYP2E1 by a subtoxic dose of acetaminophen in rats: increase in dichloromethane metabolism and carboxyhemoglobin elevation. Drug Metab Dispos. 2007 Oct;35(10):1754-8.
49 Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8.
50 Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94.
51 Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000.
52 Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71.
53 Human recombinant cytochrome P450 enzymes display distinct hydrogen peroxide generating activities during substrate independent NADPH oxidase reactions. Toxicol Sci. 2014 Oct;141(2):344-52. doi: 10.1093/toxsci/kfu133. Epub 2014 Jul 24.
54 Effect of penicillin-based antibiotics, amoxicillin, ampicillin, and piperacillin, on drug-metabolizing activities of human hepatic cytochromes P450. J Toxicol Sci. 2016 Feb;41(1):143-6.
55 Cannabidiol, a major phytocannabinoid, as a potent atypical inhibitor for CYP2D6. Drug Metab Dispos. 2011 Nov;39(11):2049-56. doi: 10.1124/dmd.111.041384. Epub 2011 Aug 5.
56 Identification of human P450 isoforms involved in the metabolism of the antiallergic drug, oxatomide, and its kinetic parameters and inhibition constants. Biol Pharm Bull. 2005 Feb;28(2):328-34.
57 Pharmacokinetics of desipramine HCl when administered with cinacalcet HCl. Eur J Clin Pharmacol. 2007 Feb;63(2):159-63.
58 Effects of capsaicin and dihydrocapsaicin on human and rat liver microsomal CYP450 enzyme activities in vitro and in vivo. J Asian Nat Prod Res. 2012;14(4):382-95.
59 Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metab Dispos. 2001 Jan;29(1):30-5.
60 Inhibition of cytochrome P4502D6 activity with paroxetine normalizes the ultrarapid metabolizer phenotype as measured by nortriptyline pharmacokinetics and the debrisoquin test. Clin Pharmacol Ther. 2001 Oct;70(4):327-35.
61 Interaction of buprenorphine and its metabolite norbuprenorphine with cytochromes p450 in vitro. Drug Metab Dispos. 2003 Jun;31(6):768-72.
62 Expression, purification, and characterization of mouse CYP2d22. Drug Metab Dispos. 2006 Jul;34(7):1167-74.
63 Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. Cancer Res. 1994 Feb 1;54(3):730-7.
64 Michaelis-Menten kinetic analysis of drugs of abuse to estimate their affinity to human P-glycoprotein. Toxicol Lett. 2013 Feb 27;217(2):137-42. doi: 10.1016/j.toxlet.2012.12.012. Epub 2012 Dec 27.
65 Editor's Highlight: PlacentalDisposition and Effects of Crizotinib: An Ex Vivo Study in the Isolated Dual-Side Perfused Human Cotyledon. Toxicol Sci. 2017 Jun 1;157(2):500-509. doi: 10.1093/toxsci/kfx063.
66 Functional evaluation of polymorphisms in the human ABCB1 gene and the impact on clinical responses of antiepileptic drugs. Pharmacogenet Genomics. 2008 May;18(5):390-402. doi: 10.1097/FPC.0b013e3282f85e36.
67 Cepharanthine potently enhances the sensitivity of anticancer agents in K562 cells. Cancer Sci. 2005 Jun;96(6):372-6. doi: 10.1111/j.1349-7006.2005.00057.x.
68 Clinical pharmacokinetic monitoring of itraconazole is warranted in only a subset of patients. Ther Drug Monit. 2005 Jun;27(3):322-33. doi: 10.1097/01.ftd.0000150135.22645.ea.
69 Evaluation of antipsychotic drugs as inhibitors of multidrug resistance transporter P-glycoprotein. Psychopharmacology (Berl). 2006 Sep;187(4):415-23. doi: 10.1007/s00213-006-0437-9. Epub 2006 Jun 30.
70 Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76.
71 Characterization of the ATPase activity of the Mr 170,000 to 180,000 membrane glycoprotein (P-glycoprotein) associated with multidrug resistance in K562/ADM cells. Cancer Res. 1988 Sep 1;48(17):4926-32.
72 Verapamil-induced hyperprolactinemia complicated by a pituitary incidentaloma. Ann Pharmacother. 1995 Oct;29(10):999-1001. doi: 10.1177/106002809502901009.
73 [Impotence and gynecomastia secondary to hyperprolactinemia induced by ranitidine]. Therapie. 1994 Jul-Aug;49(4):361-2.
74 Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release. Mol Cell Endocrinol. 2005 Jul 15;239(1-2):27-36. doi: 10.1016/j.mce.2005.04.008.
75 Cholinergic modulation of the cerebral metabolic response to citalopram in Alzheimer's disease. Brain. 2009 Feb;132(Pt 2):392-401. doi: 10.1093/brain/awn326. Epub 2009 Jan 19.
76 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
77 The effect of thioridazine on prolactinoma growth in a schizophrenic man: case report. Gen Hosp Psychiatry. 1985 Oct;7(4):364-6. doi: 10.1016/0163-8343(85)90053-2.
78 Influence of naloxone on muscle sympathetic nerve activity, systemic and calf haemodynamics and ambulatory blood pressure after exercise in mild essential hypertension. J Hypertens. 1995 Apr;13(4):447-61.
79 The efficacy, safety, and tolerability of aripiprazole for the treatment of schizoaffective disorder: results from a pooled analysis of a sub-population of subjects from two randomized, double-blind, placebo-controlled, pivotal trials. J Affect Disord. 2009 May;115(1-2):18-26. doi: 10.1016/j.jad.2008.12.017. Epub 2009 Feb 23.
80 Serum prolactin levels among outpatients with major depressive disorder during the acute phase of treatment with fluoxetine. J Clin Psychiatry. 2006 Jun;67(6):952-7. doi: 10.4088/jcp.v67n0612.
81 Massive breast enlargement in a patient receiving D-penicillamine for systemic sclerosis. J Rheumatol. 1985 Oct;12(5):990-1.
82 Cannabidiol enhances cytotoxicity of anti-cancer drugs in human head and neck squamous cell carcinoma. Sci Rep. 2020 Nov 26;10(1):20622. doi: 10.1038/s41598-020-77674-y.
83 Oxidative Stress Alters miRNA and Gene Expression Profiles in Villous First Trimester Trophoblasts. Biomed Res Int. 2015;2015:257090. doi: 10.1155/2015/257090. Epub 2015 Aug 3.
84 Quercetin potentiates apoptosis by inhibiting nuclear factor-kappaB signaling in H460 lung cancer cells. Biol Pharm Bull. 2013;36(6):944-51. doi: 10.1248/bpb.b12-01004.
85 Increased sensitivity for troglitazone-induced cytotoxicity using a human in vitro co-culture model. Toxicol In Vitro. 2009 Oct;23(7):1387-95.
86 Transcriptional and Metabolic Dissection of ATRA-Induced Granulocytic Differentiation in NB4 Acute Promyelocytic Leukemia Cells. Cells. 2020 Nov 5;9(11):2423. doi: 10.3390/cells9112423.
87 Cannabidiol Modulates the Immunophenotype and Inhibits the Activation of the Inflammasome in Human Gingival Mesenchymal Stem Cells. Front Physiol. 2016 Nov 24;7:559. doi: 10.3389/fphys.2016.00559. eCollection 2016.
88 ERE-independent ERalpha target genes differentially expressed in human breast tumors. Mol Cell Endocrinol. 2005 Dec 21;245(1-2):53-9. doi: 10.1016/j.mce.2005.10.003. Epub 2005 Nov 17.
89 Reactive metabolite of gefitinib activates inflammasomes: implications for gefitinib-induced idiosyncratic reaction. J Toxicol Sci. 2020;45(11):673-680. doi: 10.2131/jts.45.673.
90 Gypenosides protect retinal pigment epithelium cells from oxidative stress. Food Chem Toxicol. 2018 Feb;112:76-85.
91 (9)-Tetrahydrocannabinol Suppresses Monocyte-Mediated Astrocyte Production of Monocyte Chemoattractant Protein 1 and Interleukin-6 in a Toll-Like Receptor 7-Stimulated Human Coculture. J Pharmacol Exp Ther. 2019 Oct;371(1):191-201. doi: 10.1124/jpet.119.260661. Epub 2019 Aug 5.
92 Changes in gene expression profiles in response to selenium supplementation among individuals with arsenic-induced pre-malignant skin lesions. Toxicol Lett. 2007 Mar 8;169(2):162-76. doi: 10.1016/j.toxlet.2007.01.006. Epub 2007 Jan 19.
93 Profiling the immunotoxicity of chemicals based on in vitro evaluation by a combination of the Multi-ImmunoTox assay and the IL-8 Luc assay. Arch Toxicol. 2018 Jun;92(6):2043-2054. doi: 10.1007/s00204-018-2199-7. Epub 2018 Mar 29.
94 Spironolactone induces apoptosis in human mononuclear cells. Association between apoptosis and cytokine suppression. Apoptosis. 2006 Apr;11(4):573-9. doi: 10.1007/s10495-006-4919-3.
95 Monomeric and oligomeric flavanols maintain the endogenous glucocorticoid response in human macrophages in pro-oxidant conditions in vitro. Chem Biol Interact. 2018 Aug 1;291:237-244.
96 Nicotine up-regulates IL-8 expression in human gingival epithelial cells following stimulation with IL-1 or P. gingivalis lipopolysaccharide via nicotinic acetylcholine receptor signalling. Arch Oral Biol. 2012 May;57(5):483-90. doi: 10.1016/j.archoralbio.2011.10.007. Epub 2011 Nov 25.
97 Ca(2+) Signaling and IL-8 Secretion in Human Testicular Peritubular Cells Involve the Cation Channel TRPV2. Int J Mol Sci. 2018 Sep 19;19(9):2829. doi: 10.3390/ijms19092829.
98 Calcium pantothenate modulates gene expression in proliferating human dermal fibroblasts. Exp Dermatol. 2009 Nov;18(11):969-78. doi: 10.1111/j.1600-0625.2009.00884.x. Epub 2009 Apr 8.
99 Nitrogen mustard prevents transport of Fra-1 into the nucleus to promote c-Fos- and FosB-dependent IL-8 induction in injured mouse epidermis. Toxicol Lett. 2020 Feb 1;319:256-263. doi: 10.1016/j.toxlet.2019.10.006. Epub 2019 Oct 19.
100 Nitric oxide synthase inhibitors attenuate ozone-induced airway inflammation in guinea pigs. Possible role of interleukin-8. Am J Respir Crit Care Med. 2000 Jan;161(1):249-56. doi: 10.1164/ajrccm.161.1.9804096.
101 [Reversal effect of MDR1 and MDR3 gene silencing on resistance of A2780/taxol cells to paclitaxel]. Zhonghua Fu Chan Ke Za Zhi. 2007 Jun;42(6):412-6.
102 8-Methoxypsoralen disrupts MDR3-mediated phospholipids efflux and bile acid homeostasis and its relevance to hepatotoxicity. Toxicology. 2017 Jul 1;386:40-48. doi: 10.1016/j.tox.2017.05.011. Epub 2017 May 24.
103 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.
104 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
105 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.
106 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
107 Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact. 2009 Apr 15;179(1):17-24.
108 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.
109 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
110 Discovery of antiandrogen activity of nonsteroidal scaffolds of marketed drugs. Proc Natl Acad Sci U S A. 2007 Jul 17;104(29):11927-32. doi: 10.1073/pnas.0609752104. Epub 2007 Jul 2.
111 Integrative omics data analyses of repeated dose toxicity of valproic acid in vitro reveal new mechanisms of steatosis induction. Toxicology. 2018 Jan 15;393:160-170.
112 Temozolomide induces activation of Wnt/-catenin signaling in glioma cells via PI3K/Akt pathway: implications in glioma therapy. Cell Biol Toxicol. 2020 Jun;36(3):273-278. doi: 10.1007/s10565-019-09502-7. Epub 2019 Nov 22.
113 No evidence for binding of clozapine, olanzapine and/or haloperidol to selected receptors involved in body weight regulation. Pharmacogenomics J. 2007 Aug;7(4):275-81. doi: 10.1038/sj.tpj.6500418. Epub 2006 Sep 19.
114 Nephrotoxicity induced by cisplatin is primarily due to the activation of the 5-hydroxytryptamine degradation system in proximal renal tubules. Chem Biol Interact. 2021 Nov 1;349:109662. doi: 10.1016/j.cbi.2021.109662. Epub 2021 Sep 21.
115 Prenatal arsenic exposure and the epigenome: identifying sites of 5-methylcytosine alterations that predict functional changes in gene expression in newborn cord blood and subsequent birth outcomes. Toxicol Sci. 2015 Jan;143(1):97-106. doi: 10.1093/toxsci/kfu210. Epub 2014 Oct 10.
116 Endometrial receptivity is affected in women with high circulating progesterone levels at the end of the follicular phase: a functional genomics analysis. Hum Reprod. 2011 Jul;26(7):1813-25.
117 The role of MAPK and Nrf2 pathways in ketanserin-elicited attenuation of cigarette smoke-induced IL-8 production in human bronchial epithelial cells. Toxicol Sci. 2012 Feb;125(2):569-77. doi: 10.1093/toxsci/kfr305. Epub 2011 Nov 1.
118 Comparison of the effects of metoclopramide and domperidone on HERG channels. Pharmacology. 2005 Apr;74(1):31-6. doi: 10.1159/000083234. Epub 2005 Jan 7.
119 Further insights into the effect of quinidine in short QT syndrome caused by a mutation in HERG. J Cardiovasc Electrophysiol. 2005 Jan;16(1):54-8. doi: 10.1046/j.1540-8167.2005.04470.x.
120 Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev Technol. 2004 Oct;2(5):497-506. doi: 10.1089/adt.2004.2.497.
121 Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. Toxicol Sci. 2013 Dec;136(2):581-94. doi: 10.1093/toxsci/kft205. Epub 2013 Sep 19.
122 Pharmacology of the short QT syndrome N588K-hERG K+ channel mutation: differential impact on selected class I and class III antiarrhythmic drugs. Br J Pharmacol. 2008 Nov;155(6):957-66. doi: 10.1038/bjp.2008.325. Epub 2008 Aug 25.
123 Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy. Br J Pharmacol. 2006 Mar;147(6):642-52. doi: 10.1038/sj.bjp.0706508.
124 Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels. Naunyn Schmiedebergs Arch Pharmacol. 1999 Mar;359(3):212-9. doi: 10.1007/pl00005344.
125 Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. FEBS Lett. 2000 May 26;474(1):111-5. doi: 10.1016/s0014-5793(00)01586-6.
126 Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
127 Effects of ciglitazone and troglitazone on the proliferation of human stomach cancer cells. World J Gastroenterol. 2009 Jan 21;15(3):310-20.
128 Retinoic acid and its 4-oxo metabolites are functionally active in human skin cells in vitro. J Invest Dermatol. 2005 Jul;125(1):143-53.