Details of the Drug
General Information of Drug (ID: DM7NPJS)
Drug Name |
Paliperidone
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Synonyms |
Xeplion; Invega Sustenna; Paliperidone palmitate; JNS-010; Paliperidone (depot injection, NanoCrystal); Paliperidone (injectable, NanoCrystal), Elan; Paliperidone (depot injection, NanoCrystal), Johnson & Johnson
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Indication |
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Drug Type |
Small molecular drug
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Structure | ||||||||||||||||||||
3D MOL | 2D MOL | |||||||||||||||||||
#Ro5 Violations (Lipinski): 0 | Molecular Weight (mw) | 426.5 | ||||||||||||||||||
Topological Polar Surface Area (xlogp) | 2.2 | |||||||||||||||||||
Rotatable Bond Count (rotbonds) | 4 | |||||||||||||||||||
Hydrogen Bond Donor Count (hbonddonor) | 1 | |||||||||||||||||||
Hydrogen Bond Acceptor Count (hbondacc) | 7 | |||||||||||||||||||
ADMET Property |
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Chemical Identifiers |
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Cross-matching ID | ||||||||||||||||||||
Molecular Interaction Atlas of This Drug
Drug Therapeutic Target (DTT) |
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Drug Transporter (DTP) |
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Drug-Metabolizing Enzyme (DME) |
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Molecular Interaction Atlas (MIA) | |||||||||||||||||||||||||||||||||||||
Drug-Drug Interaction (DDI) Information of This Drug
Coadministration of a Drug Treating the Same Disease as Paliperidone
Coadministration of a Drug Treating the Disease Different from Paliperidone (Comorbidity)
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug
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: 7258). | ||||
---|---|---|---|---|---|
2 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
3 | ClinicalTrials.gov (NCT02146547) European Long-acting Antipsychotics in Schizophrenia Trial. U.S. National Institutes of Health. | ||||
4 | BDDCS applied to over 900 drugs | ||||
5 | FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41. | ||||
6 | Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds | ||||
7 | An FDA phase I clinical trial of quinacrine sterilization (QS). Int J Gynaecol Obstet. 2003 Oct;83 Suppl 2:S45-9. | ||||
8 | Invega (paliperidone) extended release tablets FDA Label | ||||
9 | ABCB1 polymorphisms influence steady-state plasma levels of 9-hydroxyrisperidone and risperidone active moiety. Ther Drug Monit. 2008 Oct;30(5):628-33. | ||||
10 | Interpreting serum risperidone concentrations. Pharmacotherapy. 2005 Feb;25(2):299-302. | ||||
11 | Different enantioselective 9-hydroxylation of risperidone by the two human CYP2D6 and CYP3A4 enzymes. Drug Metab Dispos. 2001 Oct;29(10):1263-8. | ||||
12 | 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. | ||||
13 | Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47. | ||||
14 | 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. | ||||
15 | Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9. | ||||
16 | 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. | ||||
17 | 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. | ||||
18 | Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6. | ||||
19 | 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. | ||||
20 | 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. | ||||
21 | Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5. | ||||
22 | 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. | ||||
23 | CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15. | ||||
24 | 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. | ||||
25 | Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53. | ||||
26 | Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106. | ||||
27 | Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70. | ||||
28 | Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82. | ||||
29 | 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. | ||||
30 | 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. | ||||
31 | 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. | ||||
32 | Drug Interactions Flockhart Table | ||||
33 | 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. | ||||
34 | Urinary 6 beta-hydroxycortisol excretion in rheumatoid arthritis. Br J Rheumatol. 1997 Jan;36(1):54-8. | ||||
35 | Clinical pharmacokinetics of imatinib. Clin Pharmacokinet. 2005;44(9):879-94. | ||||
36 | Kinetics and regulation of cytochrome P450-mediated etoposide metabolism. Drug Metab Dispos. 2004 Sep;32(9):993-1000. | ||||
37 | Differential mechanism-based inhibition of CYP3A4 and CYP3A5 by verapamil. Drug Metab Dispos. 2005 May;33(5):664-71. | ||||
38 | Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007. | ||||
39 | MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8. | ||||
40 | 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. | ||||
41 | Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31. | ||||
42 | Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. | ||||
43 | Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92. | ||||
44 | 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. | ||||
45 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. | ||||
46 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | ||||
47 | Pharmacotherapy for obesity. Drugs. 2005;65(10):1391-418. | ||||
48 | Encyclopedia of Psychopharmacology. Ian Stolerman. 2010. Page(105). | ||||
49 | 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. | ||||
50 | Canadian Pharmacists Association. | ||||
51 | Cohen MA, Alfonso CA, Mosquera M. Development of urinary retention during treatment with clozapine and meclizine [published correction appears in Am J Psychiatry 1994 Jun;151(6):952]. Am J Psychiatry. 1994;151(4):619-620. [PMID: 8147469] | ||||
52 | Product Information. Barhemsys (amisulpride). Acacia Pharma, Inc, Indianapolis, IN. | ||||
53 | Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA. | ||||
54 | Cerner Multum, Inc. "UK Summary of Product Characteristics.". | ||||
55 | Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL. | ||||
56 | US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.". | ||||
57 | Kulik AV, Wilbur R "Delirium and stereotypy from anticholinergic antiparkinson drugs." Prog Neuropsychopharmacol Biol Psychiatry 6 (1982): 75-82. [PMID: 7202232] | ||||
58 | Aronowitz JS, Chakos MH, Safferman AZ, Lieberman JA "Syncope associated with the combination of clozapine and enalapril." J Clin Psychopharmacol 14 (1994): 429-30. [PMID: 7884028] | ||||
59 | Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ. | ||||
60 | Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
61 | Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176] | ||||
62 | Product Information. Daurismo (glasdegib). Pfizer U.S. Pharmaceuticals Group, New York, NY. | ||||
63 | US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.". | ||||
64 | Cerner Multum, Inc. "Australian Product Information.". | ||||
65 | Burke RE, Fahn S, Mayeux R, Weinberg H, Louis K, Willner JH "Neuroleptic malignant syndrome caused by dopamine-depleting drugs in a patient with Huntington disease." Neurology 31 (1981): 1022-5. [PMID: 6115336] | ||||
66 | Product Information. Austedo (deutetrabenazine). Teva Pharmaceuticals USA, North Wales, PA. | ||||
67 | Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA. | ||||
68 | Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC. | ||||
69 | Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY. | ||||
70 | Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE. | ||||
71 | Harper KM, Knapp DJ, Criswell HE, Breese GR "Vasopressin and alcohol: A multifaceted relationship." Psychopharmacology (Berl) 235 (2018): 3363-79. [PMID: 32936259] | ||||
72 | Product Information. Braftovi (encorafenib). Array BioPharma Inc., Boulder, CO. | ||||
73 | Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA. | ||||
74 | Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN. | ||||
75 | Product Information. Addyi (flibanserin). Sprout Pharmaceuticals, Raleigh, NC. | ||||
76 | Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ. | ||||
77 | Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ. | ||||
78 | Product Information. Belviq (lorcaserin). Eisai Inc, Teaneck, NJ. | ||||
79 | Mims RB, Scott CL, Modebe O, Bethune JE "Inhibition of L-dopa-induced growth hormone stimulation by pyridoxine and chlorpromazine." J Clin Endocrinol Metab 40 (1975): 256-9. [PMID: 1117978] | ||||
80 | Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ. | ||||
81 | Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC. | ||||
82 | Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA. | ||||