General Information of Drug (ID: DM82Z30)

Drug Name
Topiramate Drug Info
Synonyms
Epitoma; Epitomax; TOR; Tipiramate; Tipiramato; Topamac; Topamax; Topimax; Topina; Topiramato; Topiramatum; Topomax; Cilag brandof topiramate; Janssen brand of topiramate; Ortho brand of topiramate; Tipiramate [French]; Tipiramato [Spanish]; Topamax Sprinkle; Topiramate tablet; Topiramatum [Latin]; Topiramic acid; McN 4853; RWJ 17021; KS-1122; KW-6485; McN-4853; RWJ-17021; Topamax (TN); Topamax, Topiramate; Topiramate (TPM); Topiramate / Placebo; Topiramato [INN-Spanish]; Topiramatum [INN-Latin]; USL-255; RWJ-17021-000; Topiramate [USAN:BAN:INN]; Topiramate (JAN/USAN/INN); Beta-D-Fructopyranose, 2,3:4,5-bis-O-(1-methylethylidene)-, sulfamate; Beta-D-Fructopyranose, 2,3:4,5-bis-O-(1-methylethylidene)-, sulfamate (9CI);Beta.-D-Fructopyranose, 2,3:4,5-bis-O-(1-methylethylidene)-, 1-sulfamate; [(3aS,5aR,8aR,8bS)-2,2,7,7-tetramethyltetrahydro-3aH-bis[1,3]dioxolo[4,5-b:4',5'-d]pyran-3a-yl]methyl sulfamate; 2,3-4,5-bis-O-(1-methylethylidene)-beta-D-fructopyranose sulfamate; 2,3:4,5-Bis-O-(1-methylethylidene) .beta.-D-fructopyranose sulfamate; 2,3:4,5-Bis-O-(1-methylethylidene)-36-D-fructo-pyranose sulfamate; 2,3:4,5-Bis-O-(1-methylethylidene)-beta-D-fructopyranose sulfamate; 2,3:4,5-Di-O-isopropylidene-(beta)-D-fructopyranose sulfamate; 2,3:4,5-Di-O-isopropylidene-beta-D-fructopyranose sulfamate; 5H-Bis[1,3]dioxolo[4,5-b:4',5'-d]pyran, beta
Indication
Disease Entry ICD 11 Status REF
Alcohol dependence 6C40.2 Approved [1]
Epilepsy 8A60-8A68 Approved [1]
Epilepsy with generalized tonic-clonic seizures Approved [2]
Hyperlipidemia 5C80.Z Approved [2]
Hypertriglyceridemia 5C80.1 Approved [2]
Obesity 5B81 Approved [2]
Metabolic syndrome x 5C50-5D2Z Investigative [2]
Seizure disorder 8A6Z Investigative [3]
Therapeutic Class
Anticonvulsants
Cross-matching ID
PubChem CID
5284627
ChEBI ID
CHEBI:63631
CAS Number
CAS 97240-79-4
TTD Drug ID
DM82Z30
VARIDT Drug ID
DR01372
INTEDE Drug ID
DR1618
ACDINA Drug ID
D00689

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Clinical Trial Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
LY293558 DM4N6EK Pain MG30-MG3Z Phase 2 [13]
NS 1209 DM9EFH0 Epilepsy 8A60-8A68 Phase 2 [14]
NBQX DMPHZI5 Neurological disorder 6B60 Phase 1 [15]
YM-90K DMWRT4L Convulsion 8A68.Z Discontinued in Phase 2 [15]
[3H]kainate DMMK7XU Discovery agent N.A. Investigative [16]
[3H]quisqualate DMDQBTX Discovery agent N.A. Investigative [17]
SYM2081 DM30WDL Discovery agent N.A. Investigative [16]
DNQX DMQXPA5 Discovery agent N.A. Investigative [18]
dysiherbaine DM0EBAF Discovery agent N.A. Investigative [16]
domoic acid DMYPVO0 Discovery agent N.A. Investigative [16]
⏷ 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 [19]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [20]
Methotrexate DM2TEOL Anterior urethra cancer Approved [21]
Folic Acid DMEMBJC Colorectal carcinoma Approved [22]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [21]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [21]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [23]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [21]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [24]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [25]
⏷ 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 [26]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [27]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [28]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [29]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [30]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [31]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [32]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [33]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [27]
Verapamil DMA7PEW Angina pectoris BA40 Approved [34]
Eplerenone DMF0NQR Heart failure BD10-BD13 Approved [35]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [36]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [37]
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [38]
Proguanil DMBL79I Malaria 1F40-1F45 Approved [39]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [39]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [40]
Nelfinavir mesylate DMFX6G8 N. A. N. A. Approved [41]
Capsaicin DMGMF6V Back pain ME84.Z Approved [42]
Axitinib DMGVH6N Renal cell carcinoma 2C90 Approved [43]
⏷ Show the Full List of 20 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Tretinoin DM49DUI Acne vulgaris ED80 Approved [44]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [45]
Triclosan DMZUR4N Malaria 1F40-1F45 Approved [46]
PDX-101 DM6OC53 Plasma cell myeloma 2A83.1 Phase 2 [47]
Benzo(a)pyrene DMN7J43 N. A. N. A. Phase 1 [48]
bisphenol A DM2ZLD7 Discovery agent N.A. Investigative [49]
Milchsaure DM462BT Pruritus EC90 Investigative [50]
⏷ Show the Full List of 7 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [51]
Vidarabine DM0N85H Hepatosplenic T-cell lymphoma Approved [51]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [52]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [53]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [54]
Etidronic acid DM1XHYJ Bone Paget disease Approved [51]
Tiaprofenic acid DM23D7J Osteoarthritis FA00-FA05 Approved [51]
Bromperidol DM24XYQ Schizophrenia 6A20 Approved [51]
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [55]
Deoxycholic acid DM3GYAL Subcutaneous fat disorder EF02 Approved [56]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Etretinate DM2CZFA Keratosis ED56 Approved [57]
FADROZOLE DM3C5GZ Breast cancer 2C60-2C65 Approved [58]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [59]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [60]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [61]
Testosterone DM7HUNW Hot flushes GA30 Approved [61]
Pyruvic acid DM7Q41G Malnutrition 5B50-5B71 Approved [62]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [7]
ABIRATERONE DM8V75C Prostate cancer 2C82.0 Approved [63]
Duloxetine DM9BI7M Depression 6A70-6A7Z Approved [64]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [59]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [7]
Lindane DMB8CNL Infestations of lice and scabies 1G00.Z Approved [65]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [66]
Metyrapone DMI7FVQ Cushing disease 5A70 Approved [67]
Rosiglitazone DMILWZR Chronic kidney disease GB61 Approved [59]
Niclosamide DMJAGXQ Cestodes infection 1F70-1F76 Approved [68]
Pioglitazone DMKJ485 Amyotrophic lateral sclerosis 8B60.0 Approved [69]
Levetiracetam DMTGDN8 Epilepsy 8A60-8A68 Approved [66]
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [70]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Carbonic anhydrase 12 (CA12)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetazolamide DM1AF5U Absence epilepsy Approved [71]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [72]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [73]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [74]
Panobinostat DM58WKG Chronic graft versus host disease Approved [75]
Estrone DM5T6US Acne vulgaris ED80 Approved [72]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [76]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [77]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [78]
Mestranol DMG3F94 Contraception QA21 Approved [72]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Carbonic anhydrase 2 (CA2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Acetazolamide DM1AF5U Absence epilepsy Approved [79]
Epinephrine DM3KJBC Acute asthma CA23 Approved [80]
Quercetin DM3NC4M Obesity 5B81 Approved [81]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [82]
Cyclophosphamide DM4O2Z7 Advanced cancer 2A00-2F9Z Approved [83]
Methazolamide DM7J2TA Glaucoma/ocular hypertension 9C61 Approved [84]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [85]
Voriconazole DMAOL2S Aspergillosis 1F20 Approved [86]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [77]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [87]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Carbamazepine DMZOLBI Epilepsy 8A60-8A68 Approved [88]
Phenytoin DMNOKBV Epilepsy 8A60-8A68 Approved [89]
Allopurinol DMLPAOB Gout FA25 Approved [90]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [91]
Clavulanate DM2FGRT Bacteremia 1A73 Approved [92]
Ticlopidine DMO946V Acute coronary syndrome BA41 Approved [93]
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [92]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [94]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [11]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [11]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [95]
Valdecoxib DMAY7H4 Osteoarthritis FA00-FA05 Approved [11]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [96]
Ethosuximide DMDZ9LT Epilepsy 8A60-8A68 Approved [11]
Zoledronate DMIXC7G Adenocarcinoma 2D40 Approved [97]
Vancomycin DM3JFIH Bacteremia 1A73 Approved [11]
Temozolomide DMKECZD Adenocarcinoma 2D40 Approved [98]
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [99]
Bortezomib DMNO38U Leukemia Approved [100]
Famotidine DMRL3AB Gastric ulcer DA60 Approved [11]
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Drug Name Drug ID Indication ICD 11 Highest Status REF
Metoclopramide DMFA5MY Nausea MD90 Approved [101]
Quinidine DMLPICK N. A. N. A. Approved [102]
Verapamil DMA7PEW Angina pectoris BA40 Approved [103]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [104]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [104]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [105]
Propranolol DM79NTF Angina pectoris BA40 Approved [106]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [107]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [108]
Flecainide DMSQDLE Tachyarrhythmias BC71 Approved [104]
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Drug(s) Affected By Pro-neuropeptide Y (NPY)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Mifepristone DMGZQEF Cushing disease 5A70 Approved [9]
Reserpine DM6VM38 Hypertension BA00-BA04 Approved [9]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [109]
Panobinostat DM58WKG Chronic graft versus host disease Approved [75]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [110]
Guanethidine DM9NSWT Moderate and severe hypertension BA00.Z Approved [111]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [78]
Hydrocortisone DMGEMB7 Acne vulgaris ED80 Approved [112]
Orlistat DMRJSP8 Obesity 5B81 Approved [113]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [114]
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Drug(s) Affected By Galanin peptides (GAL)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Angina pectoris BA40 Approved [115]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [73]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [115]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [116]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [117]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [118]
Testosterone DM7HUNW Hot flushes GA30 Approved [119]
Methazolamide DM7J2TA Glaucoma/ocular hypertension 9C61 Approved [115]
Calcitriol DM8ZVJ7 Congenital alopecia LC30 Approved [119]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [120]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Glutamate receptor ionotropic kainate 1 (GRIK1) TT0MYE2 GRIK1_HUMAN Antagonist [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [5]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) Main DME DE4LYSA CP3A4_HUMAN Substrate [6]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
3 beta-hydroxysteroid dehydrogenase/Delta 5-->4-isomerase type 2 (HSD3B2) OT02MSKN 3BHS2_HUMAN Gene/Protein Processing [7]
Carbonic anhydrase 12 (CA12) OT6WNFU8 CAH12_HUMAN Gene/Protein Processing [8]
Carbonic anhydrase 2 (CA2) OTJRMUAG CAH2_HUMAN Gene/Protein Processing [8]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Gene/Protein Processing [6]
Galanin peptides (GAL) OTB3VPTO GALA_HUMAN Drug Response [9]
Glutamate receptor ionotropic, kainate 1 (GRIK1) OTO19X5C GRIK1_HUMAN Drug Response [10]
HLA class I histocompatibility antigen, A alpha chain (HLA-A) OTAH14LU HLAA_HUMAN Gene/Protein Processing [11]
HLA class II histocompatibility antigen, DM beta chain (HLA-DMB) OT17HGXJ DMB_HUMAN Gene/Protein Processing [11]
Nuclear receptor subfamily 1 group I member 2 (NR1I2) OTC5U0N5 NR1I2_HUMAN Gene/Protein Processing [6]
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Gene/Protein Processing [12]

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: 6849).
2 Topiramate FDA Label
3 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.
4 Development of medications for alcohol use disorders: recent advances and ongoing challenges. Expert Opin Emerg Drugs. 2005 May;10(2):323-43.
5 The antiepileptic drug topiramate is a substrate for human P-glycoprotein but not multidrug resistance proteins. Pharm Res. 2009 Nov;26(11):2464-70.
6 Dose-dependent induction of cytochrome P450 (CYP) 3A4 and activation of pregnane X receptor by topiramate. Epilepsia. 2003 Dec;44(12):1521-8.
7 Effects of anticonvulsants on human p450c17 (17alpha-hydroxylase/17,20 lyase) and 3beta-hydroxysteroid dehydrogenase type 2. Epilepsia. 2005 Mar;46(3):444-8.
8 Design, synthesis, and biological evaluation of novel carbohydrate-based sulfamates as carbonic anhydrase inhibitors. J Med Chem. 2011 Mar 10;54(5):1481-9.
9 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.
10 A preliminary pharmacogenetic investigation of adverse events from topiramate in heavy drinkers. Exp Clin Psychopharmacol. 2009 Apr;17(2):122-9. doi: 10.1037/a0015700.
11 Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis. Chem Res Toxicol. 2015 May 18;28(5):927-34. doi: 10.1021/tx5005248. Epub 2015 Apr 3.
12 Effects of the antiepileptic drugs lamotrigine, topiramate and gabapentin on hERG potassium currents. Epilepsy Res. 2005 Jan;63(1):17-25. doi: 10.1016/j.eplepsyres.2004.10.002. Epub 2004 Dec 8.
13 Pharmacogenetics of new analgesics. Br J Pharmacol. 2011 Jun;163(3):447-60.
14 The efficacy of the AMPA receptor antagonist NS1209 and lidocaine in nerve injury pain: a randomized, double-blind, placebo-controlled, three-way crossover study. Anesth Analg. 2009 Apr;108(4):1311-9.
15 4,10-Dihydro-4-oxo-4H-imidazo[1,2-a]indeno[1,2-e]pyrazin-2-carboxylic acid derivatives: highly potent and selective AMPA receptors antagonists with... Bioorg Med Chem Lett. 2000 May 15;10(10):1133-7.
16 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. (Target id: 450).
17 Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotr... J Med Chem. 2008 Jul 24;51(14):4093-103.
18 Synthesis of chiral 1-(2'-amino-2'-carboxyethyl)-1,4-dihydro-6,7-quinoxaline-2,3-diones: alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate recep... J Med Chem. 1996 Oct 25;39(22):4430-8.
19 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
20 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
21 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.
22 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
23 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
24 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
25 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.
26 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.
27 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
28 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.
29 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
30 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.
31 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.
32 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
33 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.
34 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.
35 The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.
36 Characterization of the structural determinants required for potent mechanism-based inhibition of human cytochrome P450 1A1 by cannabidiol. Chem Biol Interact. 2014 May 25;215:62-8.
37 Retinoids activate the RXR/SXR-mediated pathway and induce the endogenous CYP3A4 activity in Huh7 human hepatoma cells. Toxicol Sci. 2006 Jul;92(1):51-60.
38 The novel azole R126638 is a selective inhibitor of ergosterol synthesis in Candida albicans, Trichophyton spp., and Microsporum canis. Antimicrob Agents Chemother. 2004 Sep;48(9):3272-8.
39 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.
40 Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. Bioorg Med Chem Lett. 2004 Nov 15;14(22):5591-4.
41 Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther. 2005 Feb;312(2):583-91.
42 Studies of the toxicological potential of capsinoids, XIII: inhibitory effects of capsaicin and capsinoids on cytochrome P450 3A4 in human liver microsomes. Int J Toxicol. 2010 Mar;29(2 Suppl):22S-6S.
43 Investigation of the effects of axitinib on the pharmacokinetics of loperamide and its main metabolite N-demethylated loperamide in rats by UPLC-MS/MS. Chem Biol Interact. 2019 Sep 1;310:108744. doi: 10.1016/j.cbi.2019.108744. Epub 2019 Jul 9.
44 Development of a neural teratogenicity test based on human embryonic stem cells: response to retinoic acid exposure. Toxicol Sci. 2011 Dec;124(2):370-7.
45 THC exposure of human iPSC neurons impacts genes associated with neuropsychiatric disorders. Transl Psychiatry. 2018 Apr 25;8(1):89. doi: 10.1038/s41398-018-0137-3.
46 Transcriptome and DNA methylome dynamics during triclosan-induced cardiomyocyte differentiation toxicity. Stem Cells Int. 2018 Oct 29;2018:8608327.
47 Definition of transcriptome-based indices for quantitative characterization of chemically disturbed stem cell development: introduction of the STOP-Toxukn and STOP-Toxukk tests. Arch Toxicol. 2017 Feb;91(2):839-864.
48 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
49 DNA methylome-wide alterations associated with estrogen receptor-dependent effects of bisphenols in breast cancer. Clin Epigenetics. 2019 Oct 10;11(1):138. doi: 10.1186/s13148-019-0725-y.
50 Transcriptional profiling of lactic acid treated reconstructed human epidermis reveals pathways underlying stinging and itch. Toxicol In Vitro. 2019 Jun;57:164-173.
51 Screening of a chemical library reveals novel PXR-activating pharmacologic compounds. Toxicol Lett. 2015 Jan 5;232(1):193-202. doi: 10.1016/j.toxlet.2014.10.009. Epub 2014 Oct 16.
52 Induction of PXR-mediated metabolism by beta-carotene. Biochim Biophys Acta. 2005 May 30;1740(2):162-9. doi: 10.1016/j.bbadis.2004.11.013. Epub 2004 Dec 8.
53 Lignans, bacteriocides and organochlorine compounds activate the human pregnane X receptor (PXR). Toxicol Appl Pharmacol. 2005 Dec 1;209(2):123-33. doi: 10.1016/j.taap.2005.03.015.
54 Identification and validation of novel human pregnane X receptor activators among prescribed drugs via ligand-based virtual screening. Drug Metab Dispos. 2011 Feb;39(2):337-44. doi: 10.1124/dmd.110.035808. Epub 2010 Nov 10.
55 Identification of HMG-CoA reductase inhibitors as activators for human, mouse and rat constitutive androstane receptor. Drug Metab Dispos. 2005 Jul;33(7):924-9.
56 Acetylated deoxycholic (DCA) and cholic (CA) acids are potent ligands of pregnane X (PXR) receptor. Toxicol Lett. 2017 Jan 4;265:86-96.
57 Retinoids and retinol differentially regulate steroid biosynthesis in ovarian theca cells isolated from normal cycling women and women with polycystic ovary syndrome. J Clin Endocrinol Metab. 2005 Aug;90(8):4858-65. doi: 10.1210/jc.2005-0330. Epub 2005 May 24.
58 Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase. J Med Chem. 2005 Mar 10;48(5):1563-75.
59 Cinnamic acid based thiazolidinediones inhibit human P450c17 and 3beta-hydroxysteroid dehydrogenase and improve insulin sensitivity independent of PPARgamma agonist activity. J Mol Endocrinol. 2004 Apr;32(2):425-36.
60 Use of organ culture to study the human fetal testis development: effect of retinoic acid. J Clin Endocrinol Metab. 2006 Jul;91(7):2696-703.
61 Inhibition of CYP17 expression by adrenal androgens and transforming growth factor beta in adrenocortical cells. Acta Biochim Pol. 2004;51(4):907-17.
62 Phosphorylation of CtBP1 by cAMP-dependent protein kinase modulates induction of CYP17 by stimulating partnering of CtBP1 and 2. J Biol Chem. 2008 Mar 14;283(11):6925-34. doi: 10.1074/jbc.M708432200. Epub 2008 Jan 9.
63 A fission yeast-based test system for the determination of IC50 values of anti-prostate tumor drugs acting on CYP21. J Enzyme Inhib Med Chem. 2006 Oct;21(5):547-56.
64 Steroidogenic disruptive effects of the serotonin-noradrenaline reuptake inhibitors duloxetine, venlafaxine and tramadol in the H295R cell assay and in a recombinant CYP17 assay. Toxicol In Vitro. 2018 Mar;47:63-71.
65 Steroidogenic gene expression in H295R cells and the human adrenal gland: adrenotoxic effects of lindane in vitro. J Appl Toxicol. 2006 Nov-Dec;26(6):484-92.
66 Differential effects of antiepileptic drugs on steroidogenesis in a human in vitro cell model. Acta Neurol Scand Suppl. 2009;(189):14-21.
67 The H295R system for evaluation of endocrine-disrupting effects. Ecotoxicol Environ Saf. 2006 Nov;65(3):293-305.
68 Mitochondrial Uncoupling Induces Epigenome Remodeling and Promotes Differentiation in Neuroblastoma. Cancer Res. 2023 Jan 18;83(2):181-194. doi: 10.1158/0008-5472.CAN-22-1029.
69 Pioglitazone inhibits androgen production in NCI-H295R cells by regulating gene expression of CYP17 and HSD3B2. Mol Pharmacol. 2007 Mar;71(3):787-98.
70 Prostaglandin E2 via steroidogenic factor-1 coordinately regulates transcription of steroidogenic genes necessary for estrogen synthesis in endometriosis. J Clin Endocrinol Metab. 2009 Feb;94(2):623-31.
71 Targeting hypoxic tumor cell viability with carbohydrate-based carbonic anhydrase IX and XII inhibitors. J Med Chem. 2011 Oct 13;54(19):6905-18.
72 Moving toward integrating gene expression profiling into high-throughput testing: a gene expression biomarker accurately predicts estrogen receptor alpha modulation in a microarray compendium. Toxicol Sci. 2016 May;151(1):88-103.
73 Global gene expression analysis reveals differences in cellular responses to hydroxyl- and superoxide anion radical-induced oxidative stress in caco-2 cells. Toxicol Sci. 2010 Apr;114(2):193-203. doi: 10.1093/toxsci/kfp309. Epub 2009 Dec 31.
74 Transcriptomic analysis of untreated and drug-treated differentiated HepaRG cells over a 2-week period. Toxicol In Vitro. 2015 Dec 25;30(1 Pt A):27-35.
75 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
76 DNA microarray analysis of vitamin D-induced gene expression in a human colon carcinoma cell line. Physiol Genomics. 2004 Apr 13;17(2):122-9. doi: 10.1152/physiolgenomics.00002.2003.
77 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
78 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
79 Indomethacin activates carbonic anhydrase and antagonizes the effect of the specific carbonic anhydrase inhibitor acetazolamide, by a direct mechanism of action. Int J Clin Pharmacol Ther. 2001 Jun;39(6):265-70.
80 Effects of beta-adrenergic agonists on bone-resorbing activity in human osteoclast-like cells. Biochim Biophys Acta. 2003 May 12;1640(2-3):137-42.
81 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.
82 Effect of retinoic acid on gene expression in human conjunctival epithelium: secretory phospholipase A2 mediates retinoic acid induction of MUC16. Invest Ophthalmol Vis Sci. 2005 Nov;46(11):4050-61.
83 Comparative gene expression analysis of a chronic myelogenous leukemia cell line resistant to cyclophosphamide using oligonucleotide arrays and response to tyrosine kinase inhibitors. Leuk Res. 2007 Nov;31(11):1511-20.
84 Inhibition profiling of human carbonic anhydrase II by high-throughput screening of structurally diverse, biologically active compounds. J Biomol Screen. 2006 Oct;11(7):782-91.
85 Large-scale in silico and microarray-based identification of direct 1,25-dihydroxyvitamin D3 target genes. Mol Endocrinol. 2005 Nov;19(11):2685-95.
86 Inhibition profiles of Voriconazole against acetylcholinesterase, -glycosidase, and human carbonic anhydrase I and II isoenzymes. J Biochem Mol Toxicol. 2019 Oct;33(10):e22385. doi: 10.1002/jbt.22385. Epub 2019 Sep 3.
87 Carbonic anhydrase inhibitors. Inhibition of human erythrocyte isozymes I and II with a series of antioxidant phenols bioorg. Med Chem. 2009 Apr 15;17(8):3207-11.
88 HLA-A*3101 and carbamazepine-induced hypersensitivity reactions in Europeans. N Engl J Med. 2011 Mar 24;364(12):1134-43. doi: 10.1056/NEJMoa1013297.
89 Common risk allele in aromatic antiepileptic-drug induced Stevens-Johnson syndrome and toxic epidermal necrolysis in Han Chinese. Pharmacogenomics. 2010 Mar;11(3):349-56. doi: 10.2217/pgs.09.162.
90 Positive and negative associations of HLA class I alleles with allopurinol-induced SCARs in Koreans. Pharmacogenet Genomics. 2011 May;21(5):303-7. doi: 10.1097/FPC.0b013e32834282b8.
91 A study of HLA class I and class II 4-digit allele level in Stevens-Johnson syndrome and toxic epidermal necrolysis. Int J Immunogenet. 2011 Aug;38(4):303-9. doi: 10.1111/j.1744-313X.2011.01011.x. Epub 2011 May 4.
92 HLA alleles influence the clinical signature of amoxicillin-clavulanate hepatotoxicity. PLoS One. 2013 Jul 9;8(7):e68111. doi: 10.1371/journal.pone.0068111. Print 2013.
93 Ticlopidine-induced hepatotoxicity is associated with specific human leukocyte antigen genomic subtypes in Japanese patients: a preliminary case-control study. Pharmacogenomics J. 2008 Feb;8(1):29-33. doi: 10.1038/sj.tpj.6500442. Epub 2007 Mar 6.
94 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.
95 Identification of vitamin D3 target genes in human breast cancer tissue. J Steroid Biochem Mol Biol. 2016 Nov;164:90-97.
96 Stem cell transcriptome responses and corresponding biomarkers that indicate the transition from adaptive responses to cytotoxicity. Chem Res Toxicol. 2017 Apr 17;30(4):905-922.
97 Interleukin-19 as a translational indicator of renal injury. Arch Toxicol. 2015 Jan;89(1):101-6.
98 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.
99 Chromosomal radiosensitivity in two cell lineages derived from clinically radiosensitive cancer patients. Clin Cancer Res. 2005 Sep 1;11(17):6352-8. doi: 10.1158/1078-0432.CCR-04-1931.
100 The proapoptotic effect of zoledronic acid is independent of either the bone microenvironment or the intrinsic resistance to bortezomib of myeloma cells and is enhanced by the combination with arsenic trioxide. Exp Hematol. 2011 Jan;39(1):55-65.
101 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.
102 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.
103 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.
104 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.
105 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.
106 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.
107 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.
108 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.
109 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
110 Arsenic trioxide inhibits neuroblastoma growth in vivo and promotes apoptotic cell death in vitro. Biochem Biophys Res Commun. 2000 Oct 14;277(1):179-85. doi: 10.1006/bbrc.2000.3651.
111 Release and functional role of neuropeptide Y as a sympathetic modulator in human saphenous vein biopsies. Peptides. 2004 Jan;25(1):53-64. doi: 10.1016/j.peptides.2003.11.001.
112 Neuropeptide Y in cortisol-induced hypertension in male volunteers. Clin Exp Pharmacol Physiol. 1994 May;21(5):435-8. doi: 10.1111/j.1440-1681.1994.tb02538.x.
113 [Effect of orlistat therapy on carbohydrate, lipid, vitamin and hormone plasma levels in obese subjects]. Pol Arch Med Wewn. 2004 Dec;112(6):1415-23.
114 Coordinate up-regulation of TMEM97 and cholesterol biosynthesis genes in normal ovarian surface epithelial cells treated with progesterone: implications for pathogenesis of ovarian cancer. BMC Cancer. 2007 Dec 11;7:223.
115 Discovery of molecular mechanisms of neuroprotection using cell-based bioassays and oligonucleotide arrays. Physiol Genomics. 2002 Oct 29;11(2):45-52. doi: 10.1152/physiolgenomics.00064.2002.
116 Retinoic acid receptor alpha amplifications and retinoic acid sensitivity in breast cancers. Clin Breast Cancer. 2013 Oct;13(5):401-8.
117 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
118 JunD is involved in the antiproliferative effect of Delta9-tetrahydrocannabinol on human breast cancer cells. Oncogene. 2008 Aug 28;27(37):5033-44.
119 Effects of 1alpha,25 dihydroxyvitamin D3 and testosterone on miRNA and mRNA expression in LNCaP cells. Mol Cancer. 2011 May 18;10:58.
120 Integrative "-Omics" analysis in primary human hepatocytes unravels persistent mechanisms of cyclosporine A-induced cholestasis. Chem Res Toxicol. 2016 Dec 19;29(12):2164-2174.