General Information of Drug (ID: DMPBV9D)

Drug Name
Flupirtine Drug Info
Synonyms
Flupirtine; 56995-20-1; Flupirtine [INN:BAN]; Flupirtinum [INN-Latin]; Flupirtino [INN-Spanish]; UNII-MOH3ET196H; C15H17FN4O2; EINECS 260-503-8; MOH3ET196H; JUUFBMODXQKSTD-UHFFFAOYSA-N; ethyl N-[2-amino-6-[(4-fluorophenyl)methylamino]pyridin-3-yl]carbamate; D 9998; flupirtin maleate; ethyl 2-amino-6-(4-fluorobenzylamino)pyridin-3-ylcarbamate; Flupirtinum; Flupirtino; MLS002153180; Carbamic acid, (2-amino-6-(((4-fluorophenyl)methyl)amino)-3-pyridinyl)-, ethyl ester; NCGC00015451-03; SMR001230672; Flupirtin; Carbamic acid, [2-ami
Indication
Disease Entry ICD 11 Status REF
Cancer related pain MG30 Phase 2 [1]
Fibromyalgia MG30.01 Phase 2 [1]
Cross-matching ID
PubChem CID
53276
ChEBI ID
CHEBI:94646
CAS Number
CAS 56995-20-1
TTD Drug ID
DMPBV9D

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Discontinued Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Retigabine DMGNYIH Behcet disease 4A62 Approved [5]
CNSB-001 DM2PEU5 Neuropathic pain 8E43.0 Phase 2 [6]
DMP-543 DMCNEOZ Parkinson disease 8A00.0 Discontinued in Phase 2 [7]
Drug(s) Affected By Bile salt export pump (ABCB11)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glimepiride DM5FSJA Diabetic complication 5A2Y Approved [4]
Ezetimibe DM7A8TW Atherosclerosis BD40 Approved [8]
Glipizide DMZA5PQ Diabetic complication 5A2Y Approved [8]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [9]
Indinavir DM0T3YH Human immunodeficiency virus infection 1C62 Approved [4]
Ofloxacin DM0VQN3 Acute gonococcal cervicitis Approved [8]
Primidone DM0WX6I Epilepsy 8A60-8A68 Approved [10]
Gefitinib DM15F0X Colon adenocarcinoma Approved [4]
Drospirenone DM1A9W3 Acne vulgaris ED80 Approved [11]
Nitrendipine DM21C09 Hypertension BA00-BA04 Approved [4]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [12]
Docetaxel DMDI269 Advanced cancer 2A00-2F9Z Approved [13]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [14]
Gemcitabine DMSE3I7 Anterior urethra cancer Approved [15]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [16]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [17]
Verapamil DMA7PEW Angina pectoris BA40 Approved [18]
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [19]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [20]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [22]
Selenium DM25CGV N. A. N. A. Approved [23]
Quercetin DM3NC4M Obesity 5B81 Approved [24]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [25]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [26]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [27]
Ivermectin DMDBX5F Intestinal strongyloidiasis due to nematode parasite 1F6B Approved [28]
Temozolomide DMKECZD Adenocarcinoma 2D40 Approved [29]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [30]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [31]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Caspase-2 (CASP2)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Mechlorethamine DM0CVXA Chronic myelogenous leukaemia 2A20.0 Approved [19]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [32]
Methotrexate DM2TEOL Anterior urethra cancer Approved [33]
Dactinomycin DM2YGNW Adult kidney Wilms tumor Approved [34]
Quercetin DM3NC4M Obesity 5B81 Approved [35]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [36]
Clonidine DM6RZ9Q Attention deficit hyperactivity disorder 6A05.Z Approved [37]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [38]
Leflunomide DMR8ONJ Arthritis FA20 Approved [39]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [40]
⏷ 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
Voltage-gated potassium channel Kv7 (KCNQ) TTQ29KF NOUNIPROTAC Modulator [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Gene/Protein Processing [3]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Gene/Protein Processing [4]
Caspase-2 (CASP2) OTUDYSPP CASP2_HUMAN Gene/Protein Processing [3]
Cytotoxic granule associated RNA binding protein TIA1 (TIA1) OTGPN3P8 TIA1_HUMAN Gene/Protein Processing [3]

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: 2598).
2 Treatment with the Kv7 potassium channel activator flupirtine is beneficial in two independent mouse models of pulmonary hypertension. Br J Pharmacol. 2009 August; 157(7): 1241-1249.
3 Melatonin counteracts ischemia-induced apoptosis in human retinal pigment epithelial cells. Invest Ophthalmol Vis Sci. 1998 Nov;39(12):2374-83.
4 Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development. Toxicol Sci. 2010 Dec; 118(2):485-500.
5 Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
6 The Kv7 potassium channel activator flupirtine affects clinical excitability parameters of myelinated axons in isolated rat sural nerve. J Peripher Nerv Syst. 2010 Mar;15(1):63-72.
7 KV7 channels regulate muscle tone and nonadrenergic noncholinergic relaxation of the rat gastric fundus.Pharmacol Res.2011 Oct;64(4):397-409.
8 Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43.
9 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
10 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.
11 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov;136(1):216-41.
12 4.8% sevoflurane induces activation of autophagy in human neuroblastoma SH-SY5Y cells by the AMPK/mTOR signaling pathway. Neurotoxicology. 2022 May;90:256-264. doi: 10.1016/j.neuro.2022.04.008. Epub 2022 Apr 23.
13 Enhanced chemotherapeutic efficacy of docetaxel in human lung cancer cell line via GLUT1 inhibitor. J Biochem Mol Toxicol. 2023 Jun;37(6):e23348. doi: 10.1002/jbt.23348. Epub 2023 Mar 31.
14 Breast cancer cells response to the antineoplastic agents cisplatin, carboplatin, and doxorubicin at the mRNA expression levels of distinct apoptosis-related genes, including the new member, BCL2L12. Ann N Y Acad Sci. 2007 Jan;1095:35-44. doi: 10.1196/annals.1397.005.
15 Extracellular signal-regulated kinase activation and Bcl-2 downregulation mediate apoptosis after gemcitabine treatment partly via a p53-independent pathway. Eur J Pharmacol. 2004 Oct 19;502(3):169-83. doi: 10.1016/j.ejphar.2004.09.006.
16 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.
17 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.
18 Verapamil potentiates anti-glioblastoma efficacy of temozolomide by modulating apoptotic signaling. Toxicol In Vitro. 2018 Oct;52:306-313. doi: 10.1016/j.tiv.2018.07.001. Epub 2018 Jul 9.
19 Inhibition of caspase-dependent mitochondrial permeability transition protects airway epithelial cells against mustard-induced apoptosis. Apoptosis. 2006 Sep;11(9):1545-59. doi: 10.1007/s10495-006-8764-1.
20 Sertraline, an antidepressant, induces apoptosis in hepatic cells through the mitogen-activated protein kinase pathway. Toxicol Sci. 2014 Feb;137(2):404-15. doi: 10.1093/toxsci/kft254. Epub 2013 Nov 5.
21 -Carotene Induces Apoptosis in Human Esophageal Squamous Cell Carcinoma Cell Lines via the Cav-1/AKT/NF-B Signaling Pathway. J Biochem Mol Toxicol. 2016 Mar;30(3):148-57. doi: 10.1002/jbt.21773. Epub 2016 Jan 6.
22 Minimal peroxide exposure of neuronal cells induces multifaceted adaptive responses. PLoS One. 2010 Dec 17;5(12):e14352. doi: 10.1371/journal.pone.0014352.
23 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
24 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.
25 Suppression of mammary carcinoma growth by retinoic acid: proapoptotic genes are targets for retinoic acid receptor and cellular retinoic acid-binding protein II signaling. Cancer Res. 2005 Sep 15;65(18):8193-9. doi: 10.1158/0008-5472.CAN-05-1177.
26 Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro. Toxicol In Vitro. 2015 Apr;29(3):489-501.
27 Human embryonic stem cell-derived test systems for developmental neurotoxicity: a transcriptomics approach. Arch Toxicol. 2013 Jan;87(1):123-43.
28 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
29 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.
30 Gene expression analysis of precision-cut human liver slices indicates stable expression of ADME-Tox related genes. Toxicol Appl Pharmacol. 2011 May 15;253(1):57-69.
31 17-Estradiol Activates HSF1 via MAPK Signaling in ER-Positive Breast Cancer Cells. Cancers (Basel). 2019 Oct 11;11(10):1533. doi: 10.3390/cancers11101533.
32 Carbamylation and oxidation of proteins lead to apoptotic death of lymphocytes. Chem Biol Interact. 2017 May 25;270:24-32. doi: 10.1016/j.cbi.2017.04.007. Epub 2017 Apr 8.
33 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
34 Actinomycin D and staurosporine, potent apoptosis inducers in vitro, are potentially effective chemotherapeutic agents against glioblastoma multiforme. Cancer Chemother Pharmacol. 2000;45(2):149-56. doi: 10.1007/s002800050023.
35 Quercetin-induced apoptosis of HL-60 cells by reducing PI3K/Akt. Mol Biol Rep. 2012 Jul;39(7):7785-93. doi: 10.1007/s11033-012-1621-0. Epub 2012 May 4.
36 Arsenic trioxide induces different gene expression profiles of genes related to growth and apoptosis in glioma cells dependent on the p53 status. Mol Biol Rep. 2008 Sep;35(3):421-9.
37 Clonidine Induces Apoptosis of Human Corneal Epithelial Cells through Death Receptors-Mediated, Mitochondria-Dependent Signaling Pathway. Toxicol Sci. 2017 Mar 1;156(1):252-260. doi: 10.1093/toxsci/kfw249.
38 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.
39 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
40 Lovastatin induces apoptosis of anaplastic thyroid cancer cells via inhibition of protein geranylgeranylation and de novo protein synthesis. Endocrinology. 2003 Sep;144(9):3852-9. doi: 10.1210/en.2003-0098.