General Information of Drug (ID: DMR23M1)

Drug Name
Mapracorat Drug Info
Synonyms
BOL-303242X; SEGRA, Intendis; SEGRA, Schering AG; ZK-216348; ZK-238587; ZK-245186; Mapracorat (ophthalmic, ocular inflammation); Mapracorat Ophthalmic Suspension, Bausch & Lomb; SEGRA (atopic dermatitis), Bayer; Selective glucocorticoid receptor agonists (SEGRA) Bayer Schering/AstraZeneca; Selective glucocorticoid receptor agonists (SEGRA) Schering AG/AstraZeneca; Selective glucocorticoid receptor agonists (SEGRA), Schering AG; Selective glucocorticoid receptor agonists (dermatology), Schering AG; Mapracorat (dermatological, atopic dermatitis), Intendis; SEGRA (ophthalmic disease), Bausch & Lomb; Selective glucocorticoid receptor agonist (ophthalmic disease), Bausch & Lomb; Selective glucocorticoid receptor agonists (dermatological, eczema), Intendis; Suppressor of pro-inflammatory mediators (eczema), Intendis; BOL-303242-X Ophthalmic Suspension, Bausch & Lomb; Mapracorat (ophthalmic, ocular inflammation), Bausch & Lomb; ZK-245186 (ophthalmic), Bausch & Lomb
Indication
Disease Entry ICD 11 Status REF
Ocular disease 1F00.1Z Phase 3 [1]
Cross-matching ID
PubChem CID
24795088
CAS Number
CAS 887375-26-0
TTD Drug ID
DMR23M1

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [3]
Hydrocortisone DMGEMB7 Acne vulgaris ED80 Approved [4]
Prednisolone DMQ8FR2 Acute adrenal insufficiency Approved [5]
Fluticasone DMGCSVF Allergic rhinitis CA08.0 Approved [6]
Betamethasone Valerate DMMIAXO Dermatological disease DA24.Y Approved [4]
Methylprednisolone DM4BDON Acute adrenal insufficiency Approved [4]
Deflazacort DMV0RNS Duchenne dystrophy 8C70 Approved [4]
Prednisone DM2HG4X Acute asthma CA23 Approved [7]
Budesonide DMJIBAW Allergic rhinitis CA08.0 Approved [8]
Mifepristone DMGZQEF Cushing disease 5A70 Approved [9]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [10]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [11]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [12]
Selenium DM25CGV N. A. N. A. Approved [13]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [14]
Methotrexate DM2TEOL Anterior urethra cancer Approved [15]
Quercetin DM3NC4M Obesity 5B81 Approved [16]
Troglitazone DM3VFPD Diabetic complication 5A2Y Approved [17]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [18]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [19]
⏷ Show the Full List of 20 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Colchicine DM2POTE Acute gout flare FA25.0 Approved [20]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [21]
Leflunomide DMR8ONJ Arthritis FA20 Approved [22]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [23]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [24]
Bosentan DMIOGBU Pulmonary arterial hypertension BB01.0 Approved [25]
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [26]
Miconazole DMPMYE8 Cutaneous candidiasis 1F23.14 Approved [27]
Azacitidine DMTA5OE Acute myelogenous leukaemia 2A41 Approved [28]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [29]
⏷ 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
Glucocorticoid receptor (NR3C1) TTYRL6O GCR_HUMAN Agonist [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Glucocorticoid receptor (NR3C1) OTCI2YDI GCR_HUMAN Protein Interaction/Cellular Processes [2]
Tyrosine aminotransferase (TAT) OT2CJ91O ATTY_HUMAN Gene/Protein Processing [2]

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: 8643).
2 Characterization of ZK 245186, a novel, selective glucocorticoid receptor agonist for the topical treatment of inflammatory skin diseases. Br J Pharmacol. 2009 Oct;158(4):1088-103.
3 Interaction between the glucocorticoid and erythropoietin receptors in human erythroid cells. Exp Hematol. 2009 May;37(5):559-72.
4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
5 Aldosterone (mineralocorticoid) equivalent to prednisolone (glucocorticoid) in reversing hearing loss in MRL/MpJ-Fas1pr autoimmune mice. Laryngoscope. 2000 Nov;110(11):1902-6.
6 Fluticasone furoate nasal spray in allergic rhinitis. Drugs Today (Barc). 2008 Apr;44(4):251-60.
7 Cytochromes P450 (CYP) in the Poeciliopsis lucida hepatocellular carcinoma cell line (PLHC-1): dose- and time-dependent glucocorticoid potentiation of CYP1A induction without induction of CYP3A. ArchBiochem Biophys. 1996 May 1;329(1):113-22.
8 PXR-mediated induction of human CYP3A4 and mouse Cyp3a11 by the glucocorticoid budesonide. Eur J Pharm Sci. 2009 Mar 2;36(4-5):565-71.
9 The glucocorticoid agonist activities of mifepristone (RU486) and progesterone are dependent on glucocorticoid receptor levels but not on EC50 values. Steroids. 2007 Jun;72(6-7):600-8.
10 Persistent and non-persistent changes in gene expression result from long-term estrogen exposure of MCF-7 breast cancer cells. J Steroid Biochem Mol Biol. 2011 Feb;123(3-5):140-50.
11 Arsenite and cadmium promote the development of mammary tumors. Carcinogenesis. 2020 Jul 14;41(7):1005-1014. doi: 10.1093/carcin/bgz176.
12 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.
13 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.
14 Comparative effects of microtubules disruption on glucocorticoid receptor functions in proliferating and quiescent cells. Int J Toxicol. 2010 May-Jun;29(3):326-35. doi: 10.1177/1091581810366486.
15 The contribution of methotrexate exposure and host factors on transcriptional variance in human liver. Toxicol Sci. 2007 Jun;97(2):582-94.
16 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.
17 Effects of ciglitazone and troglitazone on the proliferation of human stomach cancer cells. World J Gastroenterol. 2009 Jan 21;15(3):310-20.
18 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.
19 Adipocyte differentiation, mitochondrial gene expression and fat distribution: differences between zidovudine and tenofovir after 6 months. Antivir Ther. 2009;14(8):1089-100. doi: 10.3851/IMP1457.
20 Microtubule disarray in primary cultures of human hepatocytes inhibits transcriptional activity of the glucocorticoid receptor via activation of c-jun N-terminal kinase. Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub. 2004 Dec;148(2):135-9.
21 Essential role of cell cycle regulatory genes p21 and p27 expression in inhibition of breast cancer cells by arsenic trioxide. Med Oncol. 2011 Dec;28(4):1225-54.
22 Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. Toxicology. 2017 Dec 1;392:11-21.
23 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.
24 Histone deacetylase inhibitor valproic acid promotes the differentiation of human induced pluripotent stem cells into hepatocyte-like cells. PLoS One. 2014 Aug 1;9(8):e104010.
25 Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures. Arch Toxicol. 2018 Jun;92(6):1939-1952.
26 Dexamethasone controls aryl hydrocarbon receptor (AhR)-mediated CYP1A1 and CYP1A2 expression and activity in primary cultures of human hepatocytes. Chem Biol Interact. 2009 May 15;179(2-3):288-96.
27 Ketoconazole and miconazole are antagonists of the human glucocorticoid receptor: consequences on the expression and function of the constitutive androstane receptor and the pregnane X receptor. Mol Pharmacol. 2006 Jul;70(1):329-39.
28 Self-assembled 3D spheroids and hollow-fibre bioreactors improve MSC-derived hepatocyte-like cell maturation in vitro. Arch Toxicol. 2017 Apr;91(4):1815-1832.
29 Increased mitochondrial ROS formation by acetaminophen in human hepatic cells is associated with gene expression changes suggesting disruption of the mitochondrial electron transport chain. Toxicol Lett. 2015 Apr 16;234(2):139-50.