General Information of Drug (ID: DM2NA4K)

Drug Name
Ciclesonide Drug Info
Synonyms
Alvesco; Omnair; Omnaris; Osonase; Osonide; Alvesco HFA; Ciclesonide [INN]; Omnaris HFA; RPR 251526; Alvesco (TN); BTR-15; BTR-15K; BY-9010; BYK-20426; KS-1165; Omnaris (TN); Omniair (TN); TBN-15; B-9207-015; Ciclesonide (JAN/USAN/INN); (R)-11beta,16alpha,17,21-Tetrahydroxypregna-1,4-diene-3,20-dione cyclic 16,17-acetal with cyclohexanecarboxaldehyde, 21-isobutyrate
Indication
Disease Entry ICD 11 Status REF
Allergic rhinitis CA08.0 Approved [1]
Asthma CA23 Approved [2]
Obstructive airway disease CB40.Y Approved [3]
Seasonal allergic rhinitis CA08.01 Approved [1]
Coronavirus Disease 2019 (COVID-19) 1D6Y Phase 3 [4]
Therapeutic Class
Antiallergic Agents
Cross-matching ID
PubChem CID
6918155
ChEBI ID
CHEBI:31397
CAS Number
CAS 126544-47-6
TTD Drug ID
DM2NA4K
VARIDT Drug ID
DR01408
INTEDE Drug ID
DR0319

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Paramethasone DM6PR40 Inflammation 1A00-CA43.1 Approved [5]
Alclometasone DMAE84F Exanthem Approved [9]
I-vation DM0OYLQ Diabetic retinopathy 9B71.0 Phase 2 [10]
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 [11]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [12]
Methotrexate DM2TEOL Anterior urethra cancer Approved [13]
Folic Acid DMEMBJC Colorectal carcinoma Approved [14]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [13]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [13]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [15]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [13]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [16]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [17]
⏷ 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 [18]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [19]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [20]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [21]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [22]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [23]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [24]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [25]
Prasterone DM67VKL Chronic obstructive pulmonary disease CA22 Approved [19]
Verapamil DMA7PEW Angina pectoris BA40 Approved [26]
⏷ 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 [27]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [28]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [29]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [22]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [26]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [30]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [31]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [32]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [33]
Propranolol DM79NTF Angina pectoris BA40 Approved [34]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Flupentixol DM0DJ9O Schizophrenia 6A20 Approved [35]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [36]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [37]
Lamotrigine DM8SXYG Bipolar disorder 6A60 Approved [38]
Cepharanthine DM9Y5JB N. A. N. A. Approved [39]
Itraconazole DMCR1MV Aspergillosis 1F20 Approved [40]
Clozapine DMFC71L Schizophrenia 6A20 Approved [41]
Midostaurin DMI6E0R Acute myeloid leukaemia 2A60 Approved [42]
Trifluoperazine DMKBYWI Anxiety Approved [43]
Olanzapine DMPFN6Y Bipolar depression Approved [41]
⏷ 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
Corticosteroid-binding globulin (SERPINA6) TTJL8VG CBG_HUMAN Binder [5]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [6]

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

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
ATP-dependent translocase ABCB1 (ABCB1) OTEJROBO MDR1_HUMAN Gene/Protein Processing [8]

References

1 Ciclesonide FDA Label
2 FDA Approved Drug Products from FDA Official Website. 2019. Application Number: (NDA) 202129
3 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: 7469).
4 ClinicalTrials.gov (NCT04377711) A Study of the Safety and Efficacy of Ciclesonide in the Treatment of Non-hospitalized COVID-19 Patients. U.S. National Institutes of Health.
5 Novel human corticosteroid-binding globulin variant with low cortisol-binding affinity. J Clin Endocrinol Metab. 2000 Jan;85(1):361-7.
6 Oral and inhaled corticosteroids: differences in P-glycoprotein (ABCB1) mediated efflux. Toxicol Appl Pharmacol. 2012 May 1;260(3):294-302.
7 Identification of enzymes involved in phase I metabolism of ciclesonide by human liver microsomes. Eur J Drug Metab Pharmacokinet. 2005 Oct-Dec;30(4):275-86.
8 Oral and inhaled corticosteroids: differences in P-glycoprotein (ABCB1) mediated efflux. Toxicol Appl Pharmacol. 2012 May 1;260(3):294-302. doi: 10.1016/j.taap.2012.03.008. Epub 2012 Mar 23.
9 The anti-inflammatory effects of LY178002 and LY256548. Agents Actions. 1989 Jun;27(3-4):300-2.
10 Cortisol binding in rat skeletal muscle. J Biol Chem. 1975 Feb 25;250(4):1207-11.
11 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
12 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
13 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.
14 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
15 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
16 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
17 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.
18 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.
19 Contribution of human hepatic cytochrome P450 isoforms to regioselective hydroxylation of steroid hormones. Xenobiotica. 1998 Jun;28(6):539-47.
20 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.
21 Isoform-specific regulation of cytochromes P450 expression by estradiol and progesterone. Drug Metab Dispos. 2013 Feb;41(2):263-9.
22 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.
23 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.
24 Effects of morin on the pharmacokinetics of etoposide in rats. Biopharm Drug Dispos. 2007 Apr;28(3):151-6.
25 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.
26 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.
27 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
28 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.
29 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
30 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.
31 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
32 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
33 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
34 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
35 Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. Cancer Res. 1994 Feb 1;54(3):730-7.
36 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.
37 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.
38 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.
39 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.
40 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.
41 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.
42 Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002 Feb;87(2):167-76.
43 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.