Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMAZJFX)

Drug Name
Ciclosporin Drug Info
Synonyms
Ciclosporin; Ciclosporin (Ciclosporin A); Ciclosporina; Ciclosporina [INN-Spanish]; Ciclosporine; Ciclosporine [INN-French]; Ciclosporinum; Ciclosporinum [INN-Latin]; Cipol N; Consupren; Cyclosporin; Cyclosporine A; Equoral; Antibiotic S 7481F1; Gengraf; Neoplanta; Neoral; Ramihyphin A; Restasis; S-Neoral; Sandimmun; Sandimmun Neoral; Sandimmune; Sang 35; Sang-35; SangCyA; Sigmasporin Microoral; cyclosporin A; cyclosporine; 59865-13-3; 83HN0GTJ6D; CHEBI:4031; CSA; DSSTox_CID_365; DSSTox_RID_75541; MFCD00274558; MLS001333756; UNII-83HN0GTJ6D
Indication
Disease Entry ICD 11 Status REF
Graft-versus-host disease 4B24 Approved [1]
Psoriasis vulgaris EA90 Approved [2]
Brain injury NA07.Z Phase 4 [3]
Middle East Respiratory Syndrome (MERS) 1D64 Investigative [4]
Severe acute respiratory syndrome (SARS) 1D65 Investigative [4]
Xerophthalmia 5B55.Y Investigative [2]
Cross-matching ID
PubChem CID
5284373
ChEBI ID
CHEBI:4031
CAS Number
CAS 59865-13-3
TTD Drug ID
DMAZJFX
INTEDE Drug ID
DR0321

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Calcineurin (PPP3CA) TTA4LDE PP2BA_HUMAN Inhibitor [2]
HUMAN cyclophilin D (CYP3) TT95SAZ PPIF_HUMAN Inhibitor [4]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID Highest Status REF
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Approved [5]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Approved [6]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Approved [7]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Approved [8]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Approved [9]
Cytochrome P450 3A7 (CYP3A7) DERD86B CP3A7_HUMAN Approved [10]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Calcineurin (PPP3CA) DTT PPP3CA 6.282 7.43 6.685 6.815
P-glycoprotein 1 (ABCB1) DTP P-GP 7.009 6.988 7.442 8.135
Breast cancer resistance protein (ABCG2) DTP BCRP 6.732 7.513 6.326 9.277
Multidrug resistance-associated protein 2 (ABCC2) DTP MRP2 7.751 4.17 6.425 6.282
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 10.08 7.207 5.403 9.211
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 11.692 6.58 4.984 9.089
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Graft-versus-host disease
ICD Disease Classification 4B24
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Calcineurin (PPP3CA) DTT PPP3CA 5.29E-01 1.74E-03 9.99E-03
P-glycoprotein 1 (ABCB1) DTP P-GP 2.00E-01 2.57E-02 6.18E-02
Breast cancer resistance protein (ABCG2) DTP BCRP 6.07E-04 1.66E-01 4.54E-01
Multidrug resistance-associated protein 2 (ABCC2) DTP MRP2 7.41E-21 4.03E-01 1.33E+00
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 5.05E-02 4.52E-01 5.39E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 8.67E-01 -3.83E-03 -1.24E-02
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 Cyclosporine and tacrolimus for the treatment of rheumatoid arthritis. Curr Opin Rheumatol. 2007 May;19(3):238-45.
3 ClinicalTrials.gov (NCT00332462) A Study to Evaluate the Efficiency of Intravenously Administered Cyclosporine in de Novo Liver Transplant Recipients. U.S. National Institutes of Health.
4 Therapeutic options for the 2019 novel coronavirus (2019-nCoV). Nat Rev Drug Discov. 2020 Mar;19(3):149-150.
5 Is cyclosporine A transport inhibited by pravastatin via multidrug resistant protein 2? Eur J Clin Pharmacol. 2010 Feb;66(2):153-8.
6 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.
7 Contribution of down-regulation of intestinal and hepatic cytochrome P450 3A to increased absorption of cyclosporine A in a rat nephrosis model. J Pharmacol Exp Ther. 2008 Nov;327(2):592-9.
8 Dasatinib significantly reduced in vivo exposure to cyclosporine in a rat model: The possible involvement of CYP3A induction. Pharmacol Rep. 2019 Apr;71(2):201-205.
9 CYP3A4*18B and CYP3A5*3 polymorphisms contribute to pharmacokinetic variability of cyclosporine among healthy Chinese subjects. Eur J Pharm Sci. 2015 Aug 30;76:238-44.
10 CYP3A7, CYP3A5, CYP3A4, and ABCB1 genetic polymorphisms, cyclosporine concentration, and dose requirement in transplant recipients. Ther Drug Monit. 2008 Dec;30(6):689-99.