DGIdb - CYCLOSPORINE Drug Record

CYCLOSPORINE chembl:CHEMBL160 ApprovedImmunotherapy

Alternate Names:

CAPIMUNE
CYCLOSPORIN A
RESTASIS MULTIDOSE
SANDIMMUN
SDZ-OXL-400
VANQUORAL
RESTASIS
ANTIBIOTIC S-7481F1
SANGCYA
OPTIMMUNE
27-400
SANG-35
CEQUA
DEXIMUNE
CICLOSPORIN
IKERVIS
SANDIMMUNE
CYCLOSPORINE
NEORAL
OL-27-400
GENGRAF
CAPSORIN
NSC-290193
30-ETHYL-33-[(4E)-1-HYDROXY-2-METHYLHEX-4-EN-1-YL]-6,9,18,24-TETRAISOBUTYL-3,21-DIISOPROPYL-1,4,7,10,12,15,19,25,28-NONAMETHYL-1,4,7,10,13,16,19,22,25,28,31-UNDECAAZACYCLOTRITRIACONTANE-2,5,8,11,14,17,20,23,26,29,32-UNDECONE
OLO400
1,11-CYCLO[L-ALANYL-D-ALANYL-N-METHYL-L-LEUCYL-N-METHYL-L-LEUCYL-N-METHYL-L-VALYL-(E)-(2S,3R,4R)-2-AMINO-3-HYDROXY-N,4-DIMETHYLOCT-6-ENOYL-L-2-AMINOBUTANOYL-N-METHYLGLYCYL-N-METHYL-L-LEUCYL-L-VALYL-N-METHYL-L-LEUCINE]
CSA
CYCLO(L-ALANYL-D-ALANYL-N-METHYL-L-LEUCYL-N-METHYL-L-LEUCYL-N-METHYL-L-VALYL-((3R,4R,6E)-6,7-DIDEHYDRO-3-HYDROXY-N,4-DIMETHYL-L-2-AMINOOCTANOYL)-L-2-AMINOBUTANOYL-N-METHYLGLYCYL-N-METHYL-L-LEUCYL-L-VALYL-N-METHYLLEUCYL)
ANTIBIOTIC S 7481F1
(R-[R,R-(E)])-CYCLIC(L-ALANYL-D-ALANYL-N-METHYL-L-LEUCYL-N-METHYL-L-LEUCYL-N-METHYL-L-VALYL-3-HYDROXY-N,4-DIMETHYL-L-2-AMINO-6-OCTENOYL-L-ALPHA-AMINOBUTYRYL-N-METHYLGLYCYL-N-METHYL-L-LEUCYL-L-VALYL-N-METHYL-L-LEUCYL)
CYCLOSPORINE A
CYA
chemidplus:59865-13-3
chembl:CHEMBL160
drugbank:00091
pubchem.compound:5284373
rxcui:3008

Drug Info:

FDA Approval	approved
Drug Class	Small molecule
Drug Indications	immunosuppressant
Drug Class	immunosuppressive agents
Year of Approval	1983

(6 More Sources)

Publications:

Abdel-Hady Algharably E et al., 2018, Effect of UMOD genotype on long-term graft survival after kidney transplantation in patients treated with cyclosporine-based therapy., Pharmacogenomics J
Baran et al., 2007, Upregulation of multi drug resistance genes in doxorubicin resistant human acute myelogeneous leukemia cells and reversal of the resistance., Hematology
Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
Wu, From bedside to bench drug-induced tubulointerstitial disease cyclosporine nephropathy study from models of cultured renal epithelial cells., Chang Gung Med J
Perico et al., 1992, Thromboxane receptor blockade attenuates chronic cyclosporine nephrotoxicity and improves survival in rats with renal isograft., J. Am. Soc. Nephrol.
Juvale K et al., 2012, 4-Substituted-2-phenylquinazolines as inhibitors of BCRP., Bioorg Med Chem Lett
Utsunomiya et al., 2000, Comparison of the accumulation and efflux kinetics of technetium-99m sestamibi and technetium-99m tetrofosmin in an MRP-expressing tumour cell line., Eur J Nucl Med
Van Gool et al., 1995, Accessory signalling by B7-1 for T cell activation induced by anti-CD2: evidence for IL-2-independent CTL generation and CsA-resistant cytokine production., Scand. J. Immunol.
Ma et al., 2002, The role of Ras in T lymphocyte activation., Cell. Signal.
Toebak et al., 2008, Differential suppression of dendritic cell cytokine production by anti-inflammatory drugs., Br. J. Dermatol.
Yamashita et al., 2010, Comparison of the efficacy of tacrolimus and cyclosporine A in a murine model of dinitrofluorobenzene-induced atopic dermatitis., Eur. J. Pharmacol.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Cardenas ME et al., 1994, Immunophilins interact with calcineurin in the absence of exogenous immunosuppressive ligands., EMBO J
Grigoriu S et al., 2013, The molecular mechanism of substrate engagement and immunosuppressant inhibition of calcineurin., PLoS Biol
Bulut et al., 2004, Immunohistochemical study of cyclosporin-induced gingival overgrowth in renal transplant recipients., J. Periodontol.
Mueller et al., 1993, The effect of cyclosporine treatment on the expression of genes encoding granzyme A and perforin in the infiltrate of mouse heart transplants., Transplantation
Bernasconi et al., 2010, Cyclosporine A-sensitive, cyclophilin B-dependent endoplasmic reticulum-associated degradation., PLoS ONE
Galat et al., 2010, Molecular aspects of cyclophilins mediating therapeutic actions of their ligands., Cell. Mol. Life Sci.
Lee et al., 2010, Current implications of cyclophilins in human cancers., J. Exp. Clin. Cancer Res.
Forsythe P et al., 2014, Ciclosporin 10 years on: indications and efficacy., Vet Rec
Russell G et al., 1992, Mechanisms of action of cyclosporine and effects on connective tissues., Semin Arthritis Rheum
Seip et al., 1988, Cyclosporine in steroid-resistant Diamond-Blackfan anaemia., Acta Paediatr Scand
Cvetković M et al., 2017, Effect of Age and Allele Variants of CYP3A5, CYP3A4, and POR Genes on the Pharmacokinetics of Cyclosporin A in Pediatric Renal Transplant Recipients From Serbia., Ther Drug Monit
Lunde I et al., 2014, The influence of CYP3A, PPARA, and POR genetic variants on the pharmacokinetics of tacrolimus and cyclosporine in renal transplant recipients., Eur J Clin Pharmacol
Elens L et al., 2014, Impact of POR*28 on the pharmacokinetics of tacrolimus and cyclosporine A in renal transplant patients., Ther Drug Monit
Usui et al., 2003, Induction of CYP3As in HepG2 cells by several drugs. Association between induction of CYP3A4 and expression of glucocorticoid receptor., Biol. Pharm. Bull.
Lou K et al., 2014, Brain-penetrant, orally bioavailable microtubule-stabilizing small molecules are potential candidate therapeutics for Alzheimer's disease and related tauopathies., J Med Chem
Silva GL et al., 2001, Modulation of the multidrug-resistance phenotype by new tropane alkaloid aromatic esters from Erythroxylum pervillei., J Nat Prod
Liu XL et al., 2008, Functionalized chalcones as selective inhibitors of P-glycoprotein and breast cancer resistance protein., Bioorg Med Chem
Condello M et al., 2014, Voacamine modulates the sensitivity to doxorubicin of resistant osteosarcoma and melanoma cells and does not induce toxicity in normal fibroblasts., J Nat Prod
Marks KM et al., 2011, The selectivity of austocystin D arises from cell-line-specific drug activation by cytochrome P450 enzymes., J Nat Prod
Sánchez-Lázaro I et al., 2015, Association of SNPs with the efficacy and safety of immunosuppressant therapy after heart transplantation., Pharmacogenomics
Lee J et al., 2015, The Effect of ABCB1 C3435T Polymorphism on Cyclosporine Dose Requirements in Kidney Transplant Recipients: A Meta-Analysis., Basic Clin Pharmacol Toxicol
Sharaki O et al., 2015, Impact of CYP3A4 and MDR1 gene (G2677T) polymorphisms on dose requirement of the cyclosporine in renal transplant Egyptian recipients., Mol Biol Rep
Ferraresso M et al., 2013, Long-term effects of ABCB1 and SXR SNPs on the systemic exposure to cyclosporine in pediatric kidney transplant patients., Pharmacogenomics
Barbarino JM et al., 2013, PharmGKB summary: cyclosporine and tacrolimus pathways., Pharmacogenet Genomics
García M et al., 2013, ABCB1 polymorphisms are associated with cyclosporine-induced nephrotoxicity and gingival hyperplasia in renal transplant recipients., Eur J Clin Pharmacol
Santoro A et al., 2011, Pharmacogenetics of calcineurin inhibitors in Brazilian renal transplant patients., Pharmacogenomics
Yanagimachi M et al., 2010, Influence of CYP3A5 and ABCB1 gene polymorphisms on calcineurin inhibitor-related neurotoxicity after hematopoietic stem cell transplantation., Clin Transplant
Zhang YT et al., 2008, ABCB1 polymorphisms may have a minor effect on ciclosporin blood concentrations in myasthenia gravis patients., Br J Clin Pharmacol
Beringer PM et al., 2008, Lack of effect of P-glycoprotein inhibition on renal clearance of dicloxacillin in patients with cystic fibrosis., Pharmacotherapy
Grinyó J et al., 2008, Association of four DNA polymorphisms with acute rejection after kidney transplantation., Transpl Int
Crettol S et al., 2008, Influence of ABCB1 genetic polymorphisms on cyclosporine intracellular concentration in transplant recipients., Pharmacogenet Genomics
Daniel F et al., 2007, Multidrug resistance gene-1 polymorphisms and resistance to cyclosporine A in patients with steroid resistant ulcerative colitis., Inflamm Bowel Dis
Hesselink DA et al., 2003, Genetic polymorphisms of the CYP3A4, CYP3A5, and MDR-1 genes and pharmacokinetics of the calcineurin inhibitors cyclosporine and tacrolimus., Clin Pharmacol Ther
Herweijer et al., 1990, Expression of mdr1 and mdr3 multidrug-resistance genes in human acute and chronic leukemias and association with stimulation of drug accumulation by cyclosporine., J. Natl. Cancer Inst.
Niederer et al., 2005, Cypermethrin blocks a mitochondria-dependent apoptotic signal initiated by deficient N-linked glycosylation within the endoplasmic reticulum., Cell. Signal.
Shah S et al., 2012, Inosine monophosphate dehydrogenase polymorphisms and renal allograft outcome., Transplantation
Pazik J et al., 2011, Lymphocyte counts in kidney allograft recipients are associated with IMPDH2 3757T>C gene polymorphism., Transplant Proc
Winnicki W et al., 2010, An inosine 5'-monophosphate dehydrogenase 2 single-nucleotide polymorphism impairs the effect of mycophenolic acid., Pharmacogenomics J
Sombogaard F et al., 2009, Interpatient variability in IMPDH activity in MMF-treated renal transplant patients is correlated with IMPDH type II 3757T > C polymorphism., Pharmacogenet Genomics
Stegmann et al., 2010, The crystal structure of PPIL1 bound to cyclosporine A suggests a binding mode for a linear epitope of the SKIP protein., PLoS ONE
Redell et al., 2007, Acutely increased cyclophilin a expression after brain injury: a role in blood-brain barrier function and tissue preservation., J. Neurosci. Res.
Schaller et al., 2007, Fusion of cyclophilin A to Fv1 enables cyclosporine-sensitive restriction of human and feline immunodeficiency viruses., J. Virol.
Patwardhan et al., 2006, The cannabinoid WIN 55,212-2 inhibits transient receptor potential vanilloid 1 (TRPV1) and evokes peripheral antihyperalgesia via calcineurin., Proc. Natl. Acad. Sci. U.S.A.
Keckesova et al., 2006, Cyclophilin A renders human immunodeficiency virus type 1 sensitive to Old World monkey but not human TRIM5 alpha antiviral activity., J. Virol.
Hong et al., 2002, Cyclosporin A blocks muscle differentiation by inducing oxidative stress and inhibiting the peptidyl-prolyl-cis-trans isomerase activity of cyclophilin A: cyclophilin A protects myoblasts from cyclosporin A-induced cytotoxicity., FASEB J.
Hopkins S et al., 2010, SCY-635, a novel nonimmunosuppressive analog of cyclosporine that exhibits potent inhibition of hepatitis C virus RNA replication in vitro., Antimicrob Agents Chemother
Grenet et al., 2000, Evidence for the impairment of the vitamin D activation pathway by cyclosporine A., Biochem. Pharmacol.
Sharma S et al., 2013, Hepatobiliary disposition of 17-OHPC and taurocholate in fetal human hepatocytes: a comparison with adult human hepatocytes., Drug Metab Dispos
Dianov et al., 1997, Reduced RNA polymerase II transcription in extracts of cockayne syndrome and xeroderma pigmentosum/Cockayne syndrome cells., Nucleic Acids Res.
Valentine et al., 1997, Induction of IL-5 expression by IL-2 is resistant to the immunosuppressive agents cyclosporin A and rapamycin., Int. Immunol.
Božina N et al., 2017, Steady-state pharmacokinetics of mycophenolic acid in renal transplant patients: exploratory analysis of the effects of cyclosporine, recipients' and donors' ABCC2 gene variants, and their interactions., Eur J Clin Pharmacol
Han N et al., 2014, Population pharmacogenetic pharmacokinetic modeling for flip-flop phenomenon of enteric-coated mycophenolate sodium in kidney transplant recipients., Eur J Clin Pharmacol
Yang et al., 2002, Hyaluronic acid and chondroitin sulphate A rapidly promote differentiation of immature DC with upregulation of costimulatory and antigen-presenting molecules, and enhancement of NF-kappaB and protein kinase activity., Scand. J. Immunol.
Cho et al., 2002, Cyclosporine differentially regulates interleukin-10, interleukin-15, and tumor necrosis factor a production by rheumatoid synoviocytes., Arthritis Rheum.
Baan et al., 2001, Conversion from cyclosporin A to tacrolimus is safe and decreases blood pressure, cholesterol levels and TGF-beta 1 type I receptor expression., Clin Transplant
Lewis et al., 2001, Interleukin-15 is the main mediator of lymphocyte proliferation in cultures mixed with human kidney tubular epithelial cells., Transplantation
Akashi et al., Dermatomyositis associated with membranous nephropathy in a 43-year-old female., Am. J. Nephrol.
Kajita et al., 2006, Effect of imatinib mesilate on the disposition kinetics of ciclosporin in rats., J. Pharm. Pharmacol.
Combes S et al., 2011, Synthesis and biological evaluation of 4-arylcoumarin analogues of combretastatins. Part 2., J Med Chem
Pawarode et al., 2007, Differential effects of the immunosuppressive agents cyclosporin A, tacrolimus and sirolimus on drug transport by multidrug resistance proteins., Cancer Chemother. Pharmacol.
Ling Q et al., 2013, Association between donor and recipient TCF7L2 gene polymorphisms and the risk of new-onset diabetes mellitus after liver transplantation in a Han Chinese population., J Hepatol
Kurzawski M et al., 2011, Association of transcription factor 7-like 2 (TCF7L2) gene polymorphism with posttransplant diabetes mellitus in kidney transplant patients medicated with tacrolimus., Pharmacol Rep
Pette et al., 1997, In vitro modulation of human, autoreactive MBP-specific CD4 + T-cell clones by cyclosporin A., J. Neuroimmunol.
Kusztal M et al., 2007, Possible association of CTLA-4 gene polymorphism with cyclosporine-induced gingival overgrowth in kidney transplant recipients., Transplant Proc
Beall et al., 1999, Cyclosporine-induced renal artery smooth muscle contraction is associated with increases in the phosphorylation of specific contractile regulatory proteins., Biochim. Biophys. Acta
Richter et al., 2003, Mycophenolate mofetil significantly reduces leukocyte graft infiltration after heterotopic cardiac transplantation in a rat model: comparative study with cyclosporine and FK 506., J. Heart Lung Transplant.
Poston et al., 1999, Antisense oligodeoxynucleotides prevent acute cardiac allograft rejection via a novel, nontoxic, highly efficient transfection method., Transplantation
Aoki et al., 1998, CsA-sensitive purine-box transcriptional regulator in bronchial epithelial cells contains NF45, NF90, and Ku., Am. J. Physiol.
Bianchi et al., 2003, Cyclosporine A up-regulates expression of matrix metalloproteinase 2 and vascular endothelial growth factor in rat heart., Int. Immunopharmacol.
Jin et al., 2004, Insights into cyclosporine A-induced atherosclerotic risk in transplant recipients: macrophage scavenger receptor regulation., Transplantation
Mampaso et al., 1993, Expression of adhesion molecules in allograft renal dysfunction. A distinct diagnostic pattern in rejection and cyclosporine nephrotoxicity., Transplantation
Ciesielski et al., 1998, Effects of cyclosporine A and methotrexate on CD18 expression in recipients of rat cardiac allografts., Transpl. Immunol.
Pyrzynska et al., 2002, Tumor suppressor p53 mediates apoptotic cell death triggered by cyclosporin A., J. Biol. Chem.
Gnoatto et al., 2003, Gene expression of extracellular matrix proteoglycans in human cyclosporin-induced gingival overgrowth., J. Periodontol.
Robida et al., 2000, Cyclosporin A selectively inhibits mitogen-induced cyclooxygenase-2 gene transcription in vascular smooth muscle cells., Mol. Pharmacol.
Mueller et al., 1990, Indicators of acute renal-transplant rejection in patients treated with cyclosporine., Clin. Chem.
Woillard JB et al., 2010, Risk of diarrhoea in a long-term cohort of renal transplant patients given mycophenolate mofetil: the significant role of the UGT1A8 2 variant allele., Br J Clin Pharmacol
Sun B et al., 2017, Influence of CYP3A and ABCB1 polymorphisms on cyclosporine concentrations in renal transplant recipients., Pharmacogenomics
Liu M et al., 2012, An iminosugar N-pentafluorobenzyl-1-deoxynojirimycin as a novel potential immunosuppressant for the treatment of Th2-related diseases., Bioorg Med Chem Lett
Chan et al., 1987, Cyclosporine and dexamethasone inhibit T-lymphocyte MHC class II antigens and IL-2 receptor expression in experimental autoimmune uveitis., Immunol. Invest.
Quteineh L et al., 2017, CRTC2 polymorphism as a risk factor for the incidence of metabolic syndrome in patients with solid organ transplantation., Pharmacogenomics J
Louhelainen et al., 2006, Lipoic acid supplementation prevents cyclosporine-induced hypertension and nephrotoxicity in spontaneously hypertensive rats., J. Hypertens.
Kurzawski M et al., 2005, The impact of thiopurine s-methyltransferase polymorphism on azathioprine-induced myelotoxicity in renal transplant recipients., Ther Drug Monit
Formea CM et al., 2004, Thiopurine S-methyltransferase genotype predicts azathioprine-induced myelotoxicity in kidney transplant recipients., Am J Transplant
Wuthrich et al., 1993, Effect of dexamethasone, 6-mercaptopurine and cyclosporine A on intercellular adhesion molecule-1 and vascular cell adhesion molecule-1 expression., Biochem. Pharmacol.

CYCLOSPORINE CAMLG

Interaction Score: 8.98

Interaction Types & Directionality:

binder

Interaction Info:

Trial Name Chiron

Novel drug target Established target

Trial Name cyclosporine,Restasis

PMIDs:
20674565 20927389 20602248 20637127 17016423 17139284 24682697 1502562

Sources:
TdgClinicalTrial
CYCLOSPORINE PPP3R2

Interaction Score: 6.98

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name FOV-1101,Prednisporin

Trial Name cyclosporine,Restasis

Novel drug target Established target

PMIDs:
20674565 17016423 17139284 7529175 23468591

Sources:
TdgClinicalTrial TEND
CYCLOSPORINE PPIA

Interaction Score: 2.74

Interaction Types & Directionality:

binder

inhibitor (inhibitory)

modulator

Interaction Info:

Mechanism of Interaction Cyclophilin A modulator

Direct Interaction yes

PMIDs:
20368803 17461417 17609268 16849427 16641261 20637127 12207006 19933795

Sources:
DTC ChemblInteractions NCI
CYCLOSPORINE VCAN

Interaction Score: 1.99

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14974815

Sources:
NCI
CYCLOSPORINE GZMA

Interaction Score: 1.99

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8420038

Sources:
NCI
CYCLOSPORINE UMOD

Interaction Score: 1.99

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28418009

Sources:
PharmGKB
CYCLOSPORINE ILF3

Interaction Score: 1.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9843854

Sources:
NCI
CYCLOSPORINE ERCC6

Interaction Score: 1.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9278484

Sources:
NCI
CYCLOSPORINE IMPDH2

Interaction Score: 0.85

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22960765 21996196 19770842 19617864 18444945

Sources:
PharmGKB
CYCLOSPORINE IL15

Interaction Score: 0.8

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11817607 11683823 11571455

Sources:
NCI
CYCLOSPORINE GABPA

Interaction Score: 0.66

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16612258

Sources:
NCI
CYCLOSPORINE HSPG2

Interaction Score: 0.66

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14974815

Sources:
NCI
CYCLOSPORINE TCF7L2

Interaction Score: 0.6

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23041303 21857094

Sources:
PharmGKB
CYCLOSPORINE VCAM1

Interaction Score: 0.5

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7694584

Sources:
NCI
CYCLOSPORINE POR

Interaction Score: 0.5

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29135906 24658827 24061445

Sources:
PharmGKB
CYCLOSPORINE ICAM3

Interaction Score: 0.5

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15732868

Sources:
NCI
CYCLOSPORINE CRTC2

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26644205

Sources:
PharmGKB
CYCLOSPORINE SAG

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
3123380

Sources:
NCI
CYCLOSPORINE MBP

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9184637

Sources:
NCI
CYCLOSPORINE LOH19CR1

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
3389144

Sources:
NCI
CYCLOSPORINE TPMT

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16044099 15476481

Sources:
PharmGKB
CYCLOSPORINE ABCA1

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15084924

Sources:
NCI
CYCLOSPORINE ABCB4

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1972761

Sources:
NCI
CYCLOSPORINE IL5

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9237106

Sources:
NCI
CYCLOSPORINE PPP3CA

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CYCLOSPORINE MUC16

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12169874

Sources:
NCI
CYCLOSPORINE CD80

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11841687

Sources:
NCI
CYCLOSPORINE ABCB11

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23129211

Sources:
DTC
CYCLOSPORINE CCL17

Interaction Score: 0.25

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18028503

Sources:
NCI
CYCLOSPORINE HSPB2

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10076049

Sources:
NCI
CYCLOSPORINE CYP3A7

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28952408

Sources:
PharmGKB
CYCLOSPORINE TBXA2R

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1385733

Sources:
NCI
CYCLOSPORINE UGT1A8

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20565459

Sources:
PharmGKB
CYCLOSPORINE ANPEP

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2337986

Sources:
NCI
CYCLOSPORINE ITGAL

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
14550820 10515383

Sources:
NCI
CYCLOSPORINE ITGB2

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8212167 9777701

Sources:
NCI
CYCLOSPORINE IL10

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18444945

Sources:
PharmGKB
CYCLOSPORINE CDKN1A

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11827957

Sources:
NCI
CYCLOSPORINE CTLA4

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18021981

Sources:
PharmGKB
CYCLOSPORINE FCGR3B

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17852453

Sources:
NCI
CYCLOSPORINE JAK1

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22101135

Sources:
DTC
CYCLOSPORINE ABCB1

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24992153 11754602 17964170 23017888 24720452 21348461 26107754 25536375 25240575 24088131 23922006 22886152 21806386 20030680 18717915 18576903 18444945 18334915 17206635 12966368 1972761

Sources:
DTC NCI PharmGKB
CYCLOSPORINE ABCG2

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16805961 21488686 17031644

Sources:
DTC NCI PharmGKB
CYCLOSPORINE IL2

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7529939 12135706

Sources:
NCI
CYCLOSPORINE MMP2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12639820

Sources:
NCI
CYCLOSPORINE FCGR3A

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17852453

Sources:
NCI
CYCLOSPORINE ABCC1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23017888 11189941

Sources:
DTC NCI
CYCLOSPORINE DDIT3

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15494209

Sources:
NCI
CYCLOSPORINE ABCC2

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
28624888 25163792

Sources:
DTC PharmGKB
CYCLOSPORINE AGTR1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17477024

Sources:
NCI
CYCLOSPORINE TNF

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18444945

Sources:
PharmGKB
CYCLOSPORINE PTGS2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10999939

Sources:
NCI
CYCLOSPORINE CYP3A5

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12673034

Sources:
NCI
CYCLOSPORINE NR1I2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24088131

Sources:
PharmGKB
CYCLOSPORINE CYP2C9

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
CYCLOSPORINE VDR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10609555

Sources:
NCI
CYCLOSPORINE CYP2C19

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
CYCLOSPORINE ATXN2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CYCLOSPORINE CYP1A2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
CYCLOSPORINE CYP2D6

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
CYCLOSPORINE CYP3A4

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
CYCLOSPORINE NFE2L2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

TEND: CYCLOSPORINE
- Version: 01-August-2011
Alternate Names:

CYCLOSPORINE Primary Drug Name

Drug Info:

Year of Approval 1983

Drug Class immunosuppressive agents

Publications:
TdgClinicalTrial: CYCLOSPORINE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications immunosuppressant

Drug Class Small molecule

FDA Approval approved

Publications:

NCI: CSA

Version: 14-September-2017

Alternate Names:

C406 NCI drug code

Drug Info:

Publications:

Wu, From bedside to bench drug-induced tubulointerstitial disease cyclosporine nephropathy study from models of cultured renal epithelial cells., Chang Gung Med J

Utsunomiya et al., 2000, Comparison of the accumulation and efflux kinetics of technetium-99m sestamibi and technetium-99m tetrofosmin in an MRP-expressing tumour cell line., Eur J Nucl Med

Niederer et al., 2005, Cypermethrin blocks a mitochondria-dependent apoptotic signal initiated by deficient N-linked glycosylation within the endoplasmic reticulum., Cell. Signal.

DTC: CYCLOSPORINE

Version: 02-September-2020

Alternate Names:

CHEMBL160 ChEMBL Drug ID

Drug Info:

Publications:

Hopkins S et al., 2010, SCY-635, a novel nonimmunosuppressive analog of cyclosporine that exhibits potent inhibition of hepatitis C virus RNA replication in vitro., Antimicrob Agents Chemother

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

Juvale K et al., 2012, 4-Substituted-2-phenylquinazolines as inhibitors of BCRP., Bioorg Med Chem Lett

NCI: CYCLOSPORINE

Version: 14-September-2017

Alternate Names:

C406 NCI drug code

Drug Info:

Publications:

Baran et al., 2007, Upregulation of multi drug resistance genes in doxorubicin resistant human acute myelogeneous leukemia cells and reversal of the resistance., Hematology

Herweijer et al., 1990, Expression of mdr1 and mdr3 multidrug-resistance genes in human acute and chronic leukemias and association with stimulation of drug accumulation by cyclosporine., J. Natl. Cancer Inst.

Mueller et al., 1990, Indicators of acute renal-transplant rejection in patients treated with cyclosporine., Clin. Chem.

NCI: CICLOSPORIN

Version: 14-September-2017

Alternate Names:

C406 NCI drug code

Drug Info:

Publications:

Toebak et al., 2008, Differential suppression of dendritic cell cytokine production by anti-inflammatory drugs., Br. J. Dermatol.

Kajita et al., 2006, Effect of imatinib mesilate on the disposition kinetics of ciclosporin in rats., J. Pharm. Pharmacol.

Usui et al., 2003, Induction of CYP3As in HepG2 cells by several drugs. Association between induction of CYP3A4 and expression of glucocorticoid receptor., Biol. Pharm. Bull.

PharmGKB: cyclosporine

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Abdel-Hady Algharably E et al., 2018, Effect of UMOD genotype on long-term graft survival after kidney transplantation in patients treated with cyclosporine-based therapy., Pharmacogenomics J

Pazik J et al., 2011, Lymphocyte counts in kidney allograft recipients are associated with IMPDH2 3757T>C gene polymorphism., Transplant Proc

Winnicki W et al., 2010, An inosine 5'-monophosphate dehydrogenase 2 single-nucleotide polymorphism impairs the effect of mycophenolic acid., Pharmacogenomics J

TTD: Cyclosporine
- Version: 2020.06.01
Alternate Names:

D0O3YF TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL160
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL160
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Trial Name	Chiron
Novel drug target	Established target
Trial Name	cyclosporine,Restasis

Trial Name	FOV-1101,Prednisporin
Trial Name	cyclosporine,Restasis
Novel drug target	Established target

Mechanism of Interaction	Cyclophilin A modulator
Direct Interaction	yes

binder
inhibitor (inhibitory)
modulator

CYCLOSPORINE Drug Record

CYCLOSPORINE chembl:CHEMBL160 ApprovedImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: binder

Interaction Info: Trial Name Chiron Novel drug target Established target Trial Name cyclosporine,Restasis

PMIDs: 20674565 20927389 20602248 20637127 17016423 17139284 24682697 1502562

Sources: TdgClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name FOV-1101,Prednisporin Trial Name cyclosporine,Restasis Novel drug target Established target

PMIDs: 20674565 17016423 17139284 7529175 23468591

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: binder inhibitor (inhibitory) modulator

Interaction Info: Mechanism of Interaction Cyclophilin A modulator Direct Interaction yes

PMIDs: 20368803 17461417 17609268 16849427 16641261 20637127 12207006 19933795

Sources: DTC ChemblInteractions NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14974815

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8420038

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 28418009

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9843854

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9278484

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22960765 21996196 19770842 19617864 18444945

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11817607 11683823 11571455

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16612258

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 14974815

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23041303 21857094

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 7694584

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29135906 24658827 24061445

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15732868

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 26644205

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 3123380

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9184637

Interaction Types & Directionality:

binder

Interaction Info:

Trial Name Chiron

Novel drug target Established target

Trial Name cyclosporine,Restasis

PMIDs:
20674565 20927389 20602248 20637127 17016423 17139284 24682697 1502562

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name FOV-1101,Prednisporin

Trial Name cyclosporine,Restasis

Novel drug target Established target

PMIDs:
20674565 17016423 17139284 7529175 23468591

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

binder

inhibitor (inhibitory)

modulator

Interaction Info:

Mechanism of Interaction Cyclophilin A modulator

Direct Interaction yes

PMIDs:
20368803 17461417 17609268 16849427 16641261 20637127 12207006 19933795

Sources:
DTC ChemblInteractions NCI

Interaction Types & Directionality:

n/a

PMIDs:
14974815

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
8420038

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
28418009

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
9843854

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
9278484

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
22960765 21996196 19770842 19617864 18444945

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
11817607 11683823 11571455

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16612258

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
14974815

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
23041303 21857094

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
7694584

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
29135906 24658827 24061445

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
15732868

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
26644205

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
3123380

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
9184637

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
3389144

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16044099 15476481

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
15084924

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
1972761

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
9237106

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
12169874