PharmGKB: The Pharmacogenomics Knowledge Base

Drug/Small Molecule:
cyclosporine

2D structure

Overview

Generic Names: Ciclosporin; Cyclosporin; Cyclosporin A; cyclosporine
Trade Names: Gengraf (Abbott labs); Neoral (Novartis); Restasis; Restasis (Allergan Inc); Sandimmune (Novartis); Sangcya
PharmGKB Accession Id: PA449167

Description

A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed). (source: Drug Bank)

Indication

For treatment of transplant rejection, rheumatoid arthritis, severe psoriasis (source: Drug Bank)

ATC Therapeutic Category

  • L04AA:Selective immunosuppressants

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Cyclosporine binds to cyclophillin. The complex then inhibits calcineurin which is normally responsible for activating transcription of interleukin 2. Cyclosporine also inhibits lymphokine production and interleukin release. In ophthalmic applications, the precise mechanism of action is not known. Cyclosporine emulsion is thought to act as a partial immunomodulator in patients whose tear production is presumed to be suppressed due to ocular inflammation associated with keratoconjunctivitis sicca. (source: Drug Bank)

Pharmacology

Used in immunosuppression for prophylactic treatment of organ transplants, cyclosporine exerts specific and reversible inhibition of immunocompetent lymphocytes in the G0-or G1-phase of the cell cycle. T-lymphocytes are preferentially inhibited. The T1-helper cell is the main target, although the T1-suppressor cell may also be suppressed. Sandimmune (cyclosporine) also inhibits lymphokine production and release including interleukin-2. (source: Drug Bank)

Food Interactions

Avoid salt substitutes containing potassium.
Avoid taking with grapefruit or grapefruit juice as grapefruit can significantly increase serum levels of this product.
Red wine may reduce cyclosporine levels due to increased metabolism, therefore it appears prudent to avoid red wine (white wine does not appear to affect cyclosporine metabolism).
Take without regard to meals. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic, extensively metabolized. (source: Drug Bank)

Protein Binding

Approximately 90% is bound to proteins, primarily lipoproteins. (source: Drug Bank)

Absorption

The absorption of cyclosporine from the gastrointestinal tract is incomplete and variable. Compared to an intravenous infusion, the absolute bioavailability of the oral solution is approximately 30% based upon the results in 2 patients. (source: Drug Bank)

Toxicity

The oral LD<sub>50</sub> is 2329 mg/kg in mice, 1480 mg/kg in rats, and > 1000 mg/kg in rabbits. The I.V. LD<sub>50</sub> is 148 mg/kg in mice, 104 mg/kg in rats, and 46 mg/kg in rabbits. (source: Drug Bank)

Isomeric SMILES Code:

CC[C@H]1C(=O)N(CC(=O)N([C@H](C(=O)N[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N[C@@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N([C@H](C(=O)N1)[C@@H]([C@H](C)C/C=C/C)O)C)C(C)C)C)CC(C)C)C)CC(C)C)C)C)C)CC(C)C)C)C(C)C)CC(C)C)C)C (source: Drug Bank)

Curated Annotations (Curated Annotation)

  1. rs231775 at chr2:204440959 in CTLA4
    A study in 82 renal transplant recipients suggests that appearance of an adenosine allele(A) in this SNP of the CTLA-4 gene may be a permissive element for cyclosporine-induced gingival overgrowth.
    Related Drugs:
    cyclosporine
    Related Diseases:
    Gingival Overgrowth
    Evidence:
    PMID:18021981
  2. rs1042597 at chr2:234191610 in UGT1A8
    Risk or phenotype-associated allele: UGT1A8 c.518G, p173Gly, UGT1A8*2. Phenotype: The UGT1A8 C518G SNP tended to be associated with mycophenolic acid (MPA) C(0) (p = 0.0130), Cmax (p = 0.0368), and AUC(0-12 hours) (p = 0.0171), but not with exposure to its glucuronide, MPAG. Study size: 115. Study population/ethnicity: Caucasian cohort from the SOPHIE study who received cyclosporine in addition to Mycophenylate mofetil (MMF). Significance metric(s): p < 0.04. Type of association: GN; PK
    Variant Name:
    UGT1A8: c.518C>G, mRNA 581C>G, p.Ala173Gly, UGT1A8*2
    Related Drugs:
    cyclosporine, mycophenolate mofetil, mycophenolic acid
    Related Diseases:
    Organ Transplantation
    Evidence:
    PMID:19890249
  3. rs1045642 at chr7:86976581 in ABCB1
    rs1045642 is associated with altered inhibition by verapamil and cyclosporin A of substrate uptake in vitro.
    Variant Name:
    ABCB1:C3435T
    Related Drugs:
    cyclosporine, verapamil
    Evidence:
    PMID:17185560
  4. rs1045642 at chr7:86976581 in ABCB1
    Functional study of rs1045642 (3435C>T) and rs1128503 (2677G>T/A): in LLC-PK1 cells expressing wild-type (2677G/3435C) or polymorphic (2677G/3435T, 2677A/3435C, 2677A/3435T, 2677T/3435C, 2677T/3435T) constructs of ABCB1 in vitro, no significant differences were observed in transcellular efflux of structurally diverse P-gp substrates, verapamil, digoxin, vinblastine or cyclosporin A.
    Variant Name:
    ABCB1: c.3435C>T, mRNA 3853C>T
    Related Drugs:
    cyclosporine, digoxin, verapamil, vinblastine
    Evidence:
    PMID:12781336
  5. rs1045642 at chr7:86976581 in ABCB1
    Functional study of rs1045642 (3435C>T) and rs2032582 (2677G>T/A): in LLC-PK1 cells expressing wild-type (2677G/3435C) or polymorphic (2677G/3435T, 2677A/3435C, 2677A/3435T, 2677T/3435C, 2677T/3435T) constructs of ABCB1 in vitro, no significant differences were observed in transcellular efflux of structurally diverse P-gp substrates, verapamil, digoxin, vinblastine or cyclosporin A.
    Variant Name:
    ABCB1: c.3435C>T, mRNA 3853C>T, p.Ile1145Ile
    Related Drugs:
    cyclosporine, digoxin, verapamil, vinblastine
    Evidence:
    PMID:12781336
  6. rs1045642 at chr7:86976581 in ABCB1
    Risk or phenotype-associated allele: None. Phenotype: Efflux of P-glycoprotein substrates (verapamil; digoxin; vinblastine; cyclosporin A) in vitro were not significantly affected by combined mutations for rs1128503 (2677G>T/A) and rs1045642 (3435C>T) in LLC-PK1 cell lines. Study size: Triplicate cell assays. Study population/ethnicity: N/A. Significance metric(s): Not significant, p > 0.05. Type of association: FA
    Variant Name:
    ABCB1:3435C>T, mRNA 3853C>T, Ile1145Ile
    Related Drugs:
    cyclosporine, digoxin, verapamil, vinblastine
    Evidence:
    PMID:12781336
  7. rs1045642 at chr7:86976581 in ABCB1
    There was no significant association between the genotype C3435T distribution and the risk of Cyclosporin A failure in steroid resistance ulcerative colitis (p = 0.23).
    Variant Name:
    ABCB1:3435C>T, mRNA 3853C>T, Ile1145Ile
    Related Drugs:
    cyclosporine
    Related Diseases:
    Colitis, Ulcerative
    Evidence:
    PMID:17206635
  8. rs2032582 at chr7:86998554 in ABCB1
    Functional study of rs1045642 (3435C>T) and rs2032582 (2677G>T/A): in LLC-PK1 cells expressing wild-type (2677G/3435C) or polymorphic (2677G/3435T, 2677A/3435C, 2677A/3435T, 2677T/3435C, 2677T/3435T) constructs of ABCB1 in vitro, no significant differences were observed in transcellular efflux of structurally diverse P-gp substrates, verapamil, digoxin, vinblastine or cyclosporin A.
    Variant Name:
    ABCB1: c.2677G>T/A, mRNA 3095G>T/A, p.Ala893Ser/Thr
    Related Drugs:
    cyclosporine, digoxin, verapamil, vinblastine
    Evidence:
    PMID:12781336
  9. rs2032582 at chr7:86998554 in ABCB1
    peak blood concentration of cyclosporin A (CsA) was significantly lower in in myasthenia gravis patients harboring the 2677 T allele (893Ser); and trough CsA levels were significantly greater in 2677 TT homozygotes versus CC homozygotes
    Variant Name:
    ABCB1:2677G>T/A, mRNA 3095G>T/A, Ala893Ser/Thr
    Related Drugs:
    cyclosporine
    Related Diseases:
    Myasthenia Gravis
    Evidence:
    PMID:18717915
  10. rs2032582 at chr7:86998554 in ABCB1
    Functional study of rs1045642 (3435C>T) and rs1128503 (2677G>T/A): in LLC-PK1 cells expressing wild-type (2677G/3435C) or polymorphic (2677G/3435T, 2677A/3435C, 2677A/3435T, 2677T/3435C, 2677T/3435T) constructs of ABCB1 in vitro, no significant differences were observed in transcellular efflux of structurally diverse P-gp substrates, verapamil, digoxin, vinblastine or cyclosporin A.
    Variant Name:
    ABCB1: c.2677G>T/A, mRNA 3095G>T/A, p.Ala893Ser/Thr
    Related Drugs:
    cyclosporine, digoxin, verapamil, vinblastine
    Evidence:
    PMID:12781336
  11. rs2032582 at chr7:86998554 in ABCB1
    There is a significant association between the G2677T/A polymorphism distribution and the risk for cyclosporin A (CsA) failure in patients from France and Belgium with steroid resistance ulcerative colitis (p = 0.0001), defined as requiring colectomy within 30 days of CsA initiation. The 2677 TT genotype was significantly associated with the risk compared with the two other genotypes (odds ratio, 3.77; 95% confidence interval, 1.42-9.97, p = 0.007).
    Variant Name:
    ABCB1:2677G>T/A, mRNA 3095G>T/A, Ala893Ser/Thr
    Related Drugs:
    cyclosporine
    Related Diseases:
    Colitis, Ulcerative
    Evidence:
    PMID:17206635
  12. rs1128503 at chr7:87017537 in ABCB1
    peak blood concentration of cyclosporin A (CsA) was significantly lower in myasthenia gravis patients harboring the 1236 T allele; and trough CsA levels were significantly greater in 1236 TT homozygotes versus CC homozygotes
    Variant Name:
    ABCB1:1236T>C, mRNA 1654T>C, Gly412Gly
    Related Drugs:
    cyclosporine
    Related Diseases:
    Myasthenia Gravis
    Evidence:
    PMID:18717915
  13. rs1128503 at chr7:87017537 in ABCB1
    Risk or phenotype-associated allele: None. Phenotype: Efflux of P-glycoprotein substrates (verapamil; digoxin; vinblastine; cyclosporin A) in vitro were not significantly affected by combined mutations for rs1128503 (2677G>T/A) and rs1045642 (3435C>T) in LLC-PK1 cell lines. Study size: Triplicate cell assays. Study population/ethnicity: N/A. Significance metric(s): Not significant, p > 0.05. Type of association: FA
    Variant Name:
    ABCB1:2677G>T/A, mRNA 3095G>T/A, Ala893Ser/Thr
    Related Drugs:
    cyclosporine, digoxin, verapamil, vinblastine
    Evidence:
    PMID:12781336
  14. rs776746 at chr7:99108475 in CYP3A, CYP3A5
    Phenotype/associated allele: A meta-analysis of articles in PubMed in which dose-adjusted blood concentrations of Cyclosporine were measured in renal transplant patients implied that patients carrying the CYP3A5*3/*3 genotype will require a lower dose of Cyclosporine to reach target levels compared with CYP3A5*1/*1 or *1/*3 carriers. Study size: 15 studies ; 1742 subjects. Study population/ethnicity: France, the Netherlands, Belgium, United States, Germany, China, India ,Singapore and Malaysia. Type of association: PK.
    Variant Name:
    CYP3A5*3
    Related Drugs:
    cyclosporine
    Related Diseases:
    Organ Transplantation, Transplantation
    Evidence:
    PMID:20368718
  15. rs2740574 at chr7:99220032 in CYP3A, CYP3A4
    Risk or phenotype-associated allele: CYP3A4*1B (rs2740574) G allele. Phenotype: Of 108 renal transplant patients taking cyclosporine (CsA), 94 (87.1%) were carriers of the CYP3A4*1/*1 (rs2740574 AA) wild-type genotype, 9 (8.3%) were heterozygous CYP3A4*1/*1B (rs2740574 AG), and 5 (4.6%) were homozygous CYP3A4*1B (rs2740574 GG). There was no significant genotypic association between the CYP3A4*1B allele and CsA dose requirement (mg/kg), C(0) (ng/ml), or dose-adjusted C(0) (ng/ml per mg/kg) at 3 and 12 months after transplantation. Of 64 patients taking tacrolimus, 7 (10.9%) were heterozygous CYP3A4*1/*1B (rs2740574 AG), and 3 (4.7%) were homozygous CYP3A4*1B (rs2740574 GG). In these 64 patients taking tacrolimus, a trend was observed toward a lower dose-adjusted C(0) for CYP3A4*1B allele carriers (rs2740574 GA or GG), as compared to CYP3A4*1/*1 (rs2740574 AA) genotype carriers (p = 0.01). Comparison between all CYP3A4*1B (rs2740574) G allele carriers (n = 10) and carriers of the CYP3A4*1/*1 (rs2740574 AA) genotype (n = 54) showed a significant difference in tacrolimus dose-adjusted C(0) (p = 0.003), which remained statistically significant at month 12. A significantly higher tacrolimus dose was required in patients carrying the CYP3A4*1B (G) allele compared to CYP3A4*1/*1 (AA) genotype carriers at month 3 (p = 0.01) and at month 12 (p = 0.03). Study size: 108 administered cyclosporine, 64 administered tacrolimus. Study population/ethnicity: Renal transplant recipients from the outpatient clinic of the Erasmus Medical Center in Rotterdam in the Netherlands, who had received a renal graft at least 1 year before the start of the study and were administered CsA (n = 108) or tacroliums (n = 64). Significance metric(s): Not significant for CsA; p = (0.003 - 0.03) for tacrolimus. Type of association: GN; PK.
    Variant Name:
    CYP3A4*1B, CYP3A4-V, 5'-flanking region -392A>G; -392 G allele
    Related Drugs:
    cyclosporine, tacrolimus
    Related Diseases:
    Organ Transplantation, Transplantation
    Evidence:
    PMID:12966368
  16. rs717620 at chr10:101532568 in ABCC2, NANOGP6
    Risk or phenotype-associated allele: 5'UTR (-)24C>T, mRNA 118C>T. Phenotype: In patients who received cyclosporine in addition to mycophenylate mofetil (MMF), there was a trend toward an association between the ABCC2 C-24T SNP and mycophenolic acid (MPA) AUC(0-12 h), but without any apparent additive effect: carriers of the CT genotype were associated with higher MPA AUC(0-12 h) compared with TT and CC homozygotes. Study size: 115. Study population/ethnicity: Caucasian cohort from the SOPHIE study cotreated with mycophenylate mofetil (MMF) and cyclosporine. Significance metric(s): p = 0.0087. Type of association: GN; PK
    Variant Name:
    ABCC2: 5'UTR (-)24C>T, mRNA 118C>T
    Related Drugs:
    cyclosporine, mycophenolate mofetil, mycophenolic acid
    Related Diseases:
    Organ Transplantation
    Evidence:
    PMID:19890249
  17. rs7311358 at chr12:20907027 in SLCO1B3
    Risk or phenotype-associated allele: SCLO1B3 haplotype formed by 112Ser>Ala (rs4149117, 334T>G) and 223Met>Ile (rs7311358, 699G>A). Phenotype: HEK293 cells transiently expressing the SCLO1B3 334G-699A haplotype or reference haplotype were incubated in the presence of increasing concentrations of mycophenolic acid phenyl-glucuronide (MPAG) for 10 min. The uptake of MPAG according to the SCLO1B3 334G-699A haplotype was markedly lower than in cells expressing the reference sequence 334T-669G. Type of association: GN; FA; PK
    Variant Name:
    SCLO1B3: exon 7 c.699G>A, mRNA 825G>A, p.Met233Ile
    Related Drugs:
    cyclosporine, mycophenolate mofetil, sirolimus, tacrolimus
    Related Diseases:
    Organ Transplantation
    Evidence:
    PMID:19890249
Variant names are different names that have been used in the literature and other resources to refer to the same variant.

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
ABCB1
  • CO
  • PD
  • PK
  • FA
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ABCC2
  •   
  • PD
  • PK
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
ABCG2
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available No genotype data Literature annotations available Not annotated
BCL2
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
CTLA4
  •   
  • PD
  •   
  •   
  • GN
Publications, Variants
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP1A2
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2B6
  • CO
  • PD
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C19
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP2C8
  • CO
  • PD
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C9
  •   
  • PD
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2D6
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data Genotype Data Available Literature annotations available Has annotations
CYP2J2
  • CO
  •   
  • PK
  • FA
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP3A
  •   
  •   
  •   
  •   
  •   
Variants
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  • CO
  • PD
  • PK
  •   
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
  • CO
  • PD
  • PK
  •   
  • GN
Publications, Variants
Phenotype data available Genotype Data Available Literature annotations available Not annotated
GSTM1
  • CO
  • PD
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
GSTP1
  • CO
  • PD
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
GSTT1
  • CO
  • PD
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
HLA-A
  •   
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
HLA-DRB1
  •   
  • PD
  •   
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
MTHFR
  • CO
  • PD
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
NR1I2
  •   
  •   
  • PK
  •   
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
RCAN1
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SLC30A8
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Has annotations
SLCO1B1
  •   
  • PD
  • PK
  • FA
  • GN
Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
UGT1A8
  •   
  •   
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
UGT1A9
  •   
  •   
  • PK
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
UGT2B7
  •   
  •   
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
VDR
  • CO
  • PD
  • PK
  •   
  •   
Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ABCB1 Uncurated Annotation (source: Drug Bank)
CAMLG Uncurated Annotation (source: Drug Bank)
PPIA Uncurated Annotation (source: Drug Bank)
PPP3R2 Uncurated Annotation (source: Drug Bank)

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Not annotated
docetaxel
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
doxorubicin
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
ezetimibe
  •   
  • PD
  • PK
  •   
  •   
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
irinotecan
  •   
  •   
  •   
  • FA
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
SN-38
  •   
  •   
  •   
  • FA
  •   
Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
acetazolamide Uncurated Annotation Acetazolamide increases the effect and toxicity of cyclosporine (source: Drug Bank)
allopurinol Uncurated Annotation Allopurinol increases the effect and toxicity of cyclosporine (source: Drug Bank)
amiodarone Uncurated Annotation Amiodarone increases the effect and toxicity of cyclosporine (source: Drug Bank)
amobarbital Uncurated Annotation The barbiturate increases the effect of cyclosporine (source: Drug Bank)
amphotericin b Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
amprenavir Uncurated Annotation The protease inhibitor increases the effect of cyclosporine (source: Drug Bank)
atazanavir Uncurated Annotation Atazanavir increases the effect and toxicity of immunosuppressant (source: Drug Bank)
atorvastatin Uncurated Annotation Possible myopathy and rhabdomyolysis (source: Drug Bank)
azithromycin Uncurated Annotation The macrolide increases the effect of cyclosporine (source: Drug Bank)
bosentan Uncurated Annotation Increases the effect and toxicity of bosentan (source: Drug Bank)
bupropion Uncurated Annotation Bupropion decreases the effect of cyclosporine (source: Drug Bank)
butalbital Uncurated Annotation The barbiturate increases the effect of cyclosporine (source: Drug Bank)
carbamazepine Uncurated Annotation Carbamazepine decreases the effect of cyclosporine (source: Drug Bank)
carvedilol Uncurated Annotation Carvedilol increases the effect and toxicity of cyclosporine (source: Drug Bank)
cerivastatin Uncurated Annotation Possible myopathy and rhabdomyolysis (source: Drug Bank)
chloramphenicol Uncurated Annotation Chloramphenicol increases the effect of cyclosporine (source: Drug Bank)
chloroquine Uncurated Annotation Chloroquine increases the effect of cyclosporine (source: Drug Bank)
cilastatin Uncurated Annotation Imipenem increases the effect and toxicity of cyclosporine (source: Drug Bank)
ciprofloxacin Uncurated Annotation The quinolone increases the effect and toxicity of cyclosporine (source: Drug Bank)
clarithromycin Uncurated Annotation The macrolide increases the effect of cyclosporine (source: Drug Bank)
clindamycin Uncurated Annotation Clindamycin decreases the effect of cyclosporine (source: Drug Bank)
colchicine Uncurated Annotation Increased toxicity of both drugs (source: Drug Bank)
diclofenac Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
digoxin Uncurated Annotation Increases the effect of digoxin (source: Drug Bank)
diltiazem Uncurated Annotation Diltiazem increases the effect and toxicity of cyclosporine (source: Drug Bank)
efavirenz Uncurated Annotation Efavirenz decreases the levels of cyclosporine (source: Drug Bank)
erythromycin Uncurated Annotation The macrolide increases the effect of cyclosporine (source: Drug Bank)
ethinyl estradiol Uncurated Annotation The contraceptive increases the effect and toxicity of cyclosporine (source: Drug Bank)
etodolac Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
etoposide Uncurated Annotation Increases the effect of etoposide (source: Drug Bank)
ezetimibe Uncurated Annotation Increases the effect and toxicity of ezetimibe (source: Drug Bank)
fenoprofen Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
fluconazole Uncurated Annotation Fluconazole increases the effect of the immunosuppressant (source: Drug Bank)
fluoxetine Uncurated Annotation The antidepressant increases the effect and toxicity of cyclosporine (source: Drug Bank)
flurbiprofen Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
fluvastatin Uncurated Annotation Possible myopathy and rhabdomyolysis (source: Drug Bank)
fosamprenavir Uncurated Annotation The protease inhibitor increases the effect of cyclosporine (source: Drug Bank)
foscarnet Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
glibenclamide Uncurated Annotation The sulfonylurea increases the effect of cyclosporine (source: Drug Bank)
glimepiride Uncurated Annotation The sulfonylurea increases the effect of cyclosporine (source: Drug Bank)
glipizide Uncurated Annotation The sulfonylurea increases the effect of cyclosporine (source: Drug Bank)
griseofulvin Uncurated Annotation Griseofulvin decreases the effect of cyclosporine (source: Drug Bank)
hexobarbital Uncurated Annotation The barbiturate increases the effect of cyclosporine (source: Drug Bank)
ibuprofen Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
imatinib Uncurated Annotation Imatinib increases the effect and toxicity of cyclosporine (source: Drug Bank)
imipenem Uncurated Annotation Imipenem increases the effect and toxicity of cyclosporine (source: Drug Bank)
indinavir Uncurated Annotation The protease inhibitor increases the effect of cyclosporine (source: Drug Bank)
indomethacin Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
itraconazole Uncurated Annotation The imidazole increases the effect of immunosuppressant (source: Drug Bank)
ketoconazole Uncurated Annotation The imidazole increases the effect of immunosuppressant (source: Drug Bank)
ketoprofen Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
lovastatin Uncurated Annotation Possible myopathy and rhabdomyolysis (source: Drug Bank)
meclofenamic acid Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
mefenamic acid Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
melphalan Uncurated Annotation Melphalan increases toxicity of cyclosporine (source: Drug Bank)
mephenytoin Uncurated Annotation The hydantoin decreases the effect of cyclosporine (source: Drug Bank)
mestranol Uncurated Annotation The contraceptive increases the effect and toxicity of cyclosporine (source: Drug Bank)
methotrexate Uncurated Annotation Increases the effect and toxicity of methotrexate (source: Drug Bank)
methylphenidate Uncurated Annotation Methylphenidate increases the effect and toxicity of cyclosporine (source: Drug Bank)
methylphenobarbital Uncurated Annotation The barbiturate increases the effect of cyclosporine (source: Drug Bank)
metoclopramide Uncurated Annotation Metoclopramide increases serum levels of cyclosporine (source: Drug Bank)
modafinil Uncurated Annotation Modafinil decreases the effect of cyclosporine (source: Drug Bank)
nabumetone Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
nafcillin Uncurated Annotation Nafcillin alters serum levels of cyclosporine (source: Drug Bank)
naproxen Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
nefazodone Uncurated Annotation The antidepressant increases the effect and toxicity of cyclosporine (source: Drug Bank)
nelfinavir Uncurated Annotation The protease inhibitor increases the effect of cyclosporine (source: Drug Bank)
nicardipine Uncurated Annotation Nicardipine increases the effect and toxicity of cyclosporine (source: Drug Bank)
nifedipine Uncurated Annotation Increased risk of gingivitis (source: Drug Bank)
norfloxacin Uncurated Annotation The quinolone increases the effect and toxicity of cyclosporine (source: Drug Bank)
octreotide Uncurated Annotation Octreotide decreases the effect of cyclosporine (source: Drug Bank)
omeprazole Uncurated Annotation Omeprazole increases the effect and toxicity of cyclosporine (source: Drug Bank)
oxaprozin Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
oxcarbazepine Uncurated Annotation Oxcarbazepine decreases the effect of cyclosporine (source: Drug Bank)
pentobarbital Uncurated Annotation The barbiturate increases the effect of cyclosporine (source: Drug Bank)
phenobarbital Uncurated Annotation The barbiturate increases the effect of cyclosporine (source: Drug Bank)
phenytoin Uncurated Annotation The hydantoin decreases the effect of cyclosporine (source: Drug Bank)
piroxicam Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
posaconazole Uncurated Annotation Increased level of cyclosporine (source: Drug Bank)
pravastatin Uncurated Annotation Possible myopathy and rhabdomyolysis (source: Drug Bank)
primidone Uncurated Annotation The barbiturate increases the effect of cyclosporine (source: Drug Bank)
probucol Uncurated Annotation Probucol decreases the effect of cyclosporine (source: Drug Bank)
propafenone Uncurated Annotation Propafenone increases the effect and toxicity of cyclosporine (source: Drug Bank)
pyrazinamide Uncurated Annotation Pyrazinamide decreases the effect of cyclosporine (source: Drug Bank)
repaglinide Uncurated Annotation Increases repaglinide's effect (source: Drug Bank)
rifabutin Uncurated Annotation The rifamycin decreases the effect of cyclosporine (source: Drug Bank)
rifampin Uncurated Annotation The rifamycin decreases the effect of cyclosporine (source: Drug Bank)
ritonavir Uncurated Annotation The protease inhibitor increases the effect of cyclosporine (source: Drug Bank)
rosuvastatin Uncurated Annotation Increases the effect and toxicity of rosuvastatin (source: Drug Bank)
saquinavir Uncurated Annotation The protease inhibitor increases the effect of cyclosporine (source: Drug Bank)
sibutramine Uncurated Annotation Sibutramine increases the effect and toxicity of cyclosporine (source: Drug Bank)
simvastatin Uncurated Annotation Possible myopathy and rhabdomyolysis (source: Drug Bank)
sirolimus Uncurated Annotation Increases the effect and toxicity of sirolimus (source: Drug Bank)
sulfadiazine Uncurated Annotation The sulfonamide decreases the effect of cyclosporine (source: Drug Bank)
sulfamethazine Uncurated Annotation The sulfonamide decreases the effect of cyclosporine (source: Drug Bank)
sulfamethoxazole Uncurated Annotation The sulfonamide decreases the effect of cyclosporine (source: Drug Bank)
sulfasalazine Uncurated Annotation The sulfonamide decreases the effect of cyclosporine (source: Drug Bank)
sulfinpyrazone Uncurated Annotation Sulfinpyrazone decreases the effect of cyclosporine (source: Drug Bank)
sulindac Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
tacrolimus Uncurated Annotation Additive toxicities for these agents (source: Drug Bank)
telithromycin Uncurated Annotation Telithromycin may possibly increase this agent effect/toxicity (source: Drug Bank)
tenoxicam Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
terbinafine Uncurated Annotation Terbinafine decreases the effect of cyclosporine (source: Drug Bank)
ticlopidine Uncurated Annotation Ticlopidine decreases the effect of cyclosporine (source: Drug Bank)
tolmetin Uncurated Annotation Monitor for nephrotoxicity (source: Drug Bank)
troglitazone Uncurated Annotation Troglitazone decreases the effect of the immunosuppressant (source: Drug Bank)
troleandomycin Uncurated Annotation The macrolide increases the effect of cyclosporine (source: Drug Bank)
ursodeoxycholic acid Uncurated Annotation Ursodiol increases the levels of cyclosporine (source: Drug Bank)
verapamil Uncurated Annotation Verapamil increases the effect of cyclosporine (source: Drug Bank)
voriconazole Uncurated Annotation Voriconazole increases the effect and toxicity of cyclosporine (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Anemia, Aplastic
  •   
  • PD
  •   
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Carotid Artery Diseases
  •   
  • PD
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Diabetes Mellitus
  •   
  •   
  •   
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Drug Toxicity
  • CO
  • PD
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Epilepsy
  •   
  •   
  • PK
  • FA
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Gingival Overgrowth
  •   
  • PD
  •   
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Graft vs Host Disease
  • CO
  • PD
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
nephrotoxicity
  • CO
  •   
  •   
  •   
  • GN
Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
Organ Transplantation
  • CO
  •   
  • PK
  •   
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Retinal Diseases
  •   
  •   
  •   
  •   
  • GN
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Rhabdomyolysis
  •   
  • PD
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
Transplantation
  • CO
  • PD
  • PK
  • FA
  • GN
Publications, Variants
No phenotype data No genotype data Literature annotations available Not annotated
Uveitis
  •   
  •   
  •   
  •   
  • GN
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Physicochemical determinants of human renal clearance

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00091
ChEBI ID:
4031
KEGG Compound ID:
C05086
KEGG Drug ID:
D00184
PubChem Compound ID:
6435893
PubChem Substance ID:
199551

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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