Cyclosporine

Mechanism-of-action classes: Calcineurin Inhibitors; Cytochrome P450 3A4 Inhibitors; Immunologic Adjuvants; P-Glycoprotein Inhibitors; Unknown Cellular or Molecular Interaction.

• Kidney, Liver, and Heart Transplantation Cyclosporine capsules (modified) is indicated for the prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants. Cyclosporine capsules (modified) has been used in combination with azathioprine and corticosteroids.

• General Cyclosporine capsules (modified) is contraindicated in patients with a hypersensitivity to cyclosporine or to any of the ingredients of the formulation. Rheumatoid Arthritis Rheumatoid arthritis patients with abnormal renal function, uncontrolled hypertension, or malignancies should not receive cyclosporine capsules, (modified).contraindicated

Cyclosporine capsules (modified) has increased bioavailability in comparison to Sandimmune ® . Cyclosporine capsules (modified) and Sandimmune ® are not bioequivalent and cannot be used interchangeably without physician supervision. The daily dose of cyclosporine capsules (modified) should always be given in two divided doses (BID). It is recommended that cyclosporine capsules (modified) be administered on a consistent schedule with regard to time of day and relation to meals. Grapefruit and grapefruit juice affect metabolism, increasing blood concentration of cyclosporine, thus should be avoided. Specific Populations Renal Impairment in Kidney, Liver, and Heart Transplantation Cyclosporine undergoes minimal renal elimination and its pharmacokinetics do not appear to be significantly altered in patients with end-stage renal disease who receive routine hemodialysis treatments (see CLINICAL PHARMACOLOGY ). However, due to its nephrotoxic potential (see WARNINGS ), careful monitoring of renal function is recommended; cyclosporine dosage should be reduced if indicated (see WARNINGS and PRECAUTIONS ). Renal Impairment in Rheumatoid Arthritis and Psoriasis Patients with impaired renal function should not receive cyclosporine (see CONTRAINDICATIONS, WARNINGS and PRECAUTIONS ). Hepatic Impairment The clearance of cyclosporine may be significantly reduced in severe liver disease patients ( See CLINICAL PHARMACOLOGY ).

(See also BOXED WARNING ) All Patients Cyclosporine, the active ingredient of cyclosporine capsules, (modified), can cause nephrotoxicity and hepatotoxicity. The risk increases with increasing doses of cyclosporine. Renal dysfunction including structural kidney damage is a potential consequence of cyclosporine capsules (modified) and therefore renal function must be monitored during therapy. Care should be taken in using cyclosporine with nephrotoxic drugs (see PRECAUTIONS). Patients receiving cyclosporine capsules (modified) require frequent monitoring of serum creatinine (see Special Monitoring under DOSAGE AND ADMINISTRATION ). Elderly patients should be monitored with particular care, since decreases in renal function also occur with age. If patients are not properly monitored and doses are not properly adjusted, cyclosporine therapy can be associated with the occurrence of structural kidney damage and persistent renal dysfunction. An increase in serum creatinine and BUN may occur during cyclosporine capsules (modified) therapy and reflect a reduction in the glomerular filtration rate. Impaired renal function at any time requires close monitoring, and frequent dosage adjustment may be indicated. The frequency and severity of serum creatinine elevations increase with dose and duration of cyclosporine therapy. These elevations are likely to become more pronounced without dose reduction or discontinuation.

Kidney, Liver, and Heart Transplantation The principal adverse reactions of cyclosporine therapy are renal dysfunction, tremor, hirsutism, hypertension, and gum hyperplasia. Hypertension Hypertension, which is usually mild to moderate, may occur in approximately 50% of patients following renal transplantation and in most cardiac transplant patients. Glomerular Capillary Thrombosis Glomerular capillary thrombosis has been found in patients treated with cyclosporine and may progress to graft failure. The pathologic changes resembled those seen in the hemolytic-uremic syndrome and included thrombosis of the renal microvasculature, with platelet-fibrin thrombi occluding glomerular capillaries and afferent arterioles, microangiopathic hemolytic anemia, thrombocytopenia, and decreased renal function. Similar findings have been observed when other immunosuppressives have been employed post-transplantation. Hypomagnesemia Hypomagnesemia has been reported in some, but not all, patients exhibiting convulsions while on cyclosporine therapy. Although magnesium-depletion studies in normal subjects suggest that hypomagnesemia is associated with neurologic disorders, multiple factors, including hypertension, high dose methylprednisolone, hypocholesterolemia, and nephrotoxicity associated with high plasma concentrations of cyclosporine appear to be related to the neurological manifestations of cyclosporine toxicity.

Pregnancy Risk Summary Available data from published literature, including the Transplant Pregnancy Registry International, observational cohort studies, case-controlled studies, meta-analysis, case series, and case reports, over decades of use with cyclosporine in pregnancy have not identified a drug associated risk of major birth defects, or miscarriage. Adverse maternal or fetal outcomes including hypertension, preeclampsia, preterm birth, and low birth weight are increased in patients treated with cyclosporine. However, patients receiving cyclosporine during pregnancy have underlying medical conditions and may be treated with concomitant medications that limit the interpretability of these findings (see Data) . Embryo-fetal developmental (EFD) studies in rats and rabbits with cyclosporine have shown embryo-fetal toxicity at dose levels below the maximum recommended human dose (MRHD) based on body surface area (BSA). The alcohol content of cyclosporine capsules, (modified) should be taken into account when given to pregnant women (see WARNINGS , Special Excipients). The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S.

Metabolism

The immunosuppressive activity of cyclosporine is primarily due to parent drug. Following oral administration, absorption of cyclosporine is incomplete.

There is a minimal experience with cyclosporine overdosage. Forced emesis and gastric lavage can be of value up to 2 hours after administration of cyclosporine capsules, (modified). Transient hepatotoxicity and nephrotoxicity may occur which should resolve following drug withdrawal. Oral doses of cyclosporine up to 10 g (about 150 mg/kg) have been tolerated with relatively minor clinical consequences, such as vomiting, drowsiness, headache, tachycardia and, in a few patients, moderately severe, reversible impairment of renal function. However, serious symptoms of intoxication have been reported following accidental parenteral overdosage with cyclosporine in premature neonates. General supportive measures and symptomatic treatment should be followed in all cases of overdosage. Cyclosporine is not dialyzable to any great extent, nor is it cleared well by charcoal hemoperfusion. The oral dosage at which half of experimental animals are estimated to die is 31 times, 39 times, and > 54 times the human maintenance dose for transplant patients (6mg/kg; corrections based on body surface area) in mice, rats, and rabbits.

• Nov 14, 1983NDANDA050573Novartis
• Mar 2, 1990NDANDA050625Novartis
• Jul 14, 1995NDANDA050716Novartis
• Jul 14, 1995NDANDA050715Novartis
• Dec 23, 2002NDANDA050790Abbvie
• Aug 14, 2018NDANDA210913Sun Pharm
• Jun 23, 2021NDANDA214965Harrow Eye
• May 30, 2023NDANDA217469Harrow Eye

1. 1Drug Ineffective13,50312%
2. 2Eye Irritation9,3708.3%
3. 3Off Label Use9,1688.2%
4. 4Eye Pain4,4113.9%
5. 5Product Use In Unapproved Indication4,2673.8%
6. 6Pyrexia4,1093.7%
7. 7Headache3,7523.3%
8. 8Nausea3,6833.3%
9. 9Diarrhoea3,6343.2%
10. 10Fatigue3,4223.0%
11. 11Pneumonia3,3283.0%
12. 12Condition Aggravated3,2382.9%
13. 13Pain3,1852.8%
14. 14Vision Blurred3,1522.8%
15. 15Ocular Hyperaemia2,7532.5%

Recent PubMed references pinned to Cyclosporine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Eltrombopag Combined With Cyclosporine A in the Treatment of Pediatric Patients With SAA: Establishing the Range for Eltrombopag Concentrations.
  Clinical and translational science · 2026 · Li F, Li N, Tang X, et al.
  PMID 42257533DOI 10.1111/cts.70631
• A Sustained-Release Thermoplastic Polyurethane/Poly L-Lactide-Co-DL-Lactide (TPU/PLDLA) Cyclosporine-A Implant for the Treatment of Canine Keratoconjunctivitis Sicca: A Retrospective Case Series.
  Veterinary ophthalmology · 2026 · Padjasek M, Cisło-Sankowska A, Pajuelo D, et al.
  PMID 42192580DOI 10.1111/vop.70191
• A case of lupus nephritis achieving early remission using a treatment protocol similar to the AURORA trial with voclosporin and successfully discontinuing corticosteroids early.
  CEN case reports · 2026 · Mima A, Kumagai M, Fukumoto S, et al.
  PMID 42171925DOI 10.1007/s13730-026-01133-2
• Matching-adjusted indirect comparison of acoltremon ophthalmic solution 0.003% and cyclosporine 0.05% ophthalmic emulsion for increased tear production in patients with dry eye disease.
  Journal of comparative effectiveness research · 2026 · Pflugfelder S, Okoro T, Ainslie-Garcia M, et al.
  PMID 42132429DOI 10.57264/cer-2026-0032
• Combined cyclosporine A and urolithin A therapy ameliorates murine lupus nephritis.
  Journal of immunology (Baltimore, Md. : 1950) · 2026 · Ganugula R, Babalola KT, Arora M, et al.
  PMID 42130005DOI 10.1093/jimmun/vkag087
• Serum proteomic changes in atopic dermatitis patients treated with cyclosporine.
  PloS one · 2026 · Olydam JI, Litman T, Nijsten T, et al.
  PMID 42008513DOI 10.1371/journal.pone.0346686
• High-Dose Voclosporin Protects Against Acute Kidney Injury via Regnase-2-Mediated NGAL MRNA Decay.
  International journal of molecular sciences · 2026 · Hasegawa K, Sakamaki Y, Tamaki M, et al.
  PMID 41977336DOI 10.3390/ijms27073150
• Comparative neuropsychiatric safety signals of tacrolimus versus cyclosporine in solid organ transplantation: ten-year FAERS pharmacovigilance study.
  Frontiers in immunology · 2026 · Almalki BA, Alamer KA
  PMID 41972119DOI 10.3389/fimmu.2026.1795626

The 10 most recently updated of 1,299 ClinicalTrials.gov registrations naming Cyclosporine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Rituximab Plus Cyclosporine in Idiopathic Membranous Nephropathy
  Recruiting · Phase 2 · Interventional · 30 enrolled · National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
  NCT00977977updated 2026-06-12
• Comparison of Efficacy and Safety of Treatment With a Calcineurin Inhibitor (CNI)Versus a CNI-free Treatment in Renal Transplantation (CIME)
  Completed · Phase 3 · Interventional · 88 enrolled · Centre Hospitalier Universitaire, Amiens
  NCT01595984updated 2026-06-12
• Efficacy of Vevye Ophthalmic Solution for the Treatment of Meibomian Gland Dysfunction
  Recruiting · Phase 4 · Interventional · 48 enrolled · University of Alabama at Birmingham
  NCT07224529updated 2026-06-09
• Fungal Ulcer Treatment Augmented With Natamycin and Cyclosporine A
  Recruiting · Phase 3 · Interventional · 150 enrolled · University of California, San Francisco
  NCT06658002updated 2026-06-05
• Multicenter Randomized Two-arms Study Evaluating the BK Viral Clearance in Kidney Transplant Recipients With BK Viremia.
  Completed · Phase 4 · Interventional · 130 enrolled · University Hospital, Strasbourg, France
  NCT03216967updated 2026-06-05
• CsA+EPAG/HPAG+Romiplostim N01 in the Treatment of Newly-diagnosed SAA/TD-NSAA
  Withdrawn · Phase 2 · Interventional · 0 enrolled · Peking Union Medical College Hospital
  NCT07523009updated 2026-06-04
• Enarodustat+CsA vs CsA in the Treatment of Newly-diagnosed TD-NSAA
  Withdrawn · Phase 3 · Interventional · 0 enrolled · Peking Union Medical College Hospital
  NCT07522996updated 2026-06-04
• Luspatercept Plus CsA vs CsA for the Treatment of Newly Diagnosed Non-Transfusion-Dependent NSAA
  Withdrawn · Phase 4 · Interventional · 0 enrolled · Peking Union Medical College Hospital
  NCT06424639updated 2026-06-04
• Renal Function Evaluation After Reduction of Cyclosporine A Dose in Renal Transplant Patients
  Completed · Phase 3 · Interventional · 208 enrolled · University Hospital, Rouen
  NCT00213590updated 2026-06-04
• Open Label Trial of Oral Letermovir for CMV Prophylaxis in Thoracic Transplant Recipients
  Recruiting · Phase 2 · Interventional · 80 enrolled · University of Pennsylvania
  NCT06066957updated 2026-06-03

CPIC-curated drug–gene pairs for Cyclosporine. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• CYP3A5CPIC C (provisional)ClinPGx 3

Frequently asked questions

How does Cyclosporine work?

Mechanism-of-action classes: Calcineurin Inhibitors; Cytochrome P450 3A4 Inhibitors; Immunologic Adjuvants; P-Glycoprotein Inhibitors; Unknown Cellular or Molecular Interaction.

What is Cyclosporine used for?

According to FDA labeling, Cyclosporine carries indications including: Kidney, Liver, and Heart Transplantation Cyclosporine capsules (modified) is indicated for the prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants. Cyclosporine capsules (modified) has been used in combination with azathioprine and corticosteroids.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Cyclosporine?

Cyclosporine is classified as Calcineurin inhibitors, Other ophthalmologicals, Calcineurin Inhibitor Immunosuppressant, Calcineurin Inhibitors, Cytochrome P450 3A4 Inhibitors, Immunologic Adjuvants, P-Glycoprotein Inhibitors, Unknown Cellular or Molecular Interaction, Decreased Cytokine Activity, Decreased Cytokine Production, Decreased T Lymphocyte Production.

What are the brand names for Cyclosporine?

Cyclosporine is marketed under brand names including Atopica, Cequa, Cyclavance, Gengraf, Modulis, Neoral, Optimmune, Restasis.

What are the contraindications for Cyclosporine?

Cyclosporine labeling lists contraindications including: General Cyclosporine capsules (modified) is contraindicated in patients with a hypersensitivity to cyclosporine or to any of the ingredients of the formulation. Rheumatoid Arthritis Rheumatoid arthritis patients with abnormal renal function, uncontrolled hypertension, or malignancies should not receive cyclosporine capsules, (modified).. Always consult the full prescribing information and a clinician.