Cyclosporine (Sandimmune, Restasis)_Dosage, benefits & legal status
Also known as ciclosporin, cyclosporin, cyclosporin A, ciclosporin A, CsA, Sandimmune, Sandimmun, Neoral, Gengraf, Restasis, Cequa, Vevye, Verkazia, Ikervis
A ring of 11 unusual amino acids from a soil fungus, approved for transplants in 1983 and as dry-eye drops since 2002. The drops barely reach the blood; the capsules and infusion carry boxed warnings.
Common vial size is what vendors typically sell, not a recommendation. Enter your own vial in the calculator.
What is Cyclosporine (Sandimmune, Restasis)?
Plain language first. The technical label stays, but it never stands alone.Overview
Most people meet cyclosporine as eye drops for dry eye: an estimated 3.2 million US prescriptions in 2024, nearly all for Restasis-type 0.05% drops or Cequa. In the Restasis trials, about 15% of people had a 10 mm increase on a tear-wetting test (Schirmer) after 6 months against about 5% on inactive drops. As capsules, a liquid or an infusion it is a transplant drug: in a 1983 trial it raised one-year kidney graft survival from 64.0% to 80.4%, but those forms carry boxed warnings for infections and cancer (Neoral's also for kidney damage and high blood pressure) and need blood-level checks.
Cyclosporine is a cyclic undecapeptide made by the soil fungus Tolypocladium inflatum, found at Sandoz; Borel and colleagues described its immunosuppressive effects in 1976, and with cyclophilin it blocks calcineurin, keeping NFAT out of the nucleus and IL-2 switched off in T cells. The systemic forms (Sandimmune from 1983, Neoral from 1995, later joined by 'modified' generics such as Gengraf (2000)) prevent transplant rejection and treat severe rheumatoid arthritis and psoriasis under boxed warnings, and Sandimmune and Neoral are not bioequivalent. The eye products (Restasis 0.05%, Cequa 0.09%, Verkazia and Vevye 0.1%) act locally, leaving blood levels below 0.1 ng/mL with Restasis and Vevye.
What it's used for
Prescription eye drops for dry eye and for vernal keratoconjunctivitis, and capsules, an oral liquid or an infusion to prevent transplant rejection and to treat severe rheumatoid arthritis or psoriasis.
How does Cyclosporine (Sandimmune, Restasis) work?
What it does in the body, and where.Cyclosporine stops T cells from switching on by blocking calcineurin, the enzyme that relays their activation signal.
- 01A partner proteinCyclosporine passes into T cells and binds cyclophilin, a protein inside the cell. The pair then grips calcineurin, an enzyme switched on by calcium when a T cell recognizes a target. Residue 1, MeBmt, is central to this binding.
- 02The signal stopsCalcineurin normally strips phosphate tags from NFAT so it can move into the nucleus. With calcineurin blocked, NFAT stays outside, and IL-2 and other genes that drive T-cell activation stay off.
- 03Body and eyeFewer activated T cells means less attack on a transplanted organ, inflamed joints or skin. As eye drops it acts locally on the inflammation that suppresses tear production; the Restasis label calls it a partial immunomodulator whose exact action is unknown.
A schematic of the compound's mechanism, not a diagnostic image.
What else is it used for?
Each group carries its own evidence level.Approved means regulators have cleared it for that purpose. Investigational means it is in trials. Early research means it is being studied and is not established.
Kidney transplant (1983)
FDA-approved- Human trial209 deceased-donor kidney recipients: predicted one-year graft survival 80.4% on cyclosporine and prednisone against 64.0% on azathioprine and prednisone (P=0.003); patient survival 96.6% against 86.4%.
- No dataSerum creatinine at day 90 was higher with cyclosporine (2.6 against 2.0 mg/dL), and lymphoma developed in one cyclosporine patient.
Dry eye (Restasis)
FDA-approved- Human trialFour randomized trials, about 1,200 people: about 15% reached a 10 mm Schirmer wetting response at 6 months against about 5% on vehicle.
- Human trialBlood levels stayed below 0.1 ng/mL in every sample for up to 12 months.
Newer dry-eye drops (Cequa, Vevye)
FDA-approved- Human trialCequa, 1,048 people: a tear gain of at least 10 mm at day 84 in 16.8% against 8.6% (152 against 152) and 16.6% against 9.2% (371 against 373) of eyes.
- Human trialVevye, 1,369 people: a Schirmer gain of at least 10 mm at day 29 in 8% against 0% (51 against 51, P=0.04) and 11% against 7% (409 against 395, P=0.05).
Heart attack (CIRCUS)
tested-and-failed- Human trial970 people with an anterior ST-elevation heart attack, given cyclosporine before angioplasty: death, worsening heart failure, readmission for heart failure or heart remodeling at 1 year in 59.0% against 58.1% on placebo (OR 1.04, 95% CI 0.78 to 1.39, P=0.77).
Kidney safety on long-term use
FDA-approved- No dataIn psoriasis, rising creatinine led to stopping in 5.4%, and one person died of progressive kidney failure after treatment continued despite worsening kidney function.
- RegulatoryThe label warns that creatinine rises may cause irreversible kidney damage without a dose cut or stopping.
It is often described simply as an 11-amino-acid cyclic peptide that blocks calcineurin. That is right, but only valine 5 and alanine 7 are ordinary amino acids; the rest are N-methylated, mirror-image or unusual residues made by a fungus, not by ribosomes. 'First approved by the FDA in 1983' is true of the injection and oral solution (November 14, 1983); the current capsules date from 1990, Neoral from 1995 and the first eye drop, Restasis, from December 23, 2002. The 1983 Canadian trial is often called the original transplant trial, but Calne had already used it in 7 kidney transplant patients in 1978 without a control group, and a European multicenter trial reported preliminary results in the Lancet in July 1982. Histories name the fungus Tolypocladium inflatum, while US labels still say Beauveria nivea. Discovery dates differ from source to source, and credit for finding its immune effect is disputed between Borel and Stähelin; the first full paper was Borel and colleagues in 1976. Half-life depends on the product: about 19 hours for Sandimmune and 8.4 hours for Neoral. Sandimmune and Neoral are not bioequivalent, and generic 'cyclosporine, modified' matches Neoral, not Sandimmune. Restasis is labeled to increase tear production when eye inflammation suppresses it, not to treat dry eye in general; Vevye is the one labeled for the signs and symptoms of dry eye disease. The ESSENCE trials of Vevye are unrelated to the ESSENCE psoriasis trial of voclosporin, where cyclosporine was the comparator.
The published record
Papers and trials about Cyclosporine (Sandimmune, Restasis)
424 papers tagged human · 264 not reviews or lab · 142 clinical trial publications
122 registered trials · 31 with posted results
Furthest stage reached: Approved in the US
Counted from Europe PMC indexing, not read by a person; a human tag can land on reviews, commentary or lab papers; clinical trial publications is the narrower count. 485 papers and 100 trials indexed in detail.
At a glance
Four things to know about Cyclosporine (Sandimmune, Restasis)
Evidence
FDA-approved
Category
Immune support
Common vial
Varies
Half-life
About 19 hours (Sandimmune) or 8.4 hours (Neoral), by mouth
How much, and do you cycle it?
The range, and whether you take breaks.One drop in each eye (eye drops, label), twice daily. Continuous, set by the prescription FDA label
Eye drops are used every day, and transplant patients take it long term to prevent rejection. For rheumatoid arthritis the label says to stop if there is no benefit by 16 weeks, and for psoriasis after 6 weeks at the top dose without a satisfactory response.
How long does it stay in the body?
The half-life, and where the figure comes from.About 19 hours (Sandimmune) or 8.4 hours (Neoral), by mouthFDA label
Ranges are 10 to 27 hours for Sandimmune and 5 to 18 hours for Neoral. Absorption is incomplete and variable: Sandimmune oral solution is about 30% bioavailable (measured in 2 patients), and Neoral gives 20 to 50% more total exposure. Broken down mainly by CYP3A in the liver and cleared in bile; 6% of a dose reaches the urine. After eye drops, blood levels stay below 0.1 ng/mL with Restasis and Vevye, and peaked at 0.67 ng/mL in 55 children on Verkazia.
Source: Sandimmune prescribing information (2023) and Neoral prescribing information (2026), clinical pharmacology
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What does it cost?
Typical dose and cost, in plain numbers.Cyclosporine (Sandimmune, Restasis) is not injected
It is taken by mouth, into a vein, or as eye drops. Eye drops come at a set strength, so there is no dose to measure: one drop in each eye twice daily, about 12 hours apart, for Restasis 0.05%, Cequa 0.09% and Vevye 0.1% (Restasis 15 minutes apart from lubricant drops), and one drop in each affected eye four times daily for Verkazia 0.1%. The capsules, oral solution and infusion are dosed by body weight and adjusted to blood levels. Sandimmune by mouth starts with a single 15 mg/kg dose 4 to 12 hours before the transplant, tapered by 5% a week to 5 to 10 mg/kg a day; the infusion is 5 to 6 mg/kg a day, a third of the oral dose, used only when pills or liquid cannot be taken. Neoral starts at the same dose as Sandimmune; in a 1994 survey of Sandimmune use at US transplant centers, cited in the Neoral label, starting doses averaged 9, 8 and 7 mg/kg a day for kidney, liver and heart, in two doses; for rheumatoid arthritis it starts at 2.5 mg/kg a day in two doses and for psoriasis at 2.5 mg/kg a day, each to a maximum of 4 mg/kg a day. Sandimmune and Neoral are not bioequivalent, and switching needs blood-level monitoring. With no single dose to draw, the calculator starts with an empty dose field.
How do you store it?
Before mixing, and after.Eye drops: store them as the label or trial instructions say.
Cyclosporine (Sandimmune, Restasis) is used as eye drops, not mixed from a powder. Keep the bottle or single-use vials as the label or trial instructions say, do not let the tip touch the eye or anything else, and throw away a single-use vial once it has been opened.
What are the side effects and cautions?
Known cautions and warnings for this compound.Solubility, computed: 18% charged residues, 82% hydrophobic. Organic co-solvent likely.
A first-pass rule from peptide manufacturers' guidance. It does not account for disulfide bridges, salt form or how the powder was dried, and it predicts what should be easy rather than what will happen in your vial.
Who should avoid it
- Allergy to cyclosporine or any ingredient; for the Sandimmune infusion, also to Cremophor EL (polyoxyethylated castor oil)
- Eye drops: Restasis lists only allergy to its ingredients, and Cequa, Vevye and Verkazia list none
- Neoral for rheumatoid arthritis or psoriasis: abnormal kidney function, uncontrolled high blood pressure or cancer
- Psoriasis: at the same time as PUVA or UVB light treatment, methotrexate or other immunosuppressants, coal tar or radiation
- Sandimmune: given with corticosteroids but not with other immunosuppressants (boxed warning)
Stop and get help
- Trouble breathing, swelling or a sudden drop in blood pressure during the infusion: anaphylaxis is linked to its Cremophor EL vehicle
- A rising creatinine on blood tests: the label calls for a dose cut or stopping, decided by the prescriber, because kidney damage can become irreversible
- Fever, chills or other signs of a serious infection while on capsules, liquid or infusion
Common effects
- Restasis: eye burning in 17%; redness, discharge and other eye effects in 1 to 5%
- Cequa: pain on instillation 22% and eye redness 6%; Vevye: instillation site reactions 8%; Verkazia: eye pain 12% and itching 8%
- Transplant patients on Sandimmune (no placebo group): kidney dysfunction 25 to 38% (32% against 6% on azathioprine in the randomized kidney trials), high blood pressure 13 to 53%, tremor 21 to 55% and extra hair growth 21 to 45%, by organ
- Cyclosporine in rheumatoid arthritis trials (Neoral label): stopped for high blood pressure in 5.3% and for rising creatinine in 7%; in psoriasis, 1.0% and 5.4%
Where this page says nothing is established, that means nobody has studied it, not that a compound is safe.
Is Cyclosporine (Sandimmune, Restasis) approved?
And where the numbers on this page come from.Yes. Cyclosporine (Sandimmune, Restasis) is FDA approved and available on prescription in the United States. It is also approved in the European Union.
- Approval statusFDA-approved
- RouteBy mouth, into a vein, or as eye drops
- Checked21 October 2026
- Approved outside the USEuropean Union: In the EU, the ciclosporin eye emulsions Ikervis (March 19, 2015, severe keratitis in adults with dry eye disease) and Verkazia (July 6, 2018, severe vernal keratoconjunctivitis from age 4) are centrally authorized and held by Santen Oy; the systemic Sandimmun and Neoral are authorized country by country. Ciclosporin is on the WHO Essential Medicines List. Also approved in the US, where Sandimmune Injection, Neoral and Restasis have generics.This does not change the United States position above.
- DoseFrom the drug label. The manufacturer tested this range and a regulator reviewed it.
- Vial sizeFrom what vendors typically list; not a recommendation.
- SourcesFDA GSRS substance record, cyclosporine (UNII 83HN0GTJ6D)Drugs@FDA, NDA 050573 (Sandimmune Injection)Drugs@FDA, NDA 050790 (Restasis)Sandimmune prescribing information (2023)Neoral prescribing information, DailyMed (2026)Restasis prescribing information, DailyMedCequa prescribing information, DailyMedVevye prescribing information, DailyMedVerkazia prescribing information, DailyMedCanadian Multicentre Transplant Study Group, New England Journal of Medicine 1983;309:809-815Borel JF et al., Agents and Actions 1976;6:468-475Cung TT et al., New England Journal of Medicine 2015;373:1021-1031 (CIRCUS)David Moore, The cyclosporine story (secondary source)ClinCalc DrugStats, cyclosporine (MEPS 2024)
What has happened recently
Systemic forms: the FDA first approved cyclosporine on November 14, 1983, as Sandimmune Injection (NDA 050573) and Sandimmune Oral Solution (NDA 050574), for preventing rejection of kidney, liver and heart transplants; Sandimmune capsules followed on March 2, 1990 (NDA 050625). Neoral, a better-absorbed 'modified' formulation, was approved on July 14, 1995 (capsules NDA 050715, oral solution NDA 050716), and its label adds severe rheumatoid arthritis and severe plaque psoriasis; the modified generic Gengraf followed on May 12, 2000 (ANDA 065003). Novartis holds the Sandimmune and Neoral applications, and only the systemic forms, including generics such as Gengraf, carry boxed warnings; the eye products do not. Eye products: Restasis 0.05% emulsion (Allergan, now AbbVie) on December 23, 2002 (NDA 050790), to increase tear production suppressed by eye inflammation, now with six AB-rated generics; Cequa 0.09% solution (Sun Pharma) on August 14, 2018 (NDA 210913), to increase tear production in dry eye; Verkazia 0.1% emulsion on June 23, 2021 (NDA 214965), for vernal keratoconjunctivitis; and Vevye 0.1% water-free solution on May 30, 2023 (NDA 217469), for the signs and symptoms of dry eye disease. Verkazia and Vevye are now held by Harrow Eye in the US.
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What else is like Cyclosporine (Sandimmune, Restasis)?
Others in Immune support, side by side.If you're weighing Cyclosporine (Sandimmune, Restasis), it's worth reading Omiganan (MBI-226), Thymalin, and Vilon in the same class.
A ring of 11 unusual amino acids from a soil fungus, approved for transplants in 1983 and as dry-eye drops since 2002. The drops barely reach the blood; the capsules and infusion carry boxed warnings.
- Dose
- One drop in each eye (eye drops, label)
- How often
- Twice daily
A short, tryptophan- and arginine-rich peptide gel that disrupts microbial membranes. Two catheter-site phase 3 trials missed their primary endpoints, and its two rosacea phase 3 trials split, one positive and one negative.
- Dose
- 1% gel at catheter sites, 1.6% gel on rosacea (phase 3 trials)
- How often
- Each dressing change (catheters) or once daily (rosacea)
A thymus peptide taken in courses to refresh immune function and aging.
- Dose
- 5 up to 10 mg per day (start low, increase slowly)
- How often
- 10-day courses
A tiny bioregulator taken in courses for immunity and aging, with thin evidence.
- Dose
- Varies (course-based)
- How often
- Courses
Guides for this compound
- How to Reconstitute a Peptide
Mix peptide powder with bacteriostatic water, step by step.
- How to Read an Insulin Syringe
Read the units, convert to millilitres, and draw the exact dose.
- mcg vs mg: The Peptide Dosing Mistake to Avoid
Your vial says mg and your protocol says mcg. Here is the conversion and how to check it.
Sources
- FDA GSRS substance record, cyclosporine (UNII 83HN0GTJ6D)(2026)CAS 59865-13-3; C62H111N11O12, MW 1202.61; INN ciclosporin; full residue order and SMILES; brand names.
- Drugs@FDA, NDA 050573 (Sandimmune Injection)(2026)First approval November 14, 1983, a new molecular entity with priority review; the oral solution (NDA 050574) was approved the same day.
- Drugs@FDA, NDA 050790 (Restasis)(2026)Approved December 23, 2002; six AB-rated generic 0.05% emulsions listed; Restasis MultiDose on the same application.
- Sandimmune prescribing information (2023)(2023)Boxed warning; transplant dosing; half-life about 19 hours; oral bioavailability about 30%; anaphylaxis linked to Cremophor EL; producing fungus named Beauveria nivea.
- Neoral prescribing information, DailyMed (2026)(2026)Transplant, rheumatoid arthritis and psoriasis dosing; not bioequivalent to Sandimmune; half-life about 8.4 hours; transplant adverse reaction rates.
- Restasis prescribing information, DailyMed(2024)One drop twice daily; burning 17%; a 10 mm Schirmer wetting response in about 15% against 5% at 6 months; blood levels below 0.1 ng/mL.
- Cequa prescribing information, DailyMed(2026)Two trials in 1,048 people: a tear gain of at least 10 mm in 16.8% against 8.6% and 16.6% against 9.2% of eyes at day 84; pain on instillation 22%.
- Vevye prescribing information, DailyMed(2026)Two trials in 1,369 people: a Schirmer gain of at least 10 mm at day 29 in 8% against 0% and 11% against 7%; blood levels below 0.1 ng/mL.
- Verkazia prescribing information, DailyMed(2026)Vernal keratoconjunctivitis, one drop four times daily; eye pain 12%, itching 8%; highest blood level 0.67 ng/mL in 55 children.
- Canadian Multicentre Transplant Study Group, New England Journal of Medicine 1983;309:809-815(1983)209 deceased-donor kidney recipients: one-year graft survival 80.4% against 64.0% on azathioprine (P=0.003).
- Borel JF et al., Agents and Actions 1976;6:468-475(1976)First full report of cyclosporin A as an antilymphocytic agent.
- Cung TT et al., New England Journal of Medicine 2015;373:1021-1031 (CIRCUS)(2015)970 people with a heart attack: cyclosporine before angioplasty gave no benefit (59.0% against 58.1%, OR 1.04).
- David Moore, The cyclosporine story (secondary source)(2001)Tolypocladium inflatum isolated at Sandoz in March 1970 from soil samples from Wisconsin and Norway; credit for the immune finding disputed between Borel and Stähelin.
- ClinCalc DrugStats, cyclosporine (MEPS 2024)(2024)3,231,769 US prescriptions and 1,193,513 patients; 89.5% were the 0.05% emulsion and 10.5% the 0.09% solution.
Beyond these, 585 records are indexed. Browse the records