Approved & therapeutic
Cyclosporine
Sandimmune, Neoral, Restasis
Cyclosporine is a cyclic undecapeptide of fungal origin and the drug that made routine solid organ transplantation possible. It is approved for transplant rejection prophylaxis, rheumatoid arthritis, psoriasis and — as an ophthalmic emulsion — for dry eye disease.
Also known as: Sandimmune, Neoral, Gengraf, Restasis, ciclosporin, cyclosporin A
- Status
- Cyclosporine is approved by the U.S. FDA and has official prescribing information.
- Evidence
- Approved labeling. Official prescribing information exists, based on clinical trials in people.
- Half-life
- Approximately 8 to 27 hours, with wide interindividual variability.
- How it's taken
- Oral capsule or solution, intravenous infusion, or ophthalmic emulsion
- Mechanism
- Immune modulation
- Pathways
- Calcineurin
How Cyclosporine works
Cyclosporine binds cyclophilin, and the cyclosporine-cyclophilin complex inhibits calcineurin. Calcineurin normally dephosphorylates NFAT, allowing it to enter the nucleus and drive interleukin-2 transcription. Blocking this step selectively suppresses T-cell activation without the broad myelosuppression of cytotoxic immunosuppressants.
What research has looked at
- Its introduction in the 1980s transformed transplant survival and remains one of the clearest step changes in modern therapeutics.
- Selective T-cell suppression rather than general bone marrow suppression.
- Effective in severe psoriasis and rheumatoid arthritis refractory to other therapy.
- The topical ophthalmic emulsion treats dry eye disease with negligible systemic exposure.
Evidence level: Approved labeling. Official prescribing information exists, based on clinical trials in people. These are areas studied or reported, not promised effects.
Reported side effects and risks
- Nephrotoxicity is the defining limitation and is both acute and chronic; chronic calcineurin-inhibitor nephropathy is a major cause of long-term graft and native kidney damage.
- Hypertension, hyperlipidaemia, hyperkalaemia and hypomagnesaemia.
- Extensive CYP3A4 interactions — grapefruit juice, azoles, macrolides and many others alter levels substantially, and therapeutic drug monitoring is mandatory.
- Gingival hyperplasia and hypertrichosis, which are cosmetically significant and affect adherence.
- Increased risk of infection and of malignancy, particularly skin cancer and lymphoproliferative disease, as with any sustained immunosuppression.
- Different oral formulations are not bioequivalent and cannot be substituted without re-monitoring.
Sources
- FDA approved-drug listing for cyclosporine · U.S. Food & Drug Administration
- DailyMed prescribing information for cyclosporine · NIH · DailyMed
- PubMed research on cyclosporine calcineurin nephrotoxicity transplant · NIH · National Library of Medicine
- DrugBank record for cyclosporine · DrugBank
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Related compounds
Cyclosporine FAQ
What is Cyclosporine?
Cyclosporine is a cyclic undecapeptide of fungal origin and the drug that made routine solid organ transplantation possible. It is approved for transplant rejection prophylaxis, rheumatoid arthritis, psoriasis and — as an ophthalmic emulsion — for dry eye disease.
How does Cyclosporine work?
Cyclosporine binds cyclophilin, and the cyclosporine-cyclophilin complex inhibits calcineurin. Calcineurin normally dephosphorylates NFAT, allowing it to enter the nucleus and drive interleukin-2 transcription. Blocking this step selectively suppresses T-cell activation without the broad myelosuppression of cytotoxic immunosuppressants.
Is Cyclosporine FDA approved?
Yes. Cyclosporine is approved by the U.S. FDA and has official prescribing information. Evidence level: approved labeling. Official prescribing information exists, based on clinical trials in people.
What is the half-life of Cyclosporine?
Reported half-life: Approximately 8 to 27 hours, with wide interindividual variability.
How is Cyclosporine taken?
Oral capsule or solution, intravenous infusion, or ophthalmic emulsion.
What side effects have been reported with Cyclosporine?
Reported in the sources: Nephrotoxicity is the defining limitation and is both acute and chronic; chronic calcineurin-inhibitor nephropathy is a major cause of long-term graft and native kidney damage; Hypertension, hyperlipidaemia, hyperkalaemia and hypomagnesaemia; Extensive CYP3A4 interactions — grapefruit juice, azoles, macrolides and many others alter levels substantially, and therapeutic drug monitoring is mandatory; Gingival hyperplasia and hypertrichosis, which are cosmetically significant and affect adherence; Increased risk of infection and of malignancy, particularly skin cancer and lymphoproliferative disease, as with any sustained immunosuppression; Different oral formulations are not bioequivalent and cannot be substituted without re-monitoring.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.