Evidence Grade A — Regulatory approved. 34829 published studies. 1000 registered clinical trials.
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Cyclosporine is an immunosuppressant drug originally discovered in a soil fungus that transformed organ transplantation when introduced in the 1980s. By selectively calming the immune cells most responsible for organ rejection, it dramatically improved transplant survival rates. Today it is available as capsules, injection, and eye drops, and is used across transplant medicine, autoimmune conditions like severe psoriasis and rheumatoid arthritis, and chronic dry eye disease.
Cyclosporine is also known by these brand and alternate names:
34,829 published studies: 24605 human, 6876 animal, 2742 in-vitro, 4614 reviews
Cyclosporine is marketed as Sandimmune (approved 1983), Neoral/Gengraf (microemulsion formulation, 1995), and ophthalmic formulations Restasis (2002), Cequa (2018), and Verkazia. It is used for organ transplant rejection prophylaxis (kidney, liver, heart), severe rheumatoid arthritis, severe psoriasis, and chronic dry eye disease.
Cyclosporine transformed organ transplantation — one-year kidney graft survival improved from approximately 50% to over 80% after its introduction. Major side effects include nephrotoxicity (kidney damage with long-term use), hypertension, and increased infection and cancer risk. Therapeutic drug monitoring is essential. While newer immunosuppressants like tacrolimus have largely replaced cyclosporine as the primary calcineurin inhibitor in transplantation, cyclosporine remains widely used in dermatology, rheumatology, and ophthalmology.
Cyclosporine enters T-cells (the immune cells that drive organ rejection) and binds to a protein called cyclophilin. This drug-protein complex then blocks calcineurin, an enzyme that T-cells need to activate the genes for immune attack signals like IL-2. Without IL-2, the T-cell activation cascade is halted at a critical early step. Importantly, cyclosporine selectively targets this activation pathway without destroying the T-cells themselves, preserving some baseline immune function — a significant advantage over older immunosuppressants that killed immune cells indiscriminately.
Cyclosporine has over 40 years of clinical data. Its introduction was a watershed moment in transplant medicine — one-year kidney graft survival improved from around 50% to over 80%. The drug has since been joined by tacrolimus, which has largely replaced it as the primary immunosuppressant in transplantation, but cyclosporine remains widely used in dermatology, rheumatology, and ophthalmology. Long-term use carries significant risks including kidney damage, high blood pressure, and increased susceptibility to infections and certain cancers — all consequences of sustained immune suppression. Blood level monitoring is essential because the drug interacts with many other medications. The ophthalmic formulations (Restasis, Cequa) revitalised the commercial market by addressing chronic dry eye disease, a far more common condition than transplant rejection.
PeptideTrace tracks 1000 registered clinical trials for Cyclosporine sourced from ClinicalTrials.gov.
Efficacy of Topical Cyclosporine 0.05% in the Prevention of Ocular Surface Inflammation Secondary to Pterygia
Study of Cyclosporine in the Treatment of Dry Eye Syndrome (ST-603-007)
Efficacy of Topical Cyclosporine Versus Tears for Improving Visual Outcomes Following Multifocal IOL Implantation
Study of Cyclosporine in the Treatment of Dry Eye Syndrome (ST-603-005)
Cyclosporine Inhalation Solution (CIS) in Lung Transplant Recipients
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Health Canada Market Authorisation
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EMA Marketing Authorisation
FDA ORIG 1
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Cyclosporine is a cyclic undecapeptide (11 AA) from Tolypocladium inflatum. MW 1,202.61 Da. Seven N-methylated amino acids, D-Ala at position 8, unique C9 MeBmt amino acid. Extensive N-methylation enables passive absorption. Formulations: Sandimmune, Neoral/Gengraf (microemulsion), Restasis/Cequa (ophthalmic), Verkazia. Oral half-life 8-27 hours.
Binds cyclophilin A (Kd ~30 nM), forming complex that inhibits calcineurin phosphatase. Calcineurin normally dephosphorylates NFAT for nuclear translocation and transcription of IL-2, IL-4, TNF-alpha, IFN-gamma. Selectively inhibits T-cell activation without affecting cytotoxic/phagocytic function. Also inhibits mitochondrial permeability transition pore via cyclophilin D binding.
Marketed as Sandimmune (1983), Neoral/Gengraf (1995), Restasis (2002), Cequa (2018), Verkazia. Revolutionized transplantation (1-year kidney graft survival ~50% to >80%). Indications: organ rejection prophylaxis (kidney, liver, heart), severe RA, severe psoriasis, dry eye disease (ophthalmic).
Vancomycin is marketed as Vancocin and Firvanq (approved 1958, with oral solution Firvanq approved 2018). It is the standard treatment for serious MRSA infections (bloodstream infections, endocarditis, pneumonia, bone infections) and is first-line for severe C. difficile colitis. Vancomycin requires therapeutic drug monitoring — blood levels must be checked regularly to ensure the dose is effective without causing kidney damage or hearing loss. The rise of vancomycin-resistant enterococci (VRE) and occasional vancomycin-intermediate S. aureus (VISA) strains represent ongoing challenges. Despite being nearly 70 years old, vancomycin remains irreplaceable for many serious infections, though newer alternatives like daptomycin and the lipoglycopeptides offer advantages in specific settings.
Zilucoplan is marketed as Zilbrysq (approved October 2023) for anti-acetylcholine receptor antibody-positive generalised myasthenia gravis in adults. Administered as a daily subcutaneous self-injection. In the RAISE trial, zilucoplan showed statistically significant improvements in both activities of daily living and quantitative muscle strength scores compared to placebo, with improvements evident from week one. Its key differentiator from existing complement inhibitors (eculizumab, ravulizumab) is the self-injectable format — those alternatives require hospital-based intravenous infusions. As with all complement inhibitors, patients require meningococcal vaccination before starting treatment due to increased susceptibility to meningococcal infection.
Daptomycin is marketed as Cubicin (approved September 2003). It is indicated for complicated skin and soft tissue infections and S. aureus bloodstream infections including right-sided endocarditis. Administered as a once-daily intravenous infusion. A key limitation is that daptomycin cannot be used for pneumonia — lung surfactant inactivates the drug. In the bacteraemia trial, daptomycin was non-inferior to vancomycin with significantly lower rates of kidney problems (11% versus 26%). Creatine kinase (CK) levels must be monitored during treatment, as daptomycin can cause muscle toxicity. Generics became available after patent expiry, significantly reducing cost.
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