Sandimmune, Neoral, Gengraf, Restasis, Cequa, Verkazia
Evidence Grade A — Regulatory approved. 34724 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.
34,724 published studies: 24567 human, 6864 animal, 2736 in-vitro, 4591 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.
Peripheral Stem Cell Transplant in Treating Patients With High-Risk Leukemia
A Study to Test the Effect of Cyclosporine on the Immune System of Patients With Early HIV Disease
Study of Cyclosporine in the Treatment of Dry Eye Syndrome (ST-603-005)
Efficacy of Topical Cyclosporine Versus Tears for Improving Visual Outcomes Following Multifocal IOL Implantation
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Corticotropin is marketed as H.P. Acthar Gel (currently ANI Pharmaceuticals). It carries approximately 19 FDA-labelled indications including infantile spasms (its strongest evidence base), nephrotic syndrome, multiple sclerosis relapses, and rheumatic disorders. Acthar Gel has been at the centre of major pricing and legal controversies. The price rose from approximately $40 per vial in 2001 to over $40,000, driven by successive acquisitions and orphan-like positioning despite broad labelling. The former manufacturer Mallinckrodt agreed to a $260 million settlement over antitrust concerns. Clinically, the strongest evidence supports its use in infantile spasms, where it is considered a first-line treatment. For most other indications, debate continues over whether it offers meaningful advantages over far less expensive oral corticosteroids.
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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.
