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Drugs and Medicinal Substances

Ciclosporin

Antineoplastic and Immunomodulating Agents

Ciclosporin is a calcineurin inhibitor used as an immunosuppressant medication, given to prevent organ transplant rejection and to treat conditions including rheumatoid arthritis, psoriasis, Crohn's disease, nephrotic syndrome and eczema, as well as in eye drop form for dry eye disease. It works by forming a complex with the protein cyclophilin that blocks the enzyme calcineurin, reducing the production of inflammatory cytokines by T-lymphocytes and dampening the immune response. Employees of the pharmaceutical company Sandoz isolated new fungal strains from soil samples taken in Norway and Wisconsin, and in 1971 isolated ciclosporin from the fungus Tolypocladium inflatum; researcher Hartmann Stahelin discovered its immunosuppressive effect on January 31, 1972, and the drug's value was confirmed in kidney transplants by surgeon Roy Calne and in liver transplants by Thomas Starzl, ahead of its FDA approval in 1983. It appears on the World Health Organization's List of Essential Medicines.

Facts
Drug Class
Calcineurin inhibitor used as an immunosuppressant 1
Mechanism of Action
Binds cyclophilin in T lymphocytes, inhibiting calcineurin 1
Approved Use
Prevents transplant rejection and graft versus host disease 1
First Approved / Isolated Year
1983 1
Significant Risk
Increased risk of infection, liver problems and lymphoma 1
Classification
Approval Status
Approved 1
ATC ClassSourced to the subject's own account
L: Antineoplastic and Immunomodulating Agents 2
Route of Administration
Ophthalmic 3
WHO Essential MedicineSourced to the subject's own account
Complementary List 4
Sources
1. Ciclosporin (Wikipedia)
  • Lead section
    Ciclosporin, also spelled cyclosporine and cyclosporin, is a calcineurin inhibitor, used as an immunosuppressant medication.
  • Mechanism of action section
    Ciclosporin binds to the cytosolic protein cyclophilin (immunophilin) of lymphocytes, especially of T cells.
  • Medical uses section
    Ciclosporin is indicated to treat and prevent graft-versus-host disease in bone marrow transplantation and to prevent rejection of kidney, heart, and liver transplants.
  • History section
    In the United States, the Food and Drug Administration (FDA) approved ciclosporin for clinical use in 1983.
  • Side effects section
    Other severe side effects include an increased risk of infection, liver problems, and an increased risk of lymphoma.
  • Regulatory approval status
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2. Anatomical Therapeutic Chemical Classification System (Wikipedia)
WikipediaFirst-level anatomical group codes, Code L
Quote, First-level anatomical group codes, Code L
Antineoplastic and immunomodulating agents
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3. Wikipedia
Wikipedia contributors, Wikimedia Foundationhttps://en.wikipedia.org/wiki/Ciclosporin, lead section
Quote, https://en.wikipedia.org/wiki/Ciclosporin, lead section
organ transplants to prevent rejection. It is also used as eye drops for keratoconjunctivitis sicca. It is a cyclic peptide with chain length 11.
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4. WHO Model List of Essential Medicines (Wikipedia)
WikipediaWHO Model List of Essential Medicines, Immunomodulators for non-malignant disease section
Quote, WHO Model List of Essential Medicines, Immunomodulators for non-malignant disease section
Ciclosporin
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