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Clinical data | |
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Trade names | Prograf, Advagraf, Protopic, others |
Other names | FK-506, fujimycin |
AHFS/Drugs.com | Monograph |
MedlinePlus | a601117 |
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Routes of administration | Topical, by mouth, intravenous |
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Pharmacokinetic data | |
Bioavailability | 24% (5–67%), less after eating food rich in fat |
Protein binding | ≥98.8% |
Metabolism | Liver CYP3A4, CYP3A5 |
Elimination half-life | 11.3 h for transplant patients (range 3.5–40.6 h) |
Excretion | Mostly fecal |
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ECHA InfoCard | 100.155.367 |
Chemical and physical data | |
Formula | C44H69NO12 |
Molar mass | 804.031 g·mol−1 |
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Tacrolimus, sold under the brand name Prograf among others, is an immunosuppressive drug. After allogenic organ transplant, the risk of organ rejection is moderate. To lower the risk of organ rejection, tacrolimus is given. The drug can also be sold as a topical medication in the treatment of T-cell-mediated diseases such as eczema and psoriasis. For example, it is prescribed for severe refractory uveitis after a bone marrow transplant, exacerbations of minimal change disease, Kimura's disease, and vitiligo. It can be used to treat dry eye syndrome in cats and dogs.[7][8]
Tacrolimus inhibits calcineurin, which is involved in the production of interleukin-2, a molecule that promotes the development and proliferation of T cells, as part of the body's learned (or adaptive) immune response.
Chemically, it is a macrolide lactone[9] that was first discovered in 1987, from the fermentation broth of a Japanese soil sample that contained the bacterium Streptomyces tsukubensis. It is on the World Health Organization's List of Essential Medicines.[10] In 2021, it was the 296th most commonly prescribed medication in the United States, with more than 500,000 prescriptions.[11][12]