Tacrolimus TACR, previously known as FK, is a macrocyclic lactone antibiotic that was initially extracted in Japan from the soil microorganism, Streptomyces tsukubaensis, in Food and Drug Administration FDA for preventing rejection after liver, kidney, and heart transplants Mechanism of Action Tacrolimus, a potent inhibitor of T-lymphocyte proliferation, binds to the FK-binding protein FKBP, which is an intracellular cytoplasmic immunophilin. Administration of tacrolimus with other drugs or substances that are also metabolized by the same gene and protein can alter the blood concentrations of the drug. Monitoring of Tacrolimus Levels Tacrolimus has a low therapeutic index with a high inter-and intra-pharmacokinetic variability, and possesses several side effects and drug interactions.

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