Tacrolimus

A white or almost white powder

Specific rotation:-82°~ -90°

Water≤3.0%

Residue on ignition≤0.2%

Heavy metals≤20 ppm

Related substances

Impurity A (Ascomycin) ≤0.5%

Impurity B(Dihydro tacrolimus)≤0.5%

Any individual unknown impurity ≤0.1 %

Total impurities ≤1.0%

Tautomers I+II≤1.0%

Assay:98.0% ~ 102.0%

An immunosuppressant that blocks T cell proliferation in vitro by inhibiting the generation of several lymphokines, especially IL-2. Shown to inhibit the activity of FK-506 binding protein, thereby reversing its effects on sarcoplasmic reticulum Ca+2 release.

For use after allogenic organ transplant to reduce the activity of the patient's immune system and so the risk of organ rejection. It was first approved by the FDA in 1994 for use in liver transplantation, this has been extended to include kidney, heart.