CasNo: 104987-11-3
Molecular Formula: C44H69NO12
Appearance: White or off-white crystalline powder
Tacrolimus, a powerful immunosuppressant, is often used to prevent rejection after organ transplantation, especially in liver, kidney and heart transplantation. It reduces the attack on transplanted organs by suppressing the activity of the immune system. At the same time, tacrolimus is also used to treat certain autoimmune diseases, such as atopic dermatitis. Tacrolimus is generally obtained by chemical synthesis, and blood drug concentrations need to be strictly monitored during use to ensure efficacy and safety.
InChI:InChI=1/C44H69NO12/c1-10-13-31-19-25(2)18-26(3)20-37(54-8)40-38(55-9)22-28(5)44(52,57-40)41(49)42(50)45-17-12-11-14-32(45)43(51)56-39(29(6)34(47)24-35(31)48)27(4)21-30-15-16-33(46)36(23-30)53-7/h10,19,21,26,28-34,36-40,46-47,52H,1,11-18,20,22-24H2,2-9H3/b25-19-,27-21+/t26-,28+,29+,30-,31+,32-,33+,34-,36+,37-,38-,39+,40+,44+/m0/s1
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There is limited systemic absorption of tacrolimus over the course of therapy. The most extensive experience with tacrolimus has been in treating atopic dermatitis. In numerous trials, tacrolimus ointment 0.03–0.3% has shown to be effective in reducing the symptoms and severity of atopic dermatitis in adults and the paediatric population.
Notably, the lower incidence of rejection episodes after renal transplantation in tacrolimus recipients was reflected in improved cost effectiveness. In bone marrow transplant (BMT) recipients, the incidence of tacrolimus grade II–IV graft-versus-host disease was significantly lower with tacrolimus than cyclosporin treatment.
Interaction of other drugs with P-glycoprotein may change tacrolimus tissue distribution and modify its toxicity and immunosuppressive activity. There is evidence that ethnic and gender differences exist for tacrolimus drug interactions.
C56H97NO12Si2
14-<(tert-butyldimethylsilyl)oxy>-24,32-bis<(triisopropylsilyl)oxy>-FK506
C66H101NO11Si2
C66H101NO12Si2
C45H71NO12
C45H71NO12
(E)-(1R,9S,12S,13R,14S,17R,21S,23S,24R,25S,27R)-17-Allyl-12-[(E)-2-((1R,3R,4R)-3,4-dimethoxy-cyclohexyl)-1-methyl-vinyl]-1-hydroxy-14,23,25-trimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-aza-tricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetraone
(S)-2-Benzyl-hexahydro-pyrido[1,2-a]pyrazine-1,4-dione