Tacrolimus, also known as FK506, is a calcineurin inhibitor immunosuppressant drug. It is commonly used after organ transplantation to reduce the activity of the patient's immune system and prevent organ rejection. By inhibiting T-cell activation, FK506 helps suppress the immune system from attacking and destroying the newly transplanted organ which would be recognized as foreign tissues.
Mechanism of Action
Tacrolimus binds to an intracellular protein called FKBP-12 inside T-cells. This FK506-FKBP-12 complex then binds to and inhibits the phosphatase activity of calcineurin. Calcineurin is a key enzyme required for T-cell activation and proliferation. By inhibiting calcineurin, FK506 prevents the transcription of several interleukins essential for proper T-cell function. This ultimately leads to immunosuppression and inhibits the immune response against the transplanted organ. FK506 is up to 100 times more potent than cyclosporine in inhibiting T-cell activation and calcineurin activity.
Approved Uses
FK506 is FDA approved for use in the prophylaxis of organ transplant rejection in patients receiving liver, kidney, or heart allografts. It works to prevent both acute and chronic rejection of solid organ transplants. Tacrolimus has become the primary maintenance immunosuppressive therapy for liver, kidney, and heart transplants. It allows for improved short- and long-term graft survival rates when used adjunctively with other anti-rejection medications in transplant recipients.
Tacrolimus is also sometimes used off-label for other autoimmune and inflammatory conditions like atopic dermatitis, severe uveitis, and refractory graft-versus-host disease after bone marrow transplantation. However, its primary use remains for solid organ transplant immunosuppression.
Get more insights on Tacrolimus
For Enhanced Understanding, Dive into the Report in the Language that Connects with You
· French
· German
· Italian
· Russian
· Japanese
· Chinese
· Korean
· Portuguese
About Author:
Ravina Pandya, Content Writer, has a strong foothold in the market research industry. She specializes in writing well-researched articles from different industries, including food and beverages, information and technology, healthcare, chemical and materials, etc.
