Small molecule · Transplant / Immunosuppression

Tacrolimus

Prograf
Small moleculeCalcineurin inhibitor (immunosuppressant)

PubChem CID 445643 · 3D model

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Blocks a T-cell signaling protein called calcineurin, stopping immune cells from multiplying and attacking a transplanted organ — reaching the same target as cyclosporine, also on this site, by grabbing a different helper protein first.

How it works

Tacrolimus first latches onto a helper protein inside T cells called FKBP12. That pairing then jams a second protein, calcineurin, which T cells normally use to switch on the gene for IL-2 — the signal that tells them to multiply and attack. With calcineurin blocked, T cells can't ramp up, which is why the drug is so effective at stopping the immune system from rejecting a transplanted organ. Cyclosporine, also on this site, arrives at the same blocked switch by grabbing a different helper protein first — two different keys that jam the same lock.

What it’s used for

Given to transplant recipients, usually for life, to stop their immune system from attacking a newly transplanted kidney, liver, heart, or lung.

Mechanism
Calcineurin (immunosuppressant)
Drug class
Therapeutic area
Transplant / Immunosuppression

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