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Tacrolimus and Everolimus

Chang Gung Memorial Hospital · FDA-approved active Small molecule

Tacrolimus and everolimus are immunosuppressive agents that inhibit mTOR and calcineurin pathways to prevent T-cell activation and proliferation.

Tacrolimus and everolimus are immunosuppressive agents that inhibit mTOR and calcineurin pathways to prevent T-cell activation and proliferation. Used for Prevention of organ rejection in solid organ transplantation, Prevention and treatment of graft-versus-host disease (GVHD).

At a glance

Generic nameTacrolimus and Everolimus
Also known asPrograf, Advagraf, Zortress, Certican
SponsorChang Gung Memorial Hospital
Drug classImmunosuppressant (calcineurin inhibitor and mTOR inhibitor combination)
TargetCalcineurin (tacrolimus) and mTOR (everolimus)
ModalitySmall molecule
Therapeutic areaImmunology / Transplantation
PhaseFDA-approved

Mechanism of action

Tacrolimus binds to FK-binding protein and inhibits calcineurin, blocking T-cell receptor signaling and IL-2 production. Everolimus inhibits mTOR kinase, suppressing cell proliferation and immune response. Together, they provide synergistic immunosuppression to prevent organ rejection and graft-versus-host disease.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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