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Conversion from Tacrolimus to Sirolimus

Helio Tedesco Silva Junior · FDA-approved active Small molecule

Conversion from tacrolimus to sirolimus involves switching from a calcineurin inhibitor to an mTOR inhibitor, both immunosuppressive agents used to prevent organ rejection.

Conversion from tacrolimus to sirolimus involves switching from a calcineurin inhibitor to an mTOR inhibitor, both immunosuppressive agents used to prevent organ rejection. Used for Prevention of organ rejection in transplant recipients (conversion from tacrolimus), Reduction of tacrolimus-related nephrotoxicity in transplant patients.

At a glance

Generic nameConversion from Tacrolimus to Sirolimus
SponsorHelio Tedesco Silva Junior
Drug classImmunosuppressive agent (conversion protocol)
TargetmTOR (mammalian target of rapamycin)
ModalitySmall molecule
Therapeutic areaImmunology / Transplantation
PhaseFDA-approved

Mechanism of action

Tacrolimus and sirolimus are both immunosuppressive drugs commonly used in transplant recipients, but they work through different mechanisms. Tacrolimus inhibits calcineurin and T-cell activation, while sirolimus inhibits mTOR and blocks T-cell and B-cell proliferation. The conversion strategy aims to reduce tacrolimus-related nephrotoxicity and other adverse effects while maintaining immunosuppression through an alternative mechanism.

Approved indications

Common side effects

Key clinical trials

Primary sources

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