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Drug conversion to sirolimus

Hospital do Rim e Hipertensão · FDA-approved active Small molecule

Sirolimus is an mTOR inhibitor that suppresses T-cell proliferation and immune activation to prevent organ rejection.

Sirolimus is an mTOR inhibitor that suppresses T-cell proliferation and immune activation to prevent organ rejection. Used for Prevention of organ rejection in renal transplant recipients, Conversion therapy in transplant patients to reduce calcineurin inhibitor exposure.

At a glance

Generic nameDrug conversion to sirolimus
Also known asRapamune
SponsorHospital do Rim e Hipertensão
Drug classmTOR inhibitor
TargetmTOR (mammalian target of rapamycin)
ModalitySmall molecule
Therapeutic areaImmunology / Transplantation
PhaseFDA-approved

Mechanism of action

Sirolimus (rapamycin) binds to FKBP12 and inhibits the mammalian target of rapamycin (mTOR), a key signaling protein in cell proliferation and survival. This mechanism reduces T-cell and B-cell activation, making it effective as an immunosuppressant in transplant recipients. Drug conversion protocols involve switching patients from other immunosuppressants (such as calcineurin inhibitors) to sirolimus-based regimens to optimize long-term graft outcomes and reduce nephrotoxicity.

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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