Drug intelligence / Profile preview

mTOR inhibitor + tacrolimus

Development stage
Unknown
Lead developer
Oriol Manuel
Modality
Small Molecules
Administration
Oral
01

Overview

mTOR inhibitor + tacrolimus is a combination immunosuppressive regimen consisting of a mammalian target of rapamycin (mTOR) inhibitor and the calcineurin inhibitor tacrolimus. mTOR inhibitors, such as sirolimus and everolimus, inhibit the mTORC1 complex, which is a key regulator of cell growth and proliferation, particularly in T-cells. Tacrolimus binds to FKBP12 to form a complex that inhibits calcineurin, thereby blocking the dephosphorylation of NFAT and the subsequent production of interleukin-2 (IL-2). This dual-mechanism approach is used in solid-organ transplantation to prevent graft rejection. In clinical research, such as the HORUS-COPE trial led by Oriol Manuel, this combination is being explored for its potential to modulate immune responses and control cytomegalovirus (CMV) replication in transplant recipients, as mTOR inhibitors have been associated with lower rates of CMV infection compared to other immunosuppressive agents like mycophenolic acid (MPA).

Other names
mammalian target of rapamycin inhibitor + tacrolimusmTORi + tacrolimusmTOR inhibitor + tacrolimus
02

Targets

FKBP1APPP3CA/PPP3CB (Protein phosphatase 3 catalytic subunit alpha/beta (Calcineurin))

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