Drug intelligence / Profile preview

tacrolimus + mycophenolate + prednisone

Development stage
Unknown
Lead developer
University of Sao Paulo General Hospital
Modality
Small Molecules
Administration
Oral
01

Overview

This regimen is a standard-of-care triple immunosuppressive therapy used in kidney transplantation to prevent organ rejection. It consists of the calcineurin inhibitor tacrolimus, the antimetabolite mycophenolate (mofetil or sodium), and the corticosteroid prednisone. Tacrolimus works by inhibiting calcineurin, thereby blocking T-cell activation and cytokine production. Mycophenolate inhibits inosine monophosphate dehydrogenase (IMPDH), the rate-limiting enzyme in the de novo synthesis of guanosine nucleotides, which selectively prevents the proliferation of T and B lymphocytes. Prednisone acts as a glucocorticoid receptor agonist, exerting broad anti-inflammatory and immunosuppressive effects. In the specific clinical trial context at the University of São Paulo General Hospital, this regimen serves as the control arm or baseline therapy for sensitized kidney transplant recipients to evaluate the additional benefit of adding an mTOR inhibitor like everolimus for preventing rejection and cytomegalovirus (CMV) infection.

Other names
standard maintenance immunosuppressiontriple immunosuppressive regimenstandard triple therapystandard maintenance immunosuppression-University of Sao Paulo General Hospital-kidney transplant rejection-cytomegalovirus infection
02

Targets

CN (Calcineurin)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)GR (Glucocorticoid receptor)FKBP1A

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