Drug intelligence / Profile preview

mycophenolate + calcineurin inhibitor

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a **combination therapy** that consists of **mycophenolate** (usually as mycophenolate mofetil) and a **calcineurin inhibitor** (CNI; commonly cyclosporine, tacrolimus, pimecrolimus, or voclosporin). Both agents are used together as part of immunosuppressive regimens, primarily to prevent rejection in organ transplantation and to reduce nephrotoxicity associated with high-dose CNI. Mycophenolate (a prodrug of mycophenolic acid) inhibits inosine-monophosphate dehydrogenase, leading to selective depletion of guanosine nucleotides in T and B lymphocytes, inhibiting their proliferation and dampening immune response. Calcineurin inhibitors selectively inhibit calcineurin, impeding the activation of NFAT and reducing transcription of cytokines (mainly IL-2) essential for T-cell activation and proliferation. The combination provides immunosuppressive synergy, lowers acute rejection rates, can improve or stabilize renal function versus higher CNI doses, and is a standard approach in solid organ transplantation[1][2][3][4][5][6].

02

Targets

CN (Calcineurin)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)

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