Drug intelligence / Profile preview

mycophenolic acid + calcineurin inhibitor

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral
01

Overview

Mycophenolic acid + calcineurin inhibitor refers to a standard-of-care immunosuppressive regimen used to prevent organ rejection in kidney transplant recipients. This specific combination served as the control arm in the Novartis-sponsored TRANSFORM clinical trial, where it was compared against an everolimus-based regimen with reduced calcineurin inhibitor exposure. The regimen consists of mycophenolic acid (administered as either mycophenolate mofetil or mycophenolate sodium) and a calcineurin inhibitor (either tacrolimus or cyclosporine). Mycophenolic acid is a small molecule that inhibits inosine monophosphate dehydrogenase (IMPDH), the rate-limiting enzyme in de novo purine synthesis, which effectively suppresses T and B lymphocyte proliferation. Calcineurin inhibitors, such as tacrolimus and cyclosporine, block T-cell activation by inhibiting the phosphatase activity of calcineurin, thereby preventing the translocation of the nuclear factor of activated T-cells (NFAT) to the nucleus.

Other names
mycophenolate + calcineurin inhibitormycophenolate with standard calcineurin inhibitorMPA + CNI
02

Targets

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

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