Drug intelligence / Profile preview

belatacept + mycophenolate mofetil

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules, Fc-Fusion Proteins → Carrier/Scaffold Proteins → Recombinant Proteins and Enzymes
Administration
Intravenous, Oral
01

Overview

Belatacept + mycophenolate mofetil is a combination immunosuppressive regimen used primarily to prevent rejection in kidney transplant recipients. - **Belatacept** is a fusion protein that consists of the Fc fragment of human IgG1 linked to the extracellular domain of CTLA-4 (CD152). It acts by binding to the CD80 and CD86 on antigen-presenting cells, thereby blocking CD28-mediated T-cell costimulation, resulting in selective T-cell inhibition and reduced alloimmune response[2][1]. - **Mycophenolate mofetil** is an ester prodrug of mycophenolic acid, which inhibits inosine monophosphate dehydrogenase (IMPDH), a key enzyme in de novo guanine nucleotide synthesis, selectively inhibiting lymphocyte proliferation[4]. This combination is often used in regimens alongside corticosteroids (and sometimes induction agents such as basiliximab) to prevent and manage acute rejection post-transplantation. It is especially considered in patients intolerant to calcineurin inhibitors like cyclosporine or tacrolimus, due to its nephroprotective advantage[1][5]. The regimen has demonstrated effectiveness in maintaining stable allograft function with acceptable rates of acute rejection and infection when appropriately managed.

02

Targets

CD80 (T-lymphocyte activation antigen CD80)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)CD86 (T-lymphocyte activation antigen CD86)

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