Drug intelligence / Profile preview

belatacept + everolimus

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Intravenous (belatacept), Oral (everolimus)
01

Overview

Belatacept + everolimus is a combination of two immunosuppressive agents used investigationally as maintenance therapy for the prophylaxis of organ rejection in kidney transplant recipients. **Belatacept** is a fusion protein that acts as a selective T-cell costimulation blocker, binding CD80 and CD86 on antigen-presenting cells and preventing activation of T lymphocytes by inhibiting the CD28-mediated costimulatory signal required for full T-cell activation and proliferation. **Everolimus** is an mTOR inhibitor (mTORi) that inhibits T-cell proliferation by targeting the mTORC1 complex, thereby blocking cell cycle progression in response to interleukin-driven signals. This combination is studied as a calcineurin-inhibitor-free regimen for renal transplantation to minimize nephrotoxicity and improve long-term graft and patient outcomes, with several studies and clinical trials investigating its safety and efficacy compared to standard regimens.[2][3][5][6]

02

Targets

CD80 (T-lymphocyte activation antigen CD80)mTOR (Mammalian target of rapamycin kinase)CD86 (T-lymphocyte activation antigen CD86)CD28 (Cluster of Differentiation 28)

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