Drug intelligence / Profile preview

belatacept + sirolimus

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

Overview

Belatacept + sirolimus is a combination immunosuppressive regimen used mainly in the context of organ transplantation, particularly kidney (renal) and islet transplantation. **Belatacept** is a fusion protein that selectively blocks T-cell costimulation by binding CD80 and CD86 on antigen-presenting cells, preventing their interaction with the CD28 receptor on T cells, leading to reduced T cell activation. **Sirolimus** is an inhibitor of the mammalian target of rapamycin (**mTOR**), acting through binding FKBP12 to inhibit mTOR activity in T lymphocytes, thereby suppressing cytokine-driven proliferation and cell cycle progression. Together, these two agents provide a calcineurin inhibitor- and steroid-free immunosuppressive protocol with the aim to reduce toxicity and side effects associated with traditional regimens, while effectively prolonging allograft survival. The combination is under investigation and has shown efficacy and good tolerability in both nonhuman primate studies and early-phase clinical trials in kidney and islet transplantation settings[1][3][5][6][7].

02

Targets

CD80 (T-lymphocyte activation antigen CD80)mTOR (Mammalian target of rapamycin kinase)CD86 (T-lymphocyte activation antigen CD86)FKBP1A

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