Drug intelligence / Profile preview

basiliximab + sirolimus + tacrolimus

Development stage
Unknown
Lead developer
Novartis
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination immunosuppressive regimen consisting of basiliximab, sirolimus, and tacrolimus. Basiliximab is a chimeric monoclonal antibody that targets the interleukin-2 receptor alpha subunit (CD25) on activated T-lymphocytes, thereby inhibiting IL-2-mediated activation and proliferation of lymphocytes involved in allograft rejection. Sirolimus (also known as rapamycin) is an mTOR inhibitor that suppresses T-cell activation and proliferation by inhibiting the response to interleukin-2. Tacrolimus is a calcineurin inhibitor that blocks T-cell activation by inhibiting calcineurin phosphatase activity, thus preventing transcription of IL-2 and other cytokines. This triple-drug regimen is used primarily for prophylaxis against organ transplant rejection, particularly in kidney and liver transplantation settings[1][6]. The combination aims to maximize immunosuppression while minimizing toxicity associated with higher doses of individual agents.

02

Targets

IL2RA (Interleukin-2 receptor alpha subunit)CN (Calcineurin)mTOR (Mammalian target of rapamycin kinase)

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