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rituximab + tacrolimus + mycophenolate mofetil + steroid

Development stage
Preclinical
Lead developer
Roche
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Oral, Intramuscular
01

Overview

This is a combination immunosuppressive regimen consisting of four agents: **Rituximab** is a monoclonal antibody targeting CD20 on B lymphocytes, leading to B cell depletion. It is used in various autoimmune diseases and certain cancers. **Tacrolimus** is a calcineurin inhibitor that suppresses T-cell activation by inhibiting interleukin 2 transcription, commonly used to prevent organ transplant rejection and treat autoimmune conditions. **Mycophenolate mofetil (MMF)** inhibits inosine monophosphate dehydrogenase, blocking de novo purine synthesis in lymphocytes and thus suppressing both T and B cell proliferation; it is widely used for transplant rejection prophylaxis and immune-mediated diseases[6]. **Steroids (glucocorticoids such as prednisone or methylprednisolone)** are anti-inflammatory agents that broadly suppress immune responses by multiple mechanisms including inhibition of cytokine production. This combination has been studied primarily for the treatment of difficult nephrotic syndrome subtypes—such as frequently relapsing or steroid-dependent nephrotic syndrome, focal segmental glomerulosclerosis (FSGS), membranous nephropathy, and other refractory glomerular diseases—where single-agent therapy has failed[1][2][3]. The rationale for combining these drugs lies in their complementary mechanisms targeting different arms of the immune system to maximize efficacy while minimizing toxicity from any single agent.

Other names
MMF (for mycophenolate mofetil)RTX (for rituximab)
02

Targets

GR (Glucocorticoid receptor)CD20 (B-lymphocyte antigen CD20)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)

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