Drug intelligence / Profile preview

cyclosporine + mycophenolate sodium + corticosteroids

Development stage
Unknown
Lead developer
Novartis
Modality
Small Molecules
Administration
Oral, Intravenous (for Select Corticosteroids)
01

Overview

A combination of **cyclosporine** (a calcineurin inhibitor), **mycophenolate sodium** (an antimetabolite immunosuppressant), and **corticosteroids** is used as an immunosuppressive regimen primarily for the prophylaxis of organ rejection following allogeneic renal transplantation, and has also been investigated as multitarget therapy in certain autoimmune renal diseases such as idiopathic membranous nephropathy (IMN). - **Mechanism of action:** - Cyclosporine inhibits calcineurin, blocking T-cell activation and cytokine production. - Mycophenolate sodium inhibits inosine monophosphate dehydrogenase (IMPDH), suppressing de novo purine synthesis, thus inhibiting lymphocyte proliferation. - Corticosteroids have broad anti-inflammatory and immunosuppressive effects through inhibition of multiple steps in immune activation, including gene transcription, cytokine production, and leukocyte trafficking. - **Therapeutic rationale:** The combination provides complementary and synergistic suppression of both humoral and cellular immune responses, thereby reducing the risk of organ rejection and, in off-label use, serving for idiopathic membranous nephropathy. - **Indication:** Commonly approved for kidney transplant rejection prophylaxis; multitarget use studied in idiopathic membranous nephropathy. - **Safety:** The multitarget regimen allows lower dosages of each drug, potentially minimizing adverse effects while maintaining efficacy[1][3][4].

Other names
cyclosporine + mycophenolate sodium + corticosteroids
02

Targets

OATP1B1 (Organic anion transporting polypeptide 1B1)SLCO1B3 (Organic anion transporting polypeptide 1B3)GR (Glucocorticoid receptor)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)CN (Calcineurin)

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