Drug intelligence / Profile preview

cyclosporin A + methotrexate + steroids

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous (for Some Formulations), Intramuscular (methotrexate Sometimes)
01

Overview

This is a combination drug regimen consisting of cyclosporin A, methotrexate, and corticosteroids (steroids). It is used primarily as an immunosuppressive therapy to treat autoimmune diseases such as severe psoriasis, psoriatic arthritis, rheumatoid arthritis, and for prophylaxis of acute graft-versus-host disease (GVHD) after bone marrow transplantation. - **Cyclosporin A** is a calcineurin inhibitor that suppresses T-cell activation by inhibiting the phosphatase activity of calcineurin. This reduces interleukin-2 production and T-cell proliferation. - **Methotrexate** is a folic acid antagonist that inhibits dihydrofolate reductase leading to inhibition of DNA synthesis; it acts as a disease-modifying antirheumatic drug (DMARD) with anti-inflammatory effects. - **Steroids** (such as prednisone or prednisolone) are glucocorticoids that modulate gene expression to reduce inflammation and immune responses. The combination allows for enhanced immunosuppression with potentially lower doses of each agent, improving efficacy in controlling inflammation while attempting to limit toxicity. It has been shown effective in preventing acute GVHD post-transplantation more than cyclosporine plus steroids alone. In rheumatoid arthritis and psoriasis patients not adequately controlled by monotherapy, this triple combination can improve clinical outcomes[1][2][3][5][7].

02

Targets

GR (Glucocorticoid receptor)DHFR (Dihydrofolate reductase)PPP3CA (Protein phosphatase 3 catalytic subunit alpha)

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