Drug intelligence / Profile preview

fingolimod + cyclosporine + corticosteroids

Development stage
Phase 3
Lead developer
Novartis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination of three immunosuppressive drugs commonly used in transplantation and autoimmune conditions: - **Fingolimod** is a small molecule sphingosine 1-phosphate receptor modulator that prevents lymphocyte egress from lymph nodes by binding to S1PR receptors (mainly S1PR1). This reduces circulating lymphocytes and limits immune-mediated damage. It is primarily approved for relapsing-remitting multiple sclerosis but has been studied in transplant settings[3][6][8]. - **Cyclosporine** is a calcineurin inhibitor that binds cyclophilin to form a complex inhibiting calcineurin phosphatase activity. This blocks activation of the nuclear factor of activated T cells (NF-AT), reducing transcription of cytokines such as IL-2 and suppressing T cell activation[1]. - **Corticosteroids** are synthetic analogs of endogenous glucocorticoids with broad anti-inflammatory and immunosuppressive effects. They act via the glucocorticoid receptor to regulate gene expression involved in inflammation. This combination may be used for prevention of organ rejection after transplantation or for severe autoimmune diseases where multi-modal immunosuppression is required[8]. The specific mechanisms target different aspects of immune cell function to provide synergistic suppression.

Brand names
Tascenso
Other names
sphingosine 1-phosphate receptor modulator (for fingolimod)calcineurin inhibitor (for cyclosporine)glucocorticoids (for corticosteroids)
02

Targets

CN (Calcineurin)Cyp (Cyclophilin family)GR (Glucocorticoid receptor)S1PR3 (Sphingosine 1-phosphate receptor 3)S1PR4S1PR5 (Sphingosine-1-phosphate receptor 5)EDG1 (Sphingosine-1-phosphate receptors)

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