Drug intelligence / Profile preview

amiselimod + corticosteroid + immunosuppressant

Development stage
Unknown
Lead developer
Mitsubishi Tanabe Pharma
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

The combination **amiselimod + corticosteroid + immunosuppressant** refers to the concurrent administration of **amiselimod** (an oral selective sphingosine 1-phosphate receptor-1 modulator), a **corticosteroid** (such as prednisolone), and an **immunosuppressant** (such as azathioprine or mycophenolate mofetil)[1][4][5]. Amiselimod reduces peripheral blood lymphocyte count and modulates immune responses by targeting the sphingosine 1-phosphate receptor-1, thereby impeding lymphocyte egress from lymphoid tissues[1]. Corticosteroids act as anti-inflammatory and immunosuppressive agents primarily through glucocorticoid receptor agonism, broadly dampening immune signaling and cytokine production[2][3][5][6]. Immunosuppressants such as azathioprine or mycophenolate inhibit purine synthesis, thereby limiting lymphocyte proliferation[4][5]. This combination therapy—often used in the treatment of autoimmune diseases such as **systemic lupus erythematosus (SLE)**—was specifically evaluated in a multicenter, open-label phase 1b clinical trial for safety, pharmacokinetics, pharmacodynamics, and exploratory efficacy in SLE. The combination is generally reserved for patients with insufficient disease control on monotherapy[1][4][5]. The principal mechanism is synergistic immunomodulation affecting lymphocyte function, proliferation, and trafficking.

02

Targets

S1PR4S1PR2 (S1P receptor 2)S1PR3 (Sphingosine 1-phosphate receptor 3)S1PR5 (Sphingosine-1-phosphate receptor 5)

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