Drug intelligence / Profile preview

hydroxychloroquine + mycophenolic acid + prednisone + tacrolimus

Development stage
Unknown
Lead developer
Roche
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral, Intravenous, Topical
01

Overview

This is a combination regimen of four immunosuppressive and anti-inflammatory drugs—hydroxychloroquine, mycophenolic acid, prednisone, and tacrolimus. Each component has a distinct mechanism of action: - **Hydroxychloroquine** is an antimalarial and disease-modifying anti-rheumatic drug (DMARD) that inhibits toll-like receptor signaling in immune cells, reducing inflammation. It is used for malaria prophylaxis/treatment and autoimmune diseases such as lupus erythematosus and rheumatoid arthritis[1][8]. - **Mycophenolic acid** (active form of mycophenolate mofetil) is an antimetabolite immunosuppressant that inhibits inosine monophosphate dehydrogenase (IMPDH), suppressing lymphocyte proliferation. It is primarily used to prevent organ transplant rejection[4][9]. - **Prednisone** is a synthetic glucocorticoid corticosteroid with potent anti-inflammatory and immunosuppressive effects via glucocorticoid receptor agonism. - **Tacrolimus** is a calcineurin inhibitor that blocks T-cell activation by inhibiting interleukin-2 transcription; it’s widely used to prevent organ transplant rejection[7][10]. This combination may be employed in complex cases requiring multi-modal immunosuppression, such as severe autoimmune diseases or post-transplant regimens where multiple pathways must be targeted to control immune activity.

02

Targets

IMPDH (Inosine-5'-monophosphate dehydrogenase 1)TLR9 (Toll-like receptor 9)GR (Glucocorticoid receptor)

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