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.
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.
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.
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.