Prednisone (oral), Methylprednisolone (Solu-Medrol®; IV)
Glucocorticoid receptor agonists; inhibit synthesis of prostaglandins and leukotrienes, reduce expression of NF-κB, suppress inflammatory cytokine production, kill proliferating immune cells
Use: Organ transplantation, organ transplant rejection, autoimmune disease, chronic inflammatory disease
Azathioprine (Imuran®)
After conversion to 6-mercaptopurine in the liver inhibits purine synthesis, blocks Rac1 activation
Use: Organ transplantation, autoimmune disease
Methotrexate
Inhibits dihydrofolate reductase (high dose), inhibits AICAR transformylase thus increasing adenosine release (low dose)
Use: Rheumatoid arthritis (low dose), other autoimmune disease (low dose), cancer chemotherapy (high dose)
Cyclophosphamide (Cytoxan®)
Alkylates guanine in DNA forming intrastrand and interstrand DNA crosslinks
Use: Acute crisis in autoimmune disease; cancer chemotherapy*
Leflunomide
Inhibits dihydroorotate dehydrogenase thus inhibiting pyrimidine synthesis
Use: Rheumatoid arthritis*, other autoimmune disease
Infliximab (Remicade®)
Monoclonal antibody directed against TNFα
Use: Rheumatoid arthritis, IBD, other autoimmune disease
Rituximab
Monoclonal antibody directed against CD20 on B cells; kills B cells not long-lived plasma cells
Use: Autoimmune disease; cancer chemotherapy (B cell lymphomas)
Abatacept (Orencia®)
Extracellular domain of CTLA4 fused to antibody constant regions; prevents B7 on APC from binding to CD28 on T cell (so no costimulation)
Use: Rheumatoid arthritis
Cyclosporine
Binds to cyclophilin, complex inhibits calcineurin thus blocking T cell activation
Use: Organ transplantation
Tacrolimus (FK506)
Binds to FKBP12, complex inhibits calcineurin thus blocking T cell activation
Use: Organ transplantation
Sirolimus (rapamycin)
Binds to FKBP12, complex inhibits mTOR signalling thus blocking T cell activation
Use: Organ transplantation
Mycophenolate mofetil (Cellcept®)
Inhibits IMP dehydrogenase thus inhibiting purine synthesis
Use: Organ transplantation, autoimmune disease