Experimental and Clinical Pharmacology: Immunosuppressants - mechanisms of action and monitoring

Abstract

Although corticosteroids and drugs such as azathioprine still have a role, there is increasing use of newer potent immunosuppressants. Many of these drugs act on T-lymphocytes. Tacrolimus is a calcineurin inhibitor which has a similar mechanism of action to cyclosporin, reducing T-cell differentiation. Sirolimus and everolimus bind to the same protein as tacrolimus, but have a different mechanism of action. As some of these drugs have a narrow therapeutic range, drug concentrations must be monitored. Mycophenolate is an inhibitor of purine synthesis. Another approach is to block the receptors on T-cells with immunosuppressant antibodies such as basiliximab, daclizumab and muromonab-CD3.