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Immunosuppressive Agents for the Prevention of Transplantation Rejection

Pulmonary, Bone, Vitamins and Autocoid Therapeutic Agents

  1. William J. Pitts

Published Online: 15 SEP 2010

DOI: 10.1002/0471266949.bmc206

Burger's Medicinal Chemistry and Drug Discovery

Burger's Medicinal Chemistry and Drug Discovery

How to Cite

Pitts, W. J. 2010. Immunosuppressive Agents for the Prevention of Transplantation Rejection. Burger's Medicinal Chemistry and Drug Discovery. 983–1063.

Author Information

  1. Bristol-Myers Squibb Co., Princeton, NJ

Publication History

  1. Published Online: 15 SEP 2010

Abstract

This chapter will focus on “small” molecule therapeutics that demonstrate useful immunosuppressant activity including established classes such as calcineurin inhibitors (cyclosporin A and tacrolimus), mTOR (mammalian target of rapamycin) agents (sirolimus, everolimus), and antiproliferative/antimetabolite agents (azathioprine, mycophenolic acid derivatives). This chapter will also introduce some agents with newer pharmacology mechanisms such as sphingosine receptor modulation (FTY720), inhibition of JAK3 (CP-690,550), and inhibition of PKC θ (AEB071). Other agents useful in organ transplantation including glucocorticoids (such as prednisone and dexamethasone), nitrogen mustards (such as cyclophosphamide), and biologic agents (such as muromonab-CD3, basiliximab, and daclizumab) are discussed elsewhere.

Keywords:

  • immunosuppressant;
  • immunosuppression;
  • transplantation