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Deriving new drugs from thalidomide.

Thalidomide, a nausea-fighting sedative synthesized during the 1950s but never approved for use in the United States because of its fetus-harming effects, is spawning a new generation of drugs that can treat inflammation and immune system disorders (SN: 12/24&31/94, p.424).

George W. Muller and David I. Stirling, chemists at Celgene Corp. in Warren, N.J., reengineered thalidomide to create a new series of therapeutic agents.

The researchers have designed the drugs, they say, to regulate the body's production of tumor necrosis factor alpha. This protein plays a key role in inflammatory and immunological disorders such as rheumatoid arthritis, lupus, inflammatory bowel disease, and leprosy.

Scientists at Johns Hopkins University in Baltimore are currently studying several of these new Celgene agents for treatment of graft-versus-host disease, which often follows bone marrow transplants, Muller adds.

In designing these new molecules, Muller and Stirling said, they improved the potency of the portion of thalidomide exhibiting medicinal properties and removed the segment causing birth defects.
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Title Annotation:Chemistry; new thalidomide agents regulate body's ability to produce tumor necrosis factor alpha, a major contributor to inflammatory and immunological disorders
Author:Lipkin, Richard
Publication:Science News
Article Type:Brief Article
Date:Sep 9, 1995
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