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MULTIPLE SCLEROSIS
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halidomide-based
compounds WASHINGTON
08/19/96 /PRNewswire/ -- Modifications in the chemical structure of thalidomide
by Celgene Corporation (Nasdaq: CELG) have resulted in a novel series of
compounds that may be useful for treating a wide range of inflammatory diseases,
including rheumatoid arthritis, inflammatory bowel disease, and other
conditions, according to a collaborative study reported today by scientists at
Celgene and The Rockefeller University. The research was released today in the
Journal of Medicinal Chemistry, a publication of the American Chemical Society (ACS).
"Celgene
has adopted the name 'SelCID(TM)' for its new family of thalidomide-based
compounds. Selective in their cytokine inhibition properties, they appear to be
highly specific for the suppression of tumor necrosis factor-a (TNF-a),"
according to Sol Barer, Ph.D., President and COO of Celgene. Chronic
overproduction of TNF-a a cytokine produced by immune cells in the blood stream,
has been linked to many inflammatory conditions, including rheumatoid arthritis,
multiple sclerosis, septic shock, leprosy and tuberculosis. "This
compelling research confirms that thalidomide's ability to inhibit this
destructive immune response can be optimized through careful drug design and
synthesis," said Dr. David Stirling, Executive Vice President
Pharmaceutical Research & Development at Celgene. "The potential
benefits of thalido Page
1
10/09/00mide-like compounds for
immunotherapeutics is of considerable scientific interest. We believe this novel
class of compounds contains excellent candidates for pharmaceutical
development." According
to the Journal of Medicinal Chemistry communication, more than 20 racemic
(mixture of both chiral forms) analogues of thalidomide were synthesized and
tested for their ability to inhibit TNF-a production. Analogues with potency up
to 400 to 500 times greater than the original thalidomide were discovered in the
study. Celgene plans to report further on the safety and potency of its SelCID
analogues in near future. The new series of SelCID compounds, which are covered
under patents filed by Celgene, are undergoing evaluation in the company's
pre-clinical toxicology program. "Additionally,
our data demonstrate that both chiral forms of the analogues have a similar,
potent impact on TNF-a production," said George Muller, Ph.D., Group Leader
for Medicinal Chemistry at Celgene and co-author of the Journal report.
"This finding suggests that if one chiral form was eventually found to have
undesirable safety profile, its counterpart could afford the desired beneficial
control of TNF-a overproduction with fewer side effects." Celgene's
formulation of thalidomide (SYNOVIR(TM)) is in a pivotal clinical trial for the
treatment of AIDS-related weight loss (cachexia). SYNOVIR is also being
evaluated clinically for a variety of other disease states, including the
chronic diarrhea frequently associated with AIDS, graft- versus-host-disease
following bone marrow transplantation, and rheumatoid arthritis. Additional
co-authors of the Journal communication, entitled "Structural Modifications
of Thalidomide Product Analogs with Enhanced Tumor Necrosis Inhibitory
Activity," include: David I. Stirling, Laura G. Corral, Mary G. Shire, and
Hua Wang, of Celgene Corporation; and Gilla Kaplan and Andre L. Moreira, in the
Laboratory of Cellular Physiology and Immunology of The Rockefeller University. Celgene
Corporation uses proprietary expertise in small molecule chemistry to develop
novel therapeutic agents and provide fine chemicals for the pharmaceutical,
agrochemical, and allied industries. The company is headquartered in Warren, NJ.
The
American Chemical Society, founded in 1876, is the world's largest scientific
society, with more than 150,000 members. The Society is located in Washington,
DC. SOURCE Celgene Corporation
©
1998 International MS Support Foundation International
MS Support Foundation |
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