Erythropoietin has long been recognized as an alternative to
blood transfusion in treating the severely debilitating
phenomenon of cancer-related anemia. Although effective, human
recombinant erythropoietins are expensive and require
injection. Despite these short-comings, recombinant
erythropoietin represents a large market, however the
development of orally active small molecule mimics would
represent significant improvements to this field. Such
molecules would be indicated for cancer in general as well as
other conditions associated with anemia. Multiple myeloma is
associated with severe anemia and furthermore due to the
paucity of effective treatment options, prognosis is poor.
Erythropoietin effectively treats anemia in multiple myeloma
patients and moreover it also dramatically reduces tumor
progression in preclinical multiple myeloma models.
Erythropoietin mimics may therefore treat the anemia
associated with this disease and the underlying disease
itself. The proof of concept for developing novel
erythropoietin ligands for cancer in general and particularly
for multiple myeloma is therefore strong. This dossier :
> Overviews the causes and effects of cancer-related
anemia and how erythropoietin has become established as an
accepted therapy
> Summarizes the characteristics and treatment options
for multiple myeloma
> Profiles erythropoietin receptor ligands and also
multiple myeloma treatments currently in pharmaceutical
development
> Overviews the erythropoietin market
> Compares the potential of novel erythropoietin ligands
to the existing market
> Identifies research tools for the development of
erythropoietin ligands
> Suggests screening architectures for the development
of therapeutic candidates
> Offers practical input to help expedite the screening
process focussing on novel HTS/MTS assays designed to reduce
bench to clinic down-time and assays using human material to
fully characterize the clinical potential of hits
> Lists field leaders
Publication date:10th October 2001; 4177 words
About the Author: Dr Jon Goldhill has over 10 years of
academic and industrial research experience including 5 years
in middle management at the French pharmaceutical giants,
Sanofi-Synthelabo. Focussing on a variety of indications
including inflammatory disorders, GI disease, Urological
conditions and cancer, Dr Goldhill was responsible for target
identification and project development. Dr Goldhill is now CEO
and chief analyst at LeadDiscovery and coordinates the
identification of candidate drug discovery projects with
industrial potential.
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