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Emerging Drug Discovery Targets (18th December 2003)

Posted on: 05 Jan 04


This edition of features new generation oncolytic viruses from Cell Genesys active against colorectal cancer cells; a p38 MAPK inhibitor for the treatment of rheumatoid arthritis from Fujisawa; data describing the anti-angiogenic activity of bisphosphonates in cancer models; a new JAK3 inhibitor from Pfizer for transplant rejection; and an integrin antagonist from Merck for the treatment of osteoporosis. As usual updates on industrial advances and licensing opportunities are provided.


Emerging Drug Discovery Targets

from LeadDiscovery

18th December 2003

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"Emerging Drug Discovery Targets" provides a twice monthly summary of some of the most exciting breaking information recently featured by the pharmaceutical analysts, LeadDiscovery. Information includes editorials on recently published journal articles, selected press releases and "intelligence reports". Our target audience includes business development personnel, senior management and researchers within the drug development sector as well as bioscience investors and analysts.

Please feel free to pass this mail onto colleagues that may benefit from registration to Emerging Drug Discovery Targets. To register click here.


In this weeks edition:

  • Editorial comment on selected journal articles
      • Targeting oncolytic viruses to colorectal tumors [more]
      • FR167653, a candidate p38 MAPK inhibitor for the treatment of rheumatoid arthritis [more]
      • Bisphosphonates as inhibitors of tumor angiogenesis [more]
      • Janus tyrosine kinase 3 inhibition for the prevention of transplant rejection [more]
      • Alpha(v)beta(3) integrin antagonism as a treatment of osteoporosis [more]
  • A fortnight in Drug Development: Advances from industry [more]
      • Progress towards the treatment of Alzheimer's disease
      • New approaches to autoimmune diseases and acute and chronic inflammatory disorders
      • News from the 26th Annual San Antonio Breast Cancer Symposium
  • Today's breaking scientific publications for the drug development community [more]
  • This week's licensing opportunities [more]
  • New DiscoveryDossiers/Chemistry Libraries [more]:
      • Antibodies as Cancer Therapeutics - R&D & Business Perspectives
      • Growth Factors: Indications, Products, and Markets
      • Antidepressants: World Prescription Drug Markets
      • Market for Lead Optimization Tools and Services: Applying the new "-omics" to enhance drug discovery
      • U.S. Alzheimer's Disease Medications Markets
      • Nuclear Receptors: Key Targets for New Pharmaceuticals
  • Emerging Drug Discovery Targets archive

Targeting oncolytic viruses to colorectal tumors: Cancers of the colon and rectum remain responsible for 56,000 deaths every year in the US, second only to lung cancer. Surgery remains the main form of treatment and is often the only treatment used in early-stage disease. Current surgical practices can however cure only 40%-50% of early-stage cases and improved pharmaceutical approaches are therefore urgently sought (for a full analysis of therapeutic and market opportunities for colon cancer click here). Oncolytic viruses represent an emerging approach to the treatment of cancer. Here we highlight the development of a replication-competent virus being developed by Cell Genesys that has been engineered to selectively replicate in cancer cells expressing the carcioembryonic antigen (CEA), a protein that is frequently over-expressed in colorectal cancers. This virus demonstrates excellent efficacy without adverse effects in an animal model of colorectal cancer...[more on these findings]


FR167653, a candidate p38 MAPK inhibitor for the treatment of rheumatoid arthritis Approximately one in five people in the western world suffer from autoimmune diseases and an estimated 5 million individuals suffer from rheumatoid arthritis (RA). The field of RA therapeutics is attracting massive interest in the wake of resurgent R&D activity that has advanced our understanding of the etiology of the disease. One target analyzed in LeadDiscovery’s state of the art analysis of RA drug discovery targets and therapeutic candidates, “Rheumatoid arthritis: Emerging drug discovery targets and therapeutic candidates” (click here) is p38 mitogen-activated protein kinase (MAPK). In this edition of TherapeuticAdvances we highlight recent data describing Fujisawa Pharmaceutical’s MAPK inhibitor, FR167653...[more on these findings]


Bisphosphonates as inhibitors of tumor angiogenesis: Bone metastases to bone affects quality of life. Following their approval for the treatment of osteoporosis, bisphosphonates were also approved for the treatment and prevention of fractures related to metastatic disease. Clinical trials of zoledronic acid for example have shown that it can reduce markers of bone resorption by 40% to 60% in patients with multiple myeloma and breast, prostate, and lung cancers. More recently researchers have demonstrated that bisphosphonates have direct antitumor effects; for example zoledronic acid is a potent inhibitor of angiogenesis. Here we highlight data showing for the first time the anti-angiogenic activity of a bisphosphonate in a model of tumor progression. This data also suggests that effects are both direct, blocking multiple steps of the angiogenesis process, and indirect, reducing the liberation of angiogenic mediators by cancer cells...[more on these findings]


Janus tyrosine kinase 3 inhibition for the prevention of transplant rejection: The global market for immunosuppressant therapy is in excess of 4 billion USD per year. This therapeutic class is used for the treatment of both autoimmune diseases (see our recent analysis of rheumatoid arthritis therapeutics) and for the prevention of organ rejection in transplantation. In the context of transplantation, immunotherapy commonly involves the use of azathioprine beginning at the time of transplantation often combined with low doses of cyclosporine. However, immunosuppressants suppress all immunologic reactions, thus making overwhelming infection the leading cause of death in transplant recipients. In addition immunosuppressants are associated with severe toxicity. A newer molecular target being investigated for the prevention of transplant rejection is Janus tyrosine kinase 3 (Jak3). Jak3 is this months "Target of the Month" and here we describe Pfizer's efforts to optimize inhibitors of this kinase...[more on these findings]


Alpha(v)beta(3) integrin antagonism as a treatment of osteoporosis: An estimated 10 million Americans over the age of 50 years old suffer from osteoporosis and a further 32.9 million have low bone mass, placing them at an increased risk for developing this condition. Patients with these conditions carry an increased risk of sustaining fractures, which are both clinically problematic and costly to healthcare systems, and the development of new osteoporosis treatments therefore offers immense opportunities to the pharmaceutical industry. In a recent DiscoveryDossier we analyze therapeutic and pharmaceutical opportunities in the field of osteoporosis (click here for access). One new molecular target being investigated for the possible treatment of osteoporosis is alpha(v)beta(3) integrin. Researchers from Merck have been actively involved in the rational design of small-molecule alpha(v)beta(3) integrin antagonists and here we highlight their most recent data relating to the optimization of a series of imidazolidinones which has produced a candidate for clinical trials...[more on these findings]


A fortnight in Drug Development - Our Tour of Industry Press Releases

Key press releases selected from recent editions of the tracking service, DailyUpdates.

  • Progress towards the treatment of Alzheimer's disease [ more]
  • New approaches to autoimmune diseases and acute and chronic inflammatory disorders [more]
  • News from the 26th Annual San Antonio Breast Cancer Symposium [more]

New DiscoveryDossiers & PharmaReports:


    Last updated on: 27/08/2010 11:40:18

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