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Emerging Drug Discovery Targets

21st November 2003 Posted on: 21 Nov 03


This edition of "Emerging Drug Discovery Targets" features a potent histone deacetylase inhibitor from Norvartis for the treatment of cancer, two new approaches to metabolic disorders and VEGFR-1 as a target for rheumatoid arthritis. As usual we also provide updates on industrial advances and licensing opportunities.


Emerging Drug Discovery Targets

from LeadDiscovery

21st November 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.

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In this weeks edition:

  • Editorial comment on selected journal articles
      • NVP-LAQ824, Novartis' novel histone deacetylase inhibitor [more]
      • The involvement of PDE4D in stroke [more]
      • 11beta-hydroxysteroid dehydrogenase inhibition reduces insulin resistance [more]
      • Mutual regulation of angiogenesis and adipogenesis [more]
      • VEGFR-1 as a target for rheumatoid arthritis therapies [more]
  • A fortnight in Drug Development: Advances from industry [more]
      • The battle for the anti-hyperlipidemia market
      • Recent surges in rheumatoid arthritis development activity
      • Depressing news for anti-depressants
  • Today's breaking scientific publications for the drug development community [more]
  • This week's licensing opportunities [more]
  • New DiscoveryDossiers/Chemistry Libraries [more]:
      • Rheumatoid arthritis: Emerging drug discovery targets and therapeutic candidates
  • Emerging Drug Discovery Targets archive

NVP-LAQ824, Novartis' novel histone deacetylase inhibitor: The field of histone deacetylation continues to receive considerable interest principally due to the ability of histone deacetylase (HDAC) inhibitors to produce cytostatic activity in cancer (click here to access "Histone deacetylase inhibitors: Redefining pharmaceutical approaches to the treatment of cancer"), but more recently due to the role that this class has in other indications such as autoimmune disorders (click here). Novartis researchers have now developed a HDAC inhibitor of greater anti-proliferative potency than that of SAHA, and which almost completely blocked the growth of both human colon and lung cancer xenografts...[more on these findings]


The involvement of PDE4D in stroke Stroke represents a largely unmet market; 600,000 individuals suffer a stroke in the US each year and more than 160,000 die from stroke-related causes. Patients that present more than 3 hours after the onset of symptoms are particularly difficult to treat since neural cell death becomes a major problem as do the neurological consequences of synaptic loss. Ischemic stroke which accounts for 80-90% of strokes can be sub-divided into large vessel occlusive disease (carotid stroke) which is commonly due to atherosclerosis of the common and internal carotid arteries; small vessel occlusive disease due to non-atherosclerotic narrowing of small end-arteries in the brain; and cardiogenic stroke due to blood clots arising from the heart. The Icelandic biotech deCode have recently published ground breaking data linking PDE4D (one of four PDE4 isoforms which exists in multiple splice variants) with stroke...[more on these findings]


11beta-hydroxysteroid dehydrogenase inhibition reduces insulin resistance: Obesity and comorbid type 2 diabetes are two frequent and growing global problems. The insulin resistance syndrome was first described in 1988 and contributes to both conditions and indeed is generally accepted to represent a pathophysiological link between the two. Considerable attention has been paid to the development of molecules able to reduce insulin resistance. LeadDiscovery has recently published a report overviewing the therapeutic potential of one class of molecules that fits this profile, the GSK-3 inhibitors (Click here for access). Here we highlight a second strategy for reducing insulin resistance, the inhibition of 11beta-hydroxysteroid dehydrogenases (11beta-HSD)1, an enzyme which activates glucocorticoid. Biovitrum have firmly established this enzyme to be a target for the treatment of metabolic diseases and now have a candidate enzyme inhibitor in clinical development...[more on these findings]


Mutual regulation of angiogenesis and adipogenesis: Angiogenesis, the formation of new blood vessels, is crucial to a number of physiological processes as well as in disease states. Consequently angiogenesis represents an emerging therapeutic target which by 2006, is expected to command a market of $1.75 billion. Tumor vascularization is key to the development of solid tumors and the vast majority of pharmaceutical activity surrounding angiogenesis relates to the development of therapeutic strategies to destroy existing tumor vasculature or to prevent neovascularization. New indications for inhibitors of angiogenesis include rheumatoid arthritis (click here). In their 2002 paper Judah Folkman’s group reported that angiogenesis inhibitors were able to induce weight loss without altering calorific intake, a finding which has led to obesity emerging as a further indication for inhibitors of angiogenesis. Here we highlight the interaction between adipocyte differentiation and vasularization...[more on these findings]


VEGFR-1 as a target for rheumatoid arthritis therapies: Rheumatoid arthritis (RA) is one of the more common autoimmune diseases and as described in LeadDiscovery’s state of the art analysis of rheumatoid arthritis drug discovery targets and therapeutic candidates (click here), this field is attracting massive interest in the wake of resurgent R&D activity which has advanced our understanding of the etiology of RA. One field of research being advanced aggressively in the context of RA is angiogenesis. In our previous edition of TherapeuticAdvances we highlight the central role of Tie2 in this process (click here). Here we describe a key study supporting VEGFR-1 as a target...[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.

  • The battle for the anti-hyperlipidemia market [more]
  • Recent surges in rheumatoid arthritis development activity [more]
  • Depressing news for anti-depressants [more]

New DiscoveryDossiers:

  • Rheumatoid arthritis: Emerging drug discovery targets and therapeutic candidates[more]


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

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