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831 Features
Emerging Drug Discovery Targets; June 28th

29 Jun 04

This edition of "Emerging Drug Discovery Targets" features new approaches to improving intestinal uptake of poorly absorbed therapeutics; a dual 5-LO inhibitor/H1 receptor antagonist for the treatment of asthma; Sitaxentan as an effective treatment of pulmonary arterial hypertension; Kv1.3 potassium channel blockade as an approach to insulin resistance; Drug delivery technology predicted to allow safer and more effective use of steroids in the treatment of rheumatoid arthritis; VEGF receptor tyr
LeadDiscovery

Novartis’/Schering’s VEGF receptor tyrosine kinase inhibitor, PTK787/ZK222584 as a candidate treatment of rheumatoid arthritis.

25 Jun 04

Rheumatoid arthritis is one of the more common autoimmune diseases. LeadDiscovery’s recent state of the art evaluation of rheumatoid arthritis therapeutics evaluates advances in our understanding of the etiology of the disease. One field of research extensively analyzed in this report is angiogenesis. Inhibitors of receptor tyrosine kinase with specific activity against the VEGFRs have been developed in an attempt to prevent angiogenesis. One such molecule is PTK787/ZK222584, synthesized and dev
LeadDiscovery

Drug delivery technology predicted to allow safer and more effective use of steroids in the treatment of rheumatoid arthritis

23 Jun 04

An estimated 5 million individuals suffer from rheumatoid arthritis. Corticosteroids are the most dramatically effective short-term anti-inflammatory drugs; however, clinical benefit for rheumatoid arthritis often diminishes with time. Because of their long-term systemic side effects, corticosteroids are usually given only after a careful and prolonged trial of less hazardous drugs. Liposomes are artificial vesicles efficiently phagocytosed by macrophages and recent advances such as the developm
LeadDiscovery

Kv1.3 potassium channel blockade as an approach to insulin resistance

22 Jun 04

The R&D activity surrounding novel oral treatments of diabetes is considerable and one particular target that has recently received attention is the Kv1.3 potassium channel. Blocking this channel has been thought to be of value in the treatment of multiple sclerosis and more recently for preventing weight gain. Now researchers from Yale have demonstrated that Kv1.3 channel blockers may also increase insulin sensitivity in genetically obese and diabetic mice
LeadDiscovery

Sitaxentan as an effective treatment of pulmonary arterial hypertension

21 Jun 04

Pulmonary arterial hypertension (PAH) represents an unmet market. Initial breakthroughs in treatment focussed on the rare form of this condition, idiopathic pulmonary arterial hypertension. Recently however a key advance in the treatment of PAH was made with the launch of Actelion's twice-daily Tracleer (bosentan) as the first orally active treatment of both idiopathic and secondary PAH. Tracleer is the first generation of a class of drugs known as endothelin receptor antagonists and blocks two
LeadDiscovery

The development of a dual 5-LO inhibitor/H1 receptor antagonist for the treatment of asthma

20 Jun 04

Numerous inflammatory mediators have been implicated in the etiology of asthma. Blocking specific inflammatory mediators has frequently yielded unimpressive clinical results and instead the simultaneous targeting or more than one mediator may be of greater use. In the current edition of LeadDiscovery's TherapeuticAdvances work by researchers at UCB who have developed a dual 5-LO inhibitor/H1 receptor antagonist is highlighted
LeadDiscovery

PABORD - dedicated to Outsourcing in Research and Development

17 Jun 04

PABORD is the first exhibition and conference dedicated to Outsourcing in Research and Development for the Pharmaceutical and Biotechnology industries.
Simon Berger

Pharma NewsBytes: June 16th, 2004

16 Jun 04

Pharma NewsBytes selects out some of the most interesting press releases to have appeared on LeadDiscovery’s DailyUpdates tracking service over the past few weeks. This edition includes an update on selected releases from the American Society of Clinical Oncology and the American Diabetes Association as well as important news concerning the antipsychotic, Abilify (Aripiprazole) and novel HIV treatments
LeadDiscovery

DDP-IV inhibitors as candidates for metabolic disorders, cancer and as model molecules for optimizing intestinal absorption of new therapeutics

16 Jun 04

Researchers have developed a series of assays to identify improved DDP-IV inhibitors for the treatment of diabetes and possibly cancer. The technology described here can also be applied to improving the oral absorption of poorly absorbed drugs in general
LeadDiscovery

Biogenerics market presents new commercial opportunity

11 Jun 04

With several blockbuster biological products approaching patent expiry and the emergence of new approval pathways, the biogenerics segment represents an attractive opportunity for companies looking to escape intensifying competition in the commodity generics sector. However, with the biotech industry preparing significant opposition to any new regulatory initiatives, barriers to market entry could remain high.
Datamonitor

Safety and Efficacy Biomarkers

21 May 04

To aid in your drug development efforts, Pharmaceutical Education Associates is proud to present our inaugural “Identification and Validation of Safety and Efficacy Biomarkers” conference. Ultimately, the drug discovery process must be a collaborative one, drawing together researchers from industry, academia, and government agencies to identify and address all possible benefits and consequences. In that spirit, our top-notch speaking faculty brings together experts from all these groups to add
Jennifer McGinnis

Lilly’s pemetrexed (Alimta) offers potential improvements in the treatment of non-small cell lung cancer (NSCLC)

20 May 04

DailyUpdates 20th April: Nearly 423,000 new cases of small cell lung cancer (SCLC) and non-small cell lung cancer (NSCLC) are expected to have been diagnosed in the seven major pharmaceutical markets in 2003. Despite the high level of pharmaceutical interest, there are significant unmet needs in the disease in terms of poor survival. Docetaxel is the only drug currently approved in both the U.S. and Europe to treat patients with non-small cell lung cancer in the second-line setting. While the dr
LeadDiscovery

NicOx’s nitro-derivative of naproxen, HCT 3012, shown to be effective in a model of myocardial infarction

11 May 04

DailyUpdates 11th May: A number of clinical studies including the VIGOR trial have suggested that the NSAID naproxen may reduce the incidence of myocardial infarction. However the gastrointestinal side-effects of naproxen and its ability to exacerbate hypertension preclude its use in at-risk individuals. Upcoming data about to be published in the journal JPET demonstrate the efficacy of the safer and anti-hypertensive nitro-derivative of naproxen, HCT 3012, in a model of myocardial infarction.
LeadDiscovery

Results from the PACES trials provides further good news for Pfizer’s Celebrex (celecoxib)

10 May 04

DailyUpdates 10th May: Last week European regulators affirmed the safety of Celebrex; good news for Pfizer continues with the emergence of data from the PACES trials reporting that, compared to acetaminophen, Celebrex is both preferred by patients and is of greater efficacy.
LeadDiscovery

Emerging Drug Discovery Targets 6th May

06 May 04

This edition of Emerging Drug Discovery Targets features MBD2 inhibitors as a selective strategy for reducing tumor growth; NicOx's NO-ASA cancer candidate, NCX 4040, MIF as a target for atherogenesis; expanding indications for COX-2 inhibitors; and a dual MMP and TACE inhibitor as a treatment of rheumatoid arthritis. This edition also sees a new section "TherapyUpdate" which this month focuses on Osteoporosis. As usual we also provide updates on industrial advances and licensing opportunities a
LeadDiscovery

Gabapentin as a first line treatment of spinal cord injury-related neuropathic pain

05 May 04

DailyUpdates 5th May: As the battle lines are drawn up between gabapentin and its generic equivalents, research published by Turkish researchers suggests that the first-line use of these therapeutics in the treatment of neuropathic pain associated with spinal cord injury will represent one battle in the war between Pfizer and its competitors.
leaddiscovery

New data reveals that the calcium channel blocker ethosuximide is an effective treatment of cancer pain

29 Apr 04

DailyUpdates 29th April: Cancer pain affects over 3 million people in the US alone. The treatment of this condition, whether it is due to bone metastasis or a result of the use of cytotoxic therapies is challenging. Researchers from McGill University have now demonstrated that ethosuximide, an anti-epileptic and relatively selective T-type calcium channel blocker, is highly effective in reversing neuropathic pain caused by the commonly employed cytotoxics paclitaxel or vincristine. This contr
LeadDiscovery

Merckle demonstrate superior safety of Licofelone the first dual COX/LOX inhibitor: Opportunities for improved osteoarthritis treatment

22 Apr 04

DailyUpdates 22nd April: Phase III studies have previously shown Merkle’s first in the class COX/LOX inhibitor, Licofelone, to be equally effective to standard treatments of osteoarthritis. Moreover, gastrointestinal adverse events tended to be less frequent in patients treated with licofelone as compared to naproxen. In this month’s edition of the American Journal of Gastroenterology new data is published showing clear cut advantages of licofelone arising from the dramatic reduction in incide
LeadDiscovery

HU-320 identified as a novel synthetic cannabinoid with therapeutic activity in an experiment model of rheumatoid arthritis

20 Apr 04

DailyUpdates 20th April: An estimated 5 million individuals suffer from rheumatoid arthritis in the Western world. CB1 cannabinoid receptor ligands are in development as candidate treatments of this disease due to their analgesic properties. Now researchers from the Hebrew University and the Kennedy Institute of Rheumatology in London have demonstrated the anti-inflammatory, disease modifying efficacy of the non-psychoactive cannabinoid, HU-320 in a model of rheumatoid arthritis.
LeadDiscovery

NicOx's nitrosulindac (NCX 1102) emerges as a candidate treatment of bladder cancer

19 Apr 04

DailyUpdates 19th April: NSAIDs have shown promising activity in the prevention and possible treatment of cancer. The French pharmaceutical NicOx has successfully improved both the safety and efficacy of NSAIDs by attaching a nitric oxide donor group to various NSAIDs. In a recent study nitrosulindac has been demonstrated to act as an effective and selective cytotoxic and antiproliferative agent against bladder cancer cells. The efficacy of nitrosulindac was considerable better than sulindac.
LeadDiscovery

Gene silence to set to quieten neuropathic pain - Novartis research expands the potential of siRNA

16 Apr 04

DailyUpdates 16th April: RNA interference is emerging as a major tool to help researchers identify new therapeutic targets. Novartis researchers have recently used this technology to underline the role that the ligand activated cation-channel, P2X3 plays in neuropathic pain. This study also demonstrates the therapeutic potential of P2X3 gene silencing in the treatment of this major unmet area of analgesia.
LeadDiscovery

Paclitexel-induced neuropathic pain - McGill study may lead to the identification of novel targets for analgesia and improved cancer therapeutics

14 Apr 04

DailyUpdates 14th April: Neuropathic pain affects 26 million patients including a sub-population of cancer patients being treated with cytotoxics. McGill researchers have published the results of a study looking at neuropathic pain in various strains of mice. These data show that neuropathic pain has a genetic component suggested to be equally relevant to paclitaxel and surgically-induced pain. The study also advances the use of paclitaxel-induced hyperalgesia as a model for the development o
LeadDiscovery

Novo Nordisk publish data demonstrating proof of concept for potassium channel openers as treatments of diabetes

13 Apr 04

DailyUpdates 13th April: According to WHO, there are some 130 million diagnosed diabetics in the world, a figure that is predicted to increase to 300 million by 2025. Approximately 10-15% of these patients suffer type 1 diabetes. Novo Nordisk have shown that their Kir6.2/SUR1 channel opener, NN414 is able to preserve beta-cell function and reduction of insulitis presumable through the induction of "beta-cell rest".
LeadDiscovery

Drug delivery technology predicted to allow safer and more effective use of steroids in the treatment of rheumatoid arthritis

08 Apr 04

DailyUpdates 8th April: An estimated 5 million individuals suffer from rheumatoid arthritis in the Western world. Corticosteroids are the most dramatically effective short-term anti-inflammatory drugs; however, their clinical benefit for rheumatoid arthritis often diminishes with time. This, the severe rebounds observed following the withdrawal of corticosteroids, and long-term systemic side effects associated with corticosteroids limits their use in the treatment of rheumatoid arthritis. Rese
LeadDiscovery

Eli Lilly's Duloxetine set to become the first widely used therapeutic treatment of stress urinary incontinence

07 Apr 04

DailyUpdates 7th April: A recent survey of community-dwelling women in France, Germany, Spain and the UK found that 35% women suffer urinary incontinence, the most prevalent form of which was stress urinary incontinence. The findings also revealed that two-thirds of women affected with urinary incontinence never consulted a health care professional for treatment. The perceived and real lack of pharmaceutical options for the treatment of stress urinary incontinence is a major factor contributing
LeadDiscovery

New data shows that intensive treatment of diabetes may lower coexistent hypertension and delay renal dialysis by up to 20 years

06 Apr 04

DailyUpdates 6th April: According to WHO, there are some 130 million diagnosed diabetics in the world and the long term consequences of diabetes such as diabetic nephropathy are becoming increasingly frequent and unmet components of diabetes care. In a recent study Glasgow Royal Infirmary researchers report that intensive treatment slowed progression of renal disease within 2 years in patients with established diabetic nephropathy and predict that this approach may delay the onset of dialysis b
LeadDiscovery

Links between obesity/diabetes & Alzheimer disease: Diet-induced insulin resistance shown to increase CNS beta-amyloid levels and worsens cognition in a model of Alzheimer disease

05 Apr 04

DailyUpdates 5th April: There is growing evidence of a link between type-2 diabetes/obesity and Alzheimer disease. Researchers now report that diet-induced insulin resistance increases beta amyloid generation, amyloid plaque burden in the brain and behavioural impairment in a model of Alzheimer disease.
Leaddiscovery

Type 2 diabetes as a risk factor for Alzheimer's disease - defective insulin-degrading enzyme as an etiological link?

02 Apr 04

DailyUpdates 2nd April: There is growing evidence that type-2 diabetes is a risk factor for Alzheimer disease. In their April American Journal of Pathology article Brigham and Women's Hospital researchers add further evidence to support defects in insulin-degrading enzyme activity as a potential cause of this phenomenon. This and similar data argues for the development of cross-indication treatments of type-2 diabetes and Alzheimer disease and GSK-3 inhibitors may fit the bill.
LeadDiscovery

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