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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
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. The market for diabetes therapeutics is also rising with global sales reportedly topping $8.1 billion for the 12 months to September 2000, a 19% increase over the previous 12 months (for a full ana…

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
Pulmonary arterial hypertension (PAH) exists in a rare idiopathic or unexplained form (which occurs in familial and sporadic forms) called idiopathic pulmonary arterial hypertension (IPAH, previously referred to as primary pulmonary hypertension, PPH)) and a relatively common form of secondary pulmo…

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
The incidence of asthma has dramatically increased over recent years and although currently available treatments are generally effective, patient compliance is currently poor, especially with respect to inhaled treatment. Furthermore, 5% of patients are unresponsive to these treatments and it is this cohort that accounts for a large segment of asthma related healthcare…

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
Glucagon like Peptide-1 (GLP-1) is a gut hormone released after food consumption to stimulate insulin secretion. GLP-1 has a very short half-life due to its degradation by the proteolytic enzyme dipeptidyl peptidase-IV (DPP-IV; CD26) which cleaves peptides after proline residues. Therefore, specific inhibition of DPP-IV is an attractive therapeutic approach to stimulate glucose dependent insulin secretion. In addition to its role in glucose homeostasis, DPP-IV has been implicated in immune disorders, HIV-1 infection and tumor progression a…

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

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.
In the report 'Biogenerics: Drivers and Resistors of Market Development', Datamonitor evaluates developments in the regulatory environment for biogenerics in the US and EU. The research also analyzes possible market entry strategies and assesses the market potential of biogenerics, and the barriers to companies wishing to enter the industry. Growing demand for biogenerics Despite st…

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
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 i…

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.
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-r…

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.
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. Osteoarthritis is characterized by the degeneration of the articular cartilage and is the most prevalent form of arthritis, affecting 10% of the population, equating to a patient population of over 73 million people in the seven major pharmaceutica…

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
Emerging Drug Discovery Targets from LeadDiscovery 6th May 2004 to view this alert on line please go to http://www.leaddiscovery.co.uk/TherapeuticAdvances%20Archive/May%206th%20emerging%20targets.htm ************************************** "Emerging Drug Discovery Targets" provides a twice monthly su…

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.
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. Approximately 26 million patients worldwide (10 million in the ) suffer from some form of neuropathic pain…

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

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
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 licof…

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.
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 Ken…

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.
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 s…

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.
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 t…

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
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 ne…

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".
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…

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
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.&nb…

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
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 af…