18 junio 2011

Protein Kinase Inhibitors for CNS Diseases at the Research and Discovery Phase . Noscira Pionera en Alzheimer y Paralisis Supranuclear Progresiva .

Genetic Engineering & Biotechnology News , Medio Especializado que Publica este mes sobre la I+D en Neurologia y las lineas existentes en desarrollo clinico para tratar enfermedades como Alzheimer o Paralisis Supranuclear destacando las espectativas del Compuesto Tideglusib de Noscira , concretamente el Nypta para Alzheimer y el Zentylor para Paralisis y ambos ya en plena Fase II .

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Protein kinases (PK) have provided drug targets that have yielded innovative and highly effective therapeutics for cancer treatment. These include small molecule PK inhibitors such as Novartis’ Gleevec, Pfizer’s Sutent, GlaxoSmithKline’s Tykerb, and Bristol-Myers Squibb’s Sprycel. PK inhibitors now comprise over 30% of most major pharmaceutical companies’ pipelines. By 2020, small molecule kinase inhibitors are expected to collectively generate annual revenues of over $25 billion.

The success of kinase inhibitors in cancer has spurred research to develop similar compounds for other diseases including neurodegenerative disorders. But how close to the clinic are kinase inhibitors for central nervous system (CNS) diseases? Noscira has one drug candidate that is in Phase II for supranuclear palsy and is also ready to enter mid-stage trials in Alzheimer disease (AD).

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Clinical Development
Noscira is the only company with a clinical-stage kinase inhibitor for a neurodegenerative disease, however. Its candidate, a small molecule GSK-3beta inhibitor called tideglusib, has orphan drug designation in the EU and fast-track status in the U.S. Last October Noscira said it had completed recruitment for its Phase II trial in supranuclear palsy.

In Alzheimer disease Noscira received approval in April to begin a Phase IIb trial. The company says that the compound has proven active against all of the histopathological lesions associated with the disease in experimental models: It reduces phosphorylation of the tau protein and hippocampal and entorhinal cortex neuron loss, improves spatial memory deficits, and reduces the accumulation of amyloid plaques in the brain. It also provides neuroprotection in vivo and has an anti-inflammatory effect in a range of animal models, the firm adds.

A Phase IIa trial in Germany was completed in early 2010. It was designed with the primary goal of assessing the safety and tolerability of the molecule. The company reported that the drug was well tolerated and had “a positive effect on patients’ cognitive performance”, although the results were not statistically significant “due to the small sample size and short treatment period.”

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Zeltia , Presentación en el 7º Foro MED CAP .

Exemestano . Una pastilla al día para prevenir el cáncer de mama .