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Scientists from Drug Discovery Pipeline of GIBH have identified anti-neuroinflammatory agent to treat Alzheimer’s disease

Alzheimer’s disease (AD) is an irreversible, progressive brain disease that slowly destroys memory and thinking skills, and eventually even the ability to carry out the simplest tasks. Approximately 100 million people worldwide are living with AD and the number is still increasing. In 2012, the direct costs of caring for those with AD or other dementias to American society will total an estimated $200 billion, including $140 billion in costs to Medicare and Medicaid. Until now, there have been very few approved AD drugs, such as donepezil and memantine, providing minimal symptomatic relief rather than altering the disease progression. Thus, new therapies with improved efficacy or even the ability to modify the disease will hold a strong competitive advantage in market.



Insufficient understanding of the pathogenesis of AD makes disease-modifying anti-AD drug discovery a challenging task. Inspired by the importance of microglia-driven neuroinflammation in the progression of AD, the research group led by Dr Wenhui Hu has used a new approach which identifies inhibitors aiming at neuroinflammation cycle and in vivo pharmacology. Increasing amount of evidence has demonstrated that inhibition of neuroinflammation cycle is a promising therapeutic strategy to address AD. Dr Hu and his team have identified a compound called AD16. From their data in standard AD models it has been demonstrated that AD16 can target the neuroinflammation cycle and alter the disease progression through attenuating the subsequent neuronal synaptic dysfunction and behavioral alterations.



AD16 is a drug candidate for the treatment of AD which can target the neuroinflammation cycle. Preclinical studies demonstrate that the anti-neuroinflammatory agent is able to effectively counteract spatial learning and working memory impairments in β-amyloid induced APP/PS1 double transgenic Alzheimer mouse models. The overall in vivo efficacy of AD16 is even better than the first line marketed anti-AD drugs, donepezil and memantine. This small synthetic molecule is orally bioavailable (F = 74.9%, T1/2 = 4.3 h) and prone to penetrate the Brain-Blood Barrier. Oral administration of AD16 can significantly reduce the behavioral deficits and help to restore cognitive function in Alzheimer mouse models. No chronic toxicity and adverse effect has been observed during the pharmacological evaluation.



To protect the potential commercial value of Dr Hu’s novel neuroinflammatory inhibitors, GIBH has filed patent applications in China for the intellectual property rights of our novel neuroinflammatory inhibitors including AD16 in the treatment of AD and other neuroinflammation related diseases. Currently, the patent is under verification. Patent applications to protect the intellectual property rights of these novel neuroinflammatory inhibitors in North America and European Union have also been submitted to World Intellectual Property Organization (WIPO). Preclinical studies for drug candidate AD16 in industry-standard models of AD have been started in collaboration with South China Center for Innovative Pharmaceuticals (SCCIP). Phase I clinical trials for drug candidate AD16 will be initiated in 2014.





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