Saturday 20 February 2016

A new hope to combat Dementia?

Findings from a study led at the University of California revealed a new drug that could be a potential treatment for memory loss caused by neurodegenerative diseases. This study was performed in collaboration with Takeda Pharmaceuticals, and was recently published in the Journal of Medicinal Chemistry (February 2016).

Dementia is one of the earliest manifesting symptoms in the development of Alzheimer’s disease and Schizophrenia, affecting nearly 44.4 million people worldwide. One of the leading causes of death among senior citizens, dementia global healthcare costs account to roughly USD 818 billion today.1 Most of the currently approved medications although provide symptomatic relief, fail to curb the progress of neurodegeneration. More often than not, drugs in clinical trials are unable to qualify the stringent regulatory requirements and fall through owing to multiple organ side effects.2

Apart from understanding the molecular mechanisms contributing to neurodegeneration, there has been much emphasis on drug development research in this area. Li et al. have reported the synthesis of a library of seventy six molecules designed to target an enzyme called phosphodiesterase (Type 1) aimed to treat cognitive impairment.3 Drugs designed for central nervous system disorders often face the challenge to penetrate the blood brain barrier and to reach the target site. Apart from limited loss during metabolism, most of the synthesized molecules also displayed good brain penetration capacities. X-ray crystallography technique was employed to study the mechanism at the molecular level in detail, which will be useful to design next generation molecules. One of the best performing drugs was taken to preclinical testing, and interestingly the results indicated its potential to translate its memory enhancing potential when tested in mice.

Most of the current drug regimens have proved to be little useful in treating severe symptoms of memory dysfunctions. With an optimal balance of physicochemical properties and a favourable safety profile in Phase 1 Clinical trials, the drug in question promises to be a suitable exploratory candidate for treating dementia in advanced stages neuro disorders.

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