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Tuesday 22 May 2012

Challenges

New drug development for central nervous system disorders (CNS) easily qualifies amongst the greatest challenges for modern medicine. Companies striving to develop CNS medicines confront a higher rate of failure compared to any other discipline. The source of the challenge is the complexity of the human brain and the highly selective barrier that polices the flow of compounds into it, as well as the challenges involved in designing studies that give consistent and reliable data.

Pharmidex, Britain

Pharmidex

Essential Step

Pharmidex

 

‘Effective prediction of the ability of compounds to permeate the blood brain barrier is an essential step on the critical path for CNS drug discovery,’ explains Dr. Mohammad Alavijeh, Managing Director of Pharmidex. ‘To best assess the potential for therapeutic activity or side effects, studies need to be conducted in the particular brain region affected by the disease.’ Some assessments fall short because they treat the brain as a histologically-homogenous organ. Or place an over reliance on the results of DMPK studies in assessing CNS therapeutic potential. ‘Just because it’s in the blood, doesn’t mean it’s in the brain,’ says Alavijeh.

Direct Assessment

Pharmidex

 

Pharmidex is the only company in the world offering direct assessment of brain penetrability and free concentration of compounds in extracellular fluid as a service to CNS R&D departments. Microdialysis measurement is one part of an integrated package of blood-brain barrier services designed to expedite the transition of new chemical entities from hit to optimised lead. The range of services include ranking the ability of compounds to cross the blood brain barrier, comprehensively assessing their neuro-pharmacokinetic and -pharmacodynamic properties, and working with proprietary delivery technologies to transport compounds with high potential (but low penetrability) across the blood brain barrier…

Collaborative Agreement

In 2007, Pharmidex signed a collaborative agreement with Genzyme Pharmaceuticals to launch Cerense,SM a product development platform designed to substantially improve the development success of CNS compounds that normally exhibit poor permeability of the blood brain barrier. The platform combines a patented lipid-based drug delivery system with Pharmidex’s specialized neuro-pharmacokinetic and pharmacodynamic expertise. CeresnseSM can take a non-or lowpenetrating lead compound and establish a comprehensive set of data to demonstrate that it gets into the brain where it is able to interact with its molecular target and produce the desired therapeutic benefit.

Immense Therapies

The impact of CerenseSM technology for improving the development of CNS therapies is immense and could touch everything from the treatment of Alzheimers’ to brain cancer. Pharmidex is initially investigating the ability of CerenseSM to surmount the obstacle of getting chemotherapy into the brain. CerenseSM in conjunction with intra-arterial chemotherapy has been shown to enable enhanced access of anticancer drugs to the tumor mass and to infiltrative malignant cells at the tumor edge. ‘When we talk of blood-brain barrier solutions, we are talking prediction, assessment and delivery – all powered by NeuroPK®. Our dream is that NeuroPK® becomes established as ‘business-as-usual’ for any company developing brain medicines. This will fast-track decision-making and reduce development time for CNS medicines which is the fastest-growing unmet medical need today,’ said Dr Alavijeh.