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Biology for Chemists

23- 24 June 2008

Biology for Chemists



Chemistry & IndustrySpot on acne treatment


A safe, effective treatment for acne is being developed, Sarah Houlton reports in Chemistry & Industry


on the spotA product being developed by Summit, formerly Vastox, could provide a safe, effective treatment for acne. Current treatments are largely ineffective, and the most successful, Roaccutane, is teratogenic and can cause a wide range of side effects.

Acne develops when too much sebum is produced in the skin, and the sebaceous glands are infected by the bacterium Propionibacterium acnes. Inflammatory mediators are released into the hair follicle and the dermis around it, and the process of hyperkeratinisation occurs, where dead cells become trapped in the follicle.

Summit’s developmental product is a rational reprofiling of established drugs, explains the company’s director of clinical development, Nigel Blackburn. ‘We are taking the known side effects of older drugs, and turning them into clinical benefits,’ he said. The drugs may be on the market, or alternatively might have been abandoned during the development process, perhaps as a result of the side effects that are being turned into an advantage.

There is a potential drawback to this strategy, however – the original pharmacological activity of the drug could become a side effect in the reprofiled one. By using two different drugs, both with known sebum-reducing side effects that could be beneficial in acne, and each given in a lower dose than would normally be prescribed, Blackburn said they would hope to get additive effects that would improve the symptoms of acne.

In a Phase I study in nine patients, sebum production was reduced by up to 70% with a single oral dose, and a second Phase I study in 18 patients is now under way. ‘The Phase I results are startlingly good,’ he said. ‘Reducing sebum production has been the “holy grail” of acne treatment for 30 years, and there has been little success aside from Roaccutane which had side effects.’ The initial aim of the drug reprofiling had been to treat sebum over-production in Parkinson’s disease patients, but the sebum reduction proved so effective that the company is now targeting acne, too.

The reprofiling strategy is also being used in the development of a drug to prevent another Parkinson’s symptom – dribbling. Dry mouth is a common side effect of drugs, and the aim is to turn this to an advantage, again using a combination of two drugs at sub-therapeutic doses. ‘The preliminary evidence is that there is indeed an additive effect,’ Blackburn said. ‘We are now setting up a combined Phase I/II trial in Parkinson’s patients, and we hope to have the results next year.’

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