Ion channel specialist receives innovation award

By Mike Nagle

- Last updated on GMT

Related tags: Ion channels, Action potential

A company that specialises in designing first-in-class small
molecule drugs that modulate ion channels has been given an award
for its innovative preclinical research.

Lectus Therapeutics is focussed on designing first-in-class drugs that modulate ion-channels, which, due to its novel approach, could potentially overcome side effects seen with conventional therapeutics. The ERBI, a UK networking association for Europe's largest biotech cluster, has given its 2007 Innovation in Drug Discovery and Development Award to the biotech. Ion-channels are an important class of targets for drug development because they play a critical role in many processes in the human body, including nerve impulses and immune system signalling. However, as Lectus' CEO Roland Kozlowski explained to DrugResearcher.com, over 400 ion channel genes have been identified and their structures are often similar, both within and sometimes even between classes. This makes designing drugs particularly difficult because if they interact with one ion channel, they are likely to interfere with another one too - potentially creating unwanted side effects. To overcome this, Lectus have decided to take a novel approach: instead of targeting the ion channel itself, the company is designing compounds that bind to the channel's accessory proteins. Kozlowski said that these targets are less similar to each other and also "coupling between ion channels and accessory proteins often shows more cell and tissue specificity.""By focussing in on a particular couplet that's found in a particular tissue, a drug is more likely to target that tissue in particular,"​ he said. For example, in urinary incontinence, drugs are traditionally designed to open the potassium channels in the bladder, which are very similar to those in the circulation system and so a common side effect is a drop in blood pressure. However, Lectus hopes that a drug designed by its scientists would only exert an effect in the bladder, leaving other tissue unaffected. In this way, Kozlowski said: "[Lectus drugs] could be significantly better than existing drugs." ​ Using the company's proprietary protein-protein interaction assay, called Leptics, Kozlowski's company is designing compounds to treat pain and urinary incontinence through targeting a member of the KV family of potassium ion channels. Cardiovascular side effects are also common with pain medications that target potassium ion channels, said Kozlowski. In fact, most companies heed the US Food and Drug Administration's 'non binding recommendation' to check potential drugs for ion channel interactions that could lead to potentially fatal side-effects. The channels tested include the hERG potassium channel (named after the Ether-a-go-go gene in fruit flies), which is critical in humans for repolarising the heart and maintaining cardiac rhythm. Blocking the effect of this protein can cause arrhythmia and lead to heart attacks. Lectus has historically been a research organisation but is currently profiling candidate drugs and the Kozlowski's goal for 2007 is to become a research and development company. From there, the company will move to clinical trials as soon as possible and "although it is difficult to predict when, hopefully within the next couple of years,"​ explained Kozlowski. The biotech has a library with over 70,000 small molecules chosen for their diversity - Kozlowski stressed that Lectus don't have a library of typical ion channel modulators as they would target the wrong protein. There are over 30 approved drugs that target ion channels, with many more in development. One example is AstraZeneca's and Abraxis BioScience's marketed pain medication, Naropin (ropivacaine), is a calcium channel blocker that carries a FDA warning on its label regarding a rare risk of heart attacks for cetain uses of the drug. As reported by DrugResearcher.com last month​, Solvay Pharmaceuticals filed Pulzium (tedisamil) with regulators in the US and the European Union. The niche drug is designed to treat atrial fibrillation by blocking multiple potassium channels. Currently Lectus is interested in partnering with other drug developers, both around its technology and its compounds. However, Kozlowski said he is uninterested in fee-for-service deals. Commenting on the innovation award, Jeff Solomon, chief executive of ERBI said: "Working in the field of ion channels is one of the most challenging areas of drug discovery. Lectus impressed the judges because they have successfuly raised finance and grown the business despite the tough commercial conditions which have forced others to down-size."​ Kozlowski said: "We have bucked the trend in funding for early-stage drug development."

Related topics: Preclinical Research

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