ED drug in oral trial

Surface Logix has commenced a company-sponsored Phase I clinical trial for SLx-2101, a novel, selective, oral PDE -5 inhibitor being evaluated for the treatment of cardiovascular diseases, including endothelial dysfunction and erectile dysfunction.

The Phase I study is a single centre, randomised, double-blind study designed to evaluate the safety, tolerability, pharmacokinetic and pharmacodynamic effects of orally administered SLx-2101 in healthy male subjects.

'This study will assess the safety and tolerability of SLx-2101 and will provide significant information on the potency and duration of action of SLx-2101 across a range of doses. We also hope to establish a preliminary indication of efficacy in established models of endothelial function. Both peripheral arterial tone and erectile function are being evaluated utilising two non-invasive methods of assessing endothelial function in healthy humans in this study,' notes Dr William Prince, chief development officer. 'Although the Phase I study has just started, the first PK results look quite promising. Even at a dose of 5mg, we can detect a substantial amount of drug in the blood past 36 hours,' adds Dr. Prince.

'The initiation of human clinical studies on our first drug candidate is an important milestone for Surface Logix. SLx-2101, one of a series of novel PDE -5 inhibitors, represents the power of our core capabilities to build better drugs that address large markets,' said Jim Mahoney, chief executive officer of Surface Logix. 'We are looking forward to seeing the results of this trial, as the data should enable us to simplify, direct and accelerate the next steps in our clinical program towards large market indications associated with endothelial dysfunction.'

'The currently marketed PDE 5 inhibitors have shown limited degrees of efficacy towards cardiovascular diseases primarily due to not having the right combination of potency and duration of action,' notes Dr Paul Sweetnam, chief scientific officer. 'As demonstrated in numerous preclinical animal models, SLx-2101 is a highly potent and selective compound with rapid cellular and tissue response and an extended duration of action. Our chemistry-based Pharmacomer technology platform permits us to access untapped chemistry space and to bring new functionality to medicinal chemistry. It has allowed us to develop a PDE -5 inhibitor program quite rapidly, from conception to first molecule into the clinic in less than two years,' adds Dr Sweetnam.

About SLx-2101 and endothelial dysfunction

SLx-2101 is an oral phosphodiesterase-5 (PDE-5) inhibitor designed using Surface Logix" proprietary small molecule Pharmacomer Technology. It is being developed to treat endothelial dysfunction, a physiological disability of endothelial cells, the cells that line the inner surface of all blood vessels, arteries and veins, that prevents them from carrying out their normal biochemical functions. Normal endothelial cells are involved in mediating the processes of coagulation, platelet adhesion, immune function, control of volume and electrolyte content of the intravascular and extravascular spaces. Endothelial dysfunction is believed to be the underlying cause for several major diseases including atherosclerosis, congestive heart failure, hypertension and erectile dysfunction.

Pharmacomer technology platform

Pharmacomers are unique, small molecule functional groups (< 150 MW) that improve the pharmacokinetic (PK) and/or pharmacodynamic (PD) profile of drugs and drug-like molecules. They are designed using a set of proprietary assays, indices and correlations based on principles from physical chemistry (The Pharmacomer Technology Platform). Using this platform, our scientists can optimise the PK/PD properties of a drug by applying basic principles that govern the interaction of small molecules at the molecular level.