The United States Patent and Trademark Office (USPTO) has granted Addex Therapeutics a composition of matter patent (US Patent 8,344,138) covering ADX71441 and other GABA-B receptor (GABA-BR) positive allosteric modulators (PAM). The claims of the issued patent also cover pharmaceutical composition and method of treatment using such GABA-BR PAMs.

ADX71441 has been shown to be efficacious in a number of preclinical models, including in a validated model of Charcot-Marie-Tooth 1a (CMT1a), a rare hereditary motor and sensory demyelinating peripheral neuropathy.

"We are pleased that our efforts pioneering the field of allosteric modulation are being validated through the broad issuance of composition of matter and methods claims worldwide," said Bharatt Chowrira, CEO at Addex. "Our intellectual property estate continues to yield key patents protecting novel oral small molecules discovered utilizing our allosteric modulation technology platform. In particular, this new patent significantly enhances the value proposition for our ADX71441 programme and we look forward to advancing ADX71441 into phase I in the first half of 2013.”

ADX71441 is a potent, selective, orally available small molecule that is brain penetrant and shows good pharmacokinetic properties for once-daily dosing. Activation of gamma-aminobutyric acid subtype B (GABA-B) receptor, a Family C class of GPCR, is clinically and commercially validated. Generic GABA-B receptor agonist, baclofen, is marketed for spasticity and some spinal cord injuries, and used for overactive bladder (OAB), but is not commonly used due to severe side effects of the drug and rapid clearance. Orthosteric GABA-B receptor agonists have also shown clinical validation in gastroesophageal reflux disease (GERD). Addex' GABA-B receptor PAMs have shown efficacy in multiple preclinical models including: CMT1a, OAB, pain, osteoarthritis pain and anxiety.

Addex Intellectual Property Portfolio includes 12 issued or granted patents and 43 pending patent applications in major pharmaceutical markets around the world. These patents describe and cover composition of matter, pharmaceutical compositions, method of use, formulations and method of manufacture of oral small molecules discovered and developed using Addex' pioneering oral small molecule allosteric modulation technology platform. In addition, these patents cover Addex' powerful biological assay systems important for identifying selective allosteric modulators with high fidelity and success rate.

Addex Therapeutics discovers and develops an emerging class of small molecule drugs, called allosteric modulators, which have the potential to be more specific and confer significant therapeutic advantages over conventional "orthosteric" small molecule or biological drugs.