Dublin, Ireland, 21 February 2008 - AGI Therapeutics plc (“AGI” or the “Company”) (AIM, IEX: AGI), a speciality pharmaceutical company focused on gastrointestinal drug products, today announces the key findings of a clinical study to assess the pharmacokinetic profile of RezularTM (AGI-003), which is in Phase III clinical trials for the treatment of diarrhoea-predominant irritable bowel syndrome (IBS-D).
The pharmacokinetic study was conducted in healthy human volunteers and compared the drug exposure profile (in terms of both peak plasma concentration, or “Cmax”, and area under the plasma concentration curve, or “AUC”) after administration of 80mg of Rezular, under fed and fasting conditions, to 160mg of a marketed form of racemic verapamil. Rezular contains arverapamil, the purified R-isomer form of verapamil, whereas racemic verapamil contains equal amounts of the R- and the S-isomer.
The key findings of the study were:
(1) There were no detectable levels of the S-isomer following Rezular administration under fasting conditions and thus no evidence of any inter-conversion of Rezular to the S-isomer in vivo. Administration of Rezular under fed conditions resulted in some increase in AUC of the R-isomer compared to fasting conditions, while the S-isomer was only detected in the plasma at trace levels matching the trace amounts known to be present in the purified form of Rezular. These data indicate that the gastrointestinally active R-isomer, arverapamil, contained in Rezular can be administered to humans without exposing them to clinically relevant levels of the S-isomer, the form of verapamil which is most potent on cardiac and vascular tissue; and
(2) Under both fed and fasting conditions, both the Cmax and AUC of the R-isomer after Rezular administration were less than those seen after administration of racemic verapamil. This indicates that patients taking clinically relevant doses of Rezular will be exposed to lower systemic levels of the R-isomer compared to currently approved forms of racemic verapamil, and further supports the NDA 505(b)2-based development approach agreed with the US Food and Drug Administration (FDA) for Rezular.
Commenting on the results, Dr John Devane, CEO of AGI, said:“Verapamil has been on the market in the US for over 20 years, however the presence of the S-isomer does not allow the use of racemic verapamil to safely treat gastrointestinal conditions such as irritable bowel syndrome. We believe that Rezular has important safety benefits in the treatment of gastrointestinal-related disorders. The findings from this pharmacokinetic study further support the safety profile of Rezular and the development strategy being pursued by the Company.”
Contact Information:
AGI Therapeutics plc. Tel: +353 1 449 3254 David Kelly, Chief Financial Officer
Financial Dynamics – UK Tel: +44 (0) 20 7269 7182 Deborah Scott/Lara Mott
Financial Dynamics - Ireland Tel: +353 1 663 3607 Aisling Garvey
Piper Jaffray Limited Neil Mackison Will Carnwath Tel: +44 (0) 20 3142 8700
Davy John Frain Tel: +353 1 614 8761
About AGI Therapeutics plc
AGI is a speciality pharmaceutical company which is focused on the development and commercialisation of differentiated drug products for gastrointestinal (GI) diseases and disorders. AGI’s common shares are listed on the Alternative Investment Market of the London Stock Exchange (AIM) and on the Irish Enterprise Exchange of the Irish Stock Market (IEX) as AGI.
The Company has a portfolio of product candidates derived from its Known Molecular Entity (KME) approach to drug re-profiling and development. KME is a re-profiling methodology used by the Company to identify existing therapeutic drugs which typically have been marketed for a number of years, have established safety profiles and can be developed for new clinical indications or with improved profiles in their existing clinical indications. In this way, the Company seeks to reduce the risk, time and cost of new product development as compared to the development of new chemical entities.
AGI is developing a range of product candidates to treat a variety of prevalent GI diseases and disorders, including irritable bowel syndrome (IBS), dyspepsia, gastroparesis, ulcerative colitis, gastro-esophageal reflux disease (GERD) and diarrhoea-related conditions such as chemotherapy-induced diarrhoea (CID). The Company is targeting areas of the GI therapeutic drug products market for its product candidates where there are currently unmet medical needs or where the effectiveness of existing drug therapies can be further improved.
The Company has five active clinical stage product candidates which are either isomers or new drug delivery formulations of existing approved drugs, and which have established safety and tolerability profiles in their currently approved clinical indications.
For further information please see www.agitherapeutics.com
