Novel lead series of pan-metallo beta-lactamase inhibitors identified

HARLOW, UK and LABEGE, France I March 10, 2014 I Argenta, a Galapagos NV (Euronext: GLPG) company that provides drug discovery services from target validation to proof of concept, announced today that it has achieved a milestone with its collaboration partner Antabio in an anti-bacterial drug discovery project funded by the Wellcome Trust. The attainment of the milestone triggers the drawdown of a further €1.7 million tranche of their Seeding Drug Discovery Award.

A novel lead series of pan-metallo beta-lactamase inhibitors has been identified that, in combination with carbapenems, restores antibacterial activity against life-threatening clinical isolates whilst exhibiting no toxicity or developmental issues. Multi-drug resistant Gram-negative bacteria account for most hospital infections worldwide, causing up to 75,000 deaths yearly and extra healthcare costs/productivity losses of >€1.5 billion. One of the most effective treatments is the use of carbapenem antibiotics; however, the usefulness of these antibiotics is becoming increasingly compromised due to the rise of clinical resistance, associated with the spread of genes encoding various MBL enzymes, primarily the carbapenemases of the NDM, VIM and IMP types.

The Argenta/Antabio collaboration began in February 2013, when the Wellcome Trust awarded Antabio €4.7 Million to fund the discovery of a novel, safe and efficacious pan-inhibitor of bacterial metallo beta-lactamases (MBLs). Since then, Argenta has provided medicinal chemistry, computer-aided drug design and ADME/PK services, together with its integrated drug discovery expertise, to assist Antabio achieve its research goals.

“To have achieved on schedule our first milestone in our collaboration with the Trust is a great satisfaction for our team, and a sign that solid foundations are in place for this discovery programme.” said Marc Lemonnier, CEO of Antabio. “We believe the therapeutic potential of a small-molecule pan-MBL inhibitor is very significant and will eventually improve the outcome for patients suffering from severe nosocomial Gram-negative infections. This milestone will support further lead optimization efforts to progress our compounds rapidly towards pre-clinical candidate nomination.”

John Montana, Argenta’s Managing Director, added “We are delighted to have achieved this milestone with our collaboration partner, Antabio, and look forward to our continuing partnership on this exciting drug discovery project. Once again, this achievement underlines Argenta’s ability to deliver high quality science within exacting deadlines.”

About Argenta

Argenta is a fully-integrated drug discovery services provider and a trusted partner for many world-leading pharmaceutical and biotechnology companies including AstraZeneca, Genentech, Janssen and Zafgen.

Argenta combines a comprehensive range of discovery services with multiple disease area expertise including respiratory, oncology, pain and inflammatory disease, providing a compelling combination of scientific excellence, a full in vitro and in vivo pharmacology and DMPK capability, cutting edge medicinal chemistry thinking and cost-effectiveness.

Argenta provides fully-integrated and stand-alone services from target validation through to development candidate nomination and has built an industry-leading track record of delivering development compounds, averaging over three development compounds per year.

Founded in 2000, Argenta currently employs over 160 scientists in the UK with an average of 17 years’ pharmaceutical drug discovery expertise. Argenta has delivered 40 development candidates in 13 years, and greater than 85% of the Company’s contract research is repeat business. More information at: www.argentadiscovery.com.

About ANTABIO

ANTABIO is a France-based start-up biopharmaceutical company, situated at Labège near Toulouse, dedicated to the discovery of first-in-class small molecule compounds to treat severe hospital- and community-acquired infections caused by multi- and pan-drug resistant bacterial pathogens. Based on its patented technology and unique antibacterial discovery know-how, ANTABIO is committed to developing strong partnerships to advance novel drugs that will offer a synergistic solution to the shortfall of the current antibacterial arsenal. More information at: www.antabio.com.

About the Wellcome Trust

The Wellcome Trust is a global charitable foundation dedicated to achieving extraordinary improvements in human and animal health. It supports the brightest minds in biomedical research and the medical humanities. The Trust’s breadth of support includes public engagement, education and the application of research to improve health. It is independent of both political and commercial interests. www.wellcome.ac.uk.

SOURCE: Argenta