Antibacterial Research: Aquapharm announces discovery of novel antibiotic compound
Released: Thursday 9th August 2012
Scottish biotechnology company Aquapharm Biodiscovery has discovered a novel antibiotic compound with potent activity against a broad spectrum of multi-drug-resistant Gram-positive bacteria.
The compound, which demonstrates bactericidal potency against Multi Drug Resistant Staphylococcus Aureus (MDRSA) and Multi Drug Resistant Streptococcus Pneumoniae (MDRSP), Clostridium Difficile and Enteroccocus Faecalis which are common causes of death in patients in hospital care units is the company’s first new drug-lead with confirmed in vivo efficacy and commercial potential.
Aquapharm’s ‘AQP-182’ is one of the novel drug-like molecules identified by Aquapharm from its collection of more than 10,000 marine micro-organisms.
The firm has screened a fraction of its collection against selected anti-infective and anti-inflammatory targets, and has already identified 16 molecules of interest.
These include five novel antibiotic compounds comprising two distinct chemical scaffolds that are currently in preclinical development at Aquapharm for the treatment of bacterial infections resistant to existing therapies.
The most advanced of these molecules, according to Aquapharm’s Chief Scientific Officer Dr Tim Morley, is AQP-182 due to its potent activity against multi-drug resistant Gram-positive bacteria with in-vitro minimum-inhibitory-concentrations (MICs) against MDRSA below 0.016ug/ml.
He said: “We are very excited with the diversity of novel chemical scaffolds produced from our drug discovery platform based on marine microorganisms. From only a small portion of our natural product library we have identified 16 novel compounds belonging to totally novel and diverse chemical classes.
“The most advanced compound AQP-182 has a promising pharmacological and pharmacokinetic profile essential for the treatment of drug-resistant gram-positive bacterial infections”.
In-vivo efficacy studies have confirmed greater potency than the current ‘best in class’ drug against MDRSA in murine sepsis and thigh models. Its pharmacokinetic profile and high potency suggest it could have the potential for once-a-day dosing.
Aquapharm expects initiation of a Phase I clinical trial in the second half of 2013. The promising data on AQP-182 is expected to accelerate Aquapharm’s first commercial partnering deal later in the year, building on strong indicative interest from a number of major pharmaceutical and biotechnology companies.
Notes to Editors
DRUG RESISTANT GRAM POSITIVE INFECTIONS: SCALE & IMPACT
Antibiotic resistance is a huge concern with the UK Department of Health describing it as one of the most significant threats to patient safety in Europe. With few antibiotics in the development pipeline and a growing resistance to bacteria it is becoming increasingly more challenging to tackle. The UK is signed up to the World Health Organisation European Strategic Action Plan on Antibiotic Resistance. This action plan encourages information sharing and development of effective interventions to prevent and slow the development of multi-drug resistance bacteria. Find out more at: http://www.dh.gov.uk/health/2012/02/antibiotic-resistance-key-facts
A joint working group of the European Centre for Disease Control and the European Medicines Agency was established in 2008 to document the gap between infections caused by multi-drug resistant bacteria in the EU and the development of new antibiotics to treat them. For more on the report and its findings visit: http://www.dh.gov.uk/en/Publicationsandstatistics/Publications/PublicationsPolicyAndGuidance/DH_130267
About Aquapharm Biodiscovery Ltd.
Aquapharm Biodiscovery Limited is a biopharmaceutical company focused on discovery and development of novel and commercially valuable products derived from marine microbiology.
The company's discovery process combines microbiology, screening and natural product chemistry to provide a robust platform for the discovery of novel compounds including small molecules, peptides and larger molecules with a wide range of structural diversity, functional complexity and unique molecular architectures amenable to therapeutic areas of difficult to target protein-protein interaction and for future use as anti-inflammatory, tissue-protective and antibiotic drugs.
Aquapharm uses a range of induction technologies and culturing methodologies, including its proprietary screening technology, SeaRch™, to generate the full spectrum of pharmacologically active compounds that the marine microorganisms in its collection can produce. These technologies unlock cryptic pathways revealing a wider array of metabolites of interest than has traditionally been possible with ordinary saline fermentation.
Marine natural products are a rich new source of pharmaceutical chemistry; not only have natural products been the source of or the inspiration for over 75% of the new small-molecule chemical entities introduced as pharmaceuticals over the past 50 years, they remain a fundamental source of new chemical diversity and an integral component of modern science's pharmaceutical armoury.
Aquapharm Biodiscovery’s core focus is the development of new pharmaceuticals from its marine microbial collection using its SeaRch™ technology to address areas of high unmet medical need, in particular Gram negative and Gram positive antibiotics. Aquapharm's preclinical portfolio also includes Gram negative compounds and compounds with dual anti-oxidant and anti-inflammatory potency that stimulate the natural oxidant defence mechanisms targeting diseases such as Multiple Sclerosis.
The company is based at the European Centre for Marine Biotechnology in Oban, and Heriot-Watt University Research Park, Edinburgh
For more information, please see www.aquapharm.co.uk
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