CG400549 would be a potential first-in-class antibiotic targeting ENR (Enoyl-acyl carrier protein reductase) as CG400549 has a novel chemical structure which has never been used as an antibacterial agent previously. It is being developed to target the notorious resistant bacterial strains including MRSA (Methicillin Resistant Staphylococcus aureus) and VRSA (Vancomycin Resistant Staphylococcus aureus), or commonly referred to as the "Superbugs." This compound interrupts fatty acid synthesis process that is unique in bacteria and seems to be an excellent drug candidate for the treatment of the "Superbugs." CG400549 is currently in Phase I study (in Europe).
Background and unmet needs
Antibacterial resistance is a serious global issue and therefore, the world demand for antibiotics remains high due to escalating bacterial resistance and the increased risk of serious infections. According to the Global burden of disease and risk factors (World Bank Publications), infectious diseases are one of the leading causes of death worldwide, resulting in more than 10 million deaths each year and antibacterial resistance is largely responsible for this staggering number.
As reported by the Infectious Diseases Society of America (IDSA), there is a high unmet need for novel antibiotics. Despite the alarmingly increasing rate of resistant strains, there have been only five US approvals for new antibacterial agents between 2003 and 2008, of which four agents were considered as non-novel agents. In terms of new antibacterial classes since the 1970's the number is even lower as Oxazolidinones was the only new antibacterial class in more than three decades.
It is believed that market saturation, product restriction and the short acute nature of therapy have all played a role in reducing the incentive for pharmaceutical companies to invest in this therapeutic area. Even the US FDA has publicly stated that "product development in areas crucial to public health goals, such as antibiotics, has slowed significantly during the past decade." The antibiotics market generated sales of USD 42 billion in 2009 globally, representing 46% of sales of anti-infective agents and 5% of the global pharmaceutical market (IMS Health. IMS MIDAS 2009).
Discovery and Achievements
The results of several in vivo and in vitro experiments demonstrated that CG400549 is a promising candidate to potentially become a new class of antibiotics. Recently, clinically isolated MRSA has tendency of multi-drug resistance, whereas CG400549 exhibits excellent inhibitory effect against such multi-drugs resistant bacteria.