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KDDF-201412-14 Development of IV/PO interchangeable antibiotics inhibiting fatty acid biosynthesis for MRSA(Infectious Diseases, Chemical) [09.03.2015]


Development and Market Objectives

The objective is to develop an oral/IV switchable fatty acid biosynthesis inhibitor as a MRSA antibiotic by developing both the intravenous and oral formulations of CG400549, an antibiotic candidate which inhibits Fab I, an enzyme that plays a critical role in bacterial protein synthesis, through completion of phase 1 studies and obtaining phase 2 study approval for both formulations.

Unmet Medical Need & Target Patients

● Despite the fact that development of antibiotics for bacterial infections had made a significant progress, it had been confirmed that the bacteria will eventually develop resistance against specific antibiotics over time. This meant that the development of new antibiotics and the emergence of bacterial strains that are resistant to corresponding antibiotics, was an inevitable cycle that kept repeating itself and therefore, continuous development of novel antibiotics became an absolute requirement for treating bacterial infections.

● The prevalence rate of MRSA infection is rising globally and the reason why this bacterial strain is getting spotlight attention is the fact that it not only has resistance to existing antibiotics but also, it is the most common bacteria that causes hospital-acquired infections and, it could be fatal for the immunocompromised and week/elderly patients.

● Although antibiotics such as vancomycin, linezolid, daptomycin and others are currently available for treating MRSA, these are associated with not only significant adverse events but also, it has been recently been brought to attention that there are also resistance issues with these antibiotics. Therefore, development of new antibiotics with novel structure & target, superb efficacy and excellent safety profile, is needed.


● Using the prototype oral formulation, high safety margin has been secured through single dose and multiple dose (28 days) toxicity studies. Additionally, up to 4~8 fold higher efficacy against currently available competitor products, has been confirmed.

● Safety in humans have been confirmed through phase 1 clinical studies and efficacy in humans have been confirmed in the phase 2a skin infection study conducted in the US where all recruited subjects infected with MRSA were completely cured after receiving CG400549.


● Devising future development plans to reflect the changed clinical study guidelines in accordance with the GAIN Act, a US legislation that went effective in 2013 and, simultaneously preparing a "bridging study" to enable use of the newly developed and improved oral formulation in the next stage.


● In parallel to development of the new oral formulation, development of an injectable formulation for human use has been completed. A focused development is underway as clues to dramatically improve the current injectable formulation, have been found.

Intellectual Property

   - A compound which is effective for inhibiting Fab I, and a method for             treating a bacterial infection.
   - Patent registered in PCT/KR, US, EP, CN, JP, CA and IN.

Competitive Advantages

● The mechanism of action of CG400549 is different from currently available antibiotics and has a novel chemical structure which has never been used as an antibacterial agent previously. New class antibiotic has been a rare occurrence in the field of antibiotic development as Pfizer's Zyvox was the first new class antibiotic in 30 years. CG400549 has demonstrated having the best efficacy when it was evaluated against other MRSA agents recommended by the Infectious Diseases Society of America (IDSA) for testing efficacy in MRSA strains derived from the actual patients. Also, its efficacy in humans was confirmed when 100% of subjects who were enrolled in the phase 2a study, were completely cured from the MRSA infection.

● CG400549 was designed from CrystalGenomics' proprietary structure-based novel drug discovery platform to attack a disease protein which does not exist in humans but critical for the survival of super bacteria. Therefore, since CG400549 is able to eradicate super bacteria while having virtually no affect in humans, its superb safety profile stands out as one of the strongest differentiation attributes compared to other antibiotics. Based on the available clinical data thus far, the usual side effects associated with IDSA recommended MRSA agents which are diverse and serious, have not been observed with CG400549.



Research Period

Aug, 2015 ~ Nov, 2016



Developmental Stage


Additional Information

Contact Information

Address Company Name: CrystalGenomics, Inc.
WebSite Homepage: Contact Person: Kyung-il, Jeong
E-mail: Contact: +82-31-628-2712

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