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KDDF-201112-02 Clinical development of novel Oxazolidinone antibiotics LCB01-0371(Infectious Diseases, Chemical) [01.04.2013]


Development and Market Objectives

■  To complete Phase 1 study for a new oral oxazolidinone (LCB01-0371), for the treatment of Methicillin-resistant Staphylococcus Aureus (MRSA) and Vancomycin-Resistant Enterococci (VRE) infections.

■  To develop an intravenous (IV) formulation and license to global pharmaceutical companies following Phase 2a clinical studies


Unmet Medical Need & Target Patients

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Since it was first discovered in the 1960s, the increase in methicillin resistance in the human pathogen S. aureus (known as MRSA) has increased sharply from 2% of cases in 1974, to 22% in 1995 and 50% in 1997. According to the US Center for Disease Control, 94,000 patients were infected with MRSA in 2005, of which 19,000 died. In 2009, there were 1.10 million reported cases of MRSA infection in seven main countries around world, including 738,000 in the US alone.
As bacterial resistance to antibiotics like methicillin increases, the need to develop more effective treatments has become a global health challenge. The IDSA (Infectious Diseases Society of America) is currently engaged in a campaign to secure 10 new antibiotics by the year 2020. A portion of this campaign is aimed at lobbying for government support to ease FDA regulations, with the ECDC (European Centre for Disease Prevention and Control) in agreement 

MRSA, VRSA (Vancomycin-resistant Staphylococcus aureus) and VRE are a series of multi-drug resistant strains which exhibit resistance to most first-line antibiotics, including beta-lactams and quinolones. For highly resistant bacterial strains, the only existing treatments are Vancomycin, Zyvox, Cubicin and Synercid, and the only oral medicine is Zyvox. However, Zyvox cannot be used for more than two weeks due to side-effects of marrow toxicity, while Cubicin exhibits low efficacy toward infections of the respiratory tract and causes side-effects in skeletal muscle.
A number of pharmaceutical companies have attempted to develop new antibiotics that can overcome the side-effects and disadvantages of Zyvox, but as yet there have been no significant breakthroughs. Two Oxazolidinone candidates have entered the clinical stage, but have failed to show distinctive improvements in safety. Therefore, the development of a second generation antibiotic that can overcome the disadvantages of Zyvox with rapid efficacy and minimal side-effects has the potential to become a blockbuster product. 



LCB01-0371 has completed a Phase I SAD (Single Ascending Dose) clinical trial in healthy adults and is currently undergoing a Phase I MAD (Multiple Ascending Dose) clinical trial in healthy adults in Korea.

Intellectual Property

Substance and process patents for the current development of LCB01-0371 are registered as follows: 
[Patent status of Oxazolodinone antibiotics]

NO. Name of intellectual property Index Day of Application
Country of Application Application number
1 Novel Oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone and Pharmaceutical Compositions thereof Domestic 2008/09/24
Korea 10-2008-0093712
PCT 2009/09/22 PCT PCT/KR2009/005376
Overseas 2011/03/23 1. USA 13/120,568
2011/03/18 2. Japan 2011-527752
2011/03/24 3. China 200980137678.1
2011/03/07 4. India 435/MUMNP/2011
2011/03/09 5. Canada 2,737,299
2011/03/24 6. Australia 2009297294
2011/03/23 7. Brazil 201127596
2011/04/22 8. Russia 2011116164
2011/03/23 9. Mexico MX/a/2011/003118
2011/03/11 10. South Africa 2011/01894
2011/03/24 11. Europe 09 816 393.4
Method for preparing of (R)-3-(3-fluoro-4-(1-methyl-5,6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl)oxazolidin-2-one derivatives
Domestic 2010/03/08
Korea 10-2010-0020525
PCT 2011/03/08 PCT PCT/KR2011/001579
Overseas 2012/09/07 1. USA 13/583,492
2012/09/03 2. India 2091/MUMNP/2012
2012/09/13 3. China (TBA)

Competitive Advantages

■ Significant problems exist with current Oxazolidinone antibiotics: There is a need to improve the time course of myelosuppression and solubility.
Linezolid (Zyvox®) is an oxazolidinone antibiotic marketed by Pfizer since 2000, and has maintained its position in the spotlight as the first member of a new class of antibiotics in over 35 years. However, it cannot be injected during long term treatment using a time course approach for myelosuppression, and can only be used by infusion injection due to low solubility.

■ The distinct advantages of our current candidate can be divided broadly into five features:

1) Excellent safety: Can be injected long-term for short time courses of myelosuppression.
2) Superior effect: Exhibits superior effects in animal tests and is effective against some strains of gram negative bacillus.
3) Improved solubility: Can be used both orally and through injection, due to excellent water-solubility.
4) Excellent pharmacodynamics: Exhibits long post-antibiotic effects for extended efficacy duration.
5) Possibility to expand indications into multiple-resistance tuberculosis treatments (MDR-TB) with distinct safety advantages: Exhibits excellent effects against multiple-resistance tubercle bacillus. 30-day injection periods in animal testing showed the resultant concentration of tuberculosis bacilli to be 50 times lower than that achieved by Linezolid, with sterilizing power 4 times higher (MBC 99).


Methicillin-resistant Staphylococcus Aureus(MRSA), Vancomycin-Resistant Enterococci(VRE) infections.

Research Period

Feb.29,2012 ~ Oct.31,2013


LegoChem Biosciences, Inc.

Developmental Stage

Phase 1 clinical trial

Additional Information

Contact Information

Address Company Name: Legochem
WebSite Homepage: Contact Person: Ye Na Park/ Executive Management Team/Staff
E-mail: Contact: 042-861-0688

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