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Targeted Antimicrobial Drugs For Treatment Of M. Tuberculosis

Larta Institute
posted on 10/10/2007

Technology Description

UCLA Researchers have developed a method of precisely targeting antibiotics to the intracellular site of replication of M. tuberculosis or other similar intracellular pathogens. This is achieved by conjugating antibiotics with transferrin or other ligands that form conjugates with membrane-bound pathogens. These conjugates selectively target infected phagosomes, thus targeting the antibiotic to the pathogen.

UCSD Researchers have developed several novel alkaloids that could serve as lead compounds for the development of antimicrobial drugs for treatment against tuberculosis. These inhibitors target enzyme mycothiol S-conjugate amidase (MCA), a cellular detoxicant in Mycobacterium smegmatis, that are found in pathogenic strains of actinomycetes such as M. tuberculosis, M. avium complex and M. leprae, but is absent in eukaryotes. The combination of these inventions will provide a targeted therapeutic approach to deliver novel drugs to the site of infection.

Technology Background

Antibiotics are used, often in high doses, to combat many infectious diseases. One such disease is tuberculosis, which is becoming more prevalent in our country and worldwide. Tuberculosis is caused by an intracellular pathogen Mycobacterium tuberculosis. No method currently exists to precisely target the intracellular compartment in which the parasites associated with M.tuberculosis and other intracellular pathogens, reside. Typically, parasites in the intracellular compartment, or phagosome, receive a much lower concentration of the antibiotic than what is administered systemically. With no method of targeting antibiotics, relatively high concentrations are required often leading to adverse side effects. Additionally, even these high concentrations are often not adequate to kill the pathogen, particularly those that have developed resistance to current treatment modalities.

Targeted therapeutics allows for a lower systemic dose of the antibiotics while achieving a high concentration at the intracellular site of replication of the pathogen for treatment. Consequently, adverse side effects will be reduced with a more effective killing of the pathogen. The use of the specific targeting molecules and novel inhibitors will allow more effective antimicrobial therapy against certain intracellular parasites such as M. tuberculosis.


• Enhanced therapy for tuberculosis and other intracellular pathogens.
• Reduced dosage of antibiotics for treatment.
• Targeted treatment with sensitive antimicrobials.
• Potentially reduced side effects.

Innovation Details

File Number: B-101 

Other Information:

Intellectual Property:
These technologies are protected by US Patent 6,054,133 and Patent Application WO/02/081483; other rights may also pertain.

Additional Information:
Technology Bundling Project
Funded by Ewing Marion Kauffman Foundation and administered by Larta Institute, the Project’s expert panels examined technologies from 18 Southern California research centers and identified inventions which could be synergistically combined for unique solutions. These Linked-Solutions are now being offered for license, with reduced red tape and “1-stop technology shopping”

IP Protection

Patent Number(s): 6054133

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February 11, 2009

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