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US 12,194,105 B2Granted
Composition and method for new antimicrobial agents with secondary mode of action provided by conjugation of an antimicrobial to a guanidinium-rich molecular transporter
AssigneeThe Board of Trustees of the Leland Stanford Junior University
InventorsMelanie Huttner, Paul Wender, Lynette Cegelski, Xiaoyu Zang, Alexandra Antonoplis
Life of this patent
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Abstract
Antibiotic agents conjugated to a guanidinium-rich molecular transporter (GR-MoTr) are provided. The drug conjugates show surprising increases in efficacy compared to the unconjugated drug in difficult-to-treat bacterial infections including biofilms, stationary and persister cells, and multi-drug resistant bacteria, as well as intracellular bacteria.
Claims7
A method of reducing bacterial load, the method comprising
- contacting a bacterial cell population that comprises one or more of:
- persister cells, and MRSA biofilms, with an effective dose non-toxic to human cells of a conjugate comprising an antibiotic selected from vancomycin, oritavancin, and dalbavancin, conjugated at the carboxy terminus directly or through a linker to a guanidinium-rich molecular transporter (GR-MoTr), wherein the GR-MoTr consists of from about 4 to about 9 arginines, which may be L-arginine, D-arginine, or a combination thereof;
- wherein the bacterial cell populations comprises at least 10% of one or more of persister cells, and MRSA biofilm cells.
A method of reducing bacterial load, the method comprising
- contacting a bacterial cell population that comprises Vibrio cholerae with an effective dose non-toxic to human cells of a conjugate comprising vancomycin, oritavancin, or dalbavancin, conjugated directly or through a linker to a guanidinium-rich molecular transporter (GR-MoTr), wherein the GR-MoTr consists of from about 4 to about 9 arginines, which may be L-arginine, D-arginine, or a combination thereof.
Dependencies are inferred from the claim text.