Activity of SQ641, a capuramycin analog, in a murine model of tuberculosis.
New delivery vehicles and routes of delivery were developed for the capuramycin analogue SQ641. While this compound has remarkable in vitro potency against Mycobacterium tuberculosis, it has low solubility in water and poor intracellular activity. We demonstrate here that SQ641 dissolved in the water-soluble vitamin E analogue alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS) or incorporated into TPGS-micelles has significant activity in a mouse model of tuberculosis.
Nikonenko
Boris V
BV
Sequella, Inc., 9610 Medical Center Drive, Rockville, MD 20852, USA. borisnikonenko@sequella.com
Reddy
Venkata M
VM
Protopopova
Marina
M
Bogatcheva
Elena
E
Einck
Leo
L
Nacy
Carol A
CA
D000617:Aminoglycosides / Q000737:chemistry / Q000627:therapeutic use*; D000818:Animals; D000995:Antitubercular Agents / Q000737:chemistry / Q000627:therapeutic use*; D004195:Disease Models, Animal; D005260:Female; D051379:Mice; D008810:Mice, Inbred C57BL; D009169:Mycobacterium tuberculosis / Q000187:drug effects / Q000502:physiology*; D012995:Solubility; D014376:Tuberculosis / Q000188:drug therapy*; D014810:Vitamin E / Q000737:chemistry
D000617:Aminoglycosides; D000995:Antitubercular Agents; C049983:capuramycin; D014810:Vitamin E; C014225:tocophersolan