Document Detail

Therapeutic efficacy of benzoxazinorifamycin, KRM-1648, in combination with other antimicrobials against Mycobacterium leprae infection induced in nude mice.
MedLine Citation:
PMID:  8189088     Owner:  NLM     Status:  MEDLINE    
In this study, the in vitro and in vivo anti-Mycobacterium leprae activity of the newly developed benzoxazinorifamycin, KRM-1648, in combination with clofazimine (CFZ) or dapsone (DDS) was evaluated. In vitro anti-M. leprae activities of KRM-1648, CFZ, and DDS along with their combinations were measured by the BACTEC 460 TB System. KRM-1648 (0.01 microgram/ml), CFZ (0.5 microgram/ml), and DDS (2.0 micrograms/ml exhibited a significant anti-M. leprae activity, reducing growth index (GI) values by 78%, 30%, and 35% by day 18, respectively. Combinations of KRM-1648 with either CFZ or DDS, or both caused only a slight increase in the efficacy. BALB/c nude mice infected subcutaneously with 1 x 10(6) of M. leprae Thai-53 strain and test drugs were given to mice by gavage once daily six times per week for up to 50 days, from day 31 to day 80. Animals were observed for the growth of organisms in the hindfoot pad during the 12 months following infection. KRM-1648 given at the dose of 0.001 mg/mouse exhibited potent antileprosy activity. KRM-1648 exhibited a significant combined effect with either CFZ or DDS, or both against M. leprae infection, except that there was no significant difference in efficacy between KRM-1648 + CFZ and CFZ alone. Furthermore, the efficacy was most increased in the three-drug regimen KRM-1648 + CFZ + DDS.
H Saito; H Tomioka; K Sato; S Dekio
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.    
Journal Detail:
Title:  International journal of leprosy and other mycobacterial diseases : official organ of the International Leprosy Association     Volume:  62     ISSN:  0148-916X     ISO Abbreviation:  Int. J. Lepr. Other Mycobact. Dis.     Publication Date:  1994 Mar 
Date Detail:
Created Date:  1994-06-21     Completed Date:  1994-06-21     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  8505819     Medline TA:  Int J Lepr Other Mycobact Dis     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  43-7     Citation Subset:  IM    
Department of Microbiology and Immunology, Shimane Medical University, Izumo, Japan.
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MeSH Terms
Clofazimine / administration & dosage*
Dapsone / administration & dosage*
Drug Therapy, Combination
Leprostatic Agents / administration & dosage*
Leprosy / drug therapy*
Mice, Inbred BALB C
Mice, Nude
Rifamycins / administration & dosage*
Reg. No./Substance:
0/Leprostatic Agents; 0/Rifamycins; 129791-92-0/KRM 1648; 2030-63-9/Clofazimine; 80-08-0/Dapsone

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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