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Antimicrobial Agents and Chemotherapy, February 2004, p. 388-391, Vol. 48, No. 2
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.2.388-391.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

In Vitro and In Vivo Activities of the Novel Azole Antifungal Agent R126638

F. Odds,1 J. Ausma,2* F. Van Gerven,3 F. Woestenborghs,3 L. Meerpoel,3 J. Heeres,4 H. Vanden Bossche,3 and M. Borgers2

University of Aberdeen, Aberdeen, United Kingdom,1 Barrier Therapeutics N.V., Geel,2 Johnson and Johnson Pharmaceutical Research and Development,3 Centre Molecular Design, a Division of Janssen Pharmaceutica N.V., Beerse, Belgium4

Received 23 July 2003/ Returned for modification 4 September 2003/ Accepted 28 October 2003

R126638 is a new triazole agent with potent antifungal activity in vitro against various dermatophytes, Candida spp., and Malassezia spp. Its activity against Malassezia spp. in vitro was superior to that of ketoconazole, the agent currently used for the treatment of Malassezia-related infections. R126638 showed activity comparable to or lower than that of itraconazole against dermatophytes in vitro; however, in guinea pig models of dermatophyte infections, R126638 given orally consistently showed antifungal activity superior to that of itraconazole, with 50% effective doses (ED50s) three- to more than eightfold lower than those of itraconazole, depending on the time of initiation and the duration of treatment. The ED50 of R126638 in a mouse dermatophytosis model was more than fivefold lower than that of itraconazole. These data indicate that if the effects of R126638 seen when it is used to treat animals can be extrapolated to humans, the novel compound would be expected to show effects at doses lower than those of existing drugs and, hence, present a lower risk for side effects.

* Corresponding author. Mailing address: Barrier Therapeutics N.V., Cipalstraat 3, B-2440 Geel. Belgium. Phone: 32-14-570524. Fax: 32-14-570515. E-mail: jausma{at}barriertherapeutics.com.

Antimicrobial Agents and Chemotherapy, February 2004, p. 388-391, Vol. 48, No. 2
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.2.388-391.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Fernandez-Torres, B., Carrillo-Munoz, A., Inza, I., Guarro, J. (2006). Effect of culture medium on the disk diffusion method for determining antifungal susceptibilities of dermatophytes.. Antimicrob. Agents Chemother. 50: 2222-2224 [Abstract] [Full Text]  
  • Fernandez-Torres, B., Inza, I., Guarro, J. (2005). Evaluation of Disk Diffusion Method for Determining Eberconazole Susceptibility of Dermatophytes and Influence of Culture Medium. Antimicrob. Agents Chemother. 49: 2116-2118 [Abstract] [Full Text]  
  • Vanden Bossche, H., Ausma, J., Bohets, H., Vermuyten, K., Willemsens, G., Marichal, P., Meerpoel, L., Odds, F., Borgers, M. (2004). The Novel Azole R126638 Is a Selective Inhibitor of Ergosterol Synthesis in Candida albicans, Trichophyton spp., and Microsporum canis. Antimicrob. Agents Chemother. 48: 3272-3278 [Abstract] [Full Text]  


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