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Antimicrobial Agents and Chemotherapy, June 2007, p. 1956-1961, Vol. 51, No. 6
0066-4804/07/$08.00+0     doi:10.1128/AAC.00062-07
Copyright © 2007, American Society for Microbiology. All Rights Reserved.

Antipropionibacterial Activity of BAL19403, a Novel Macrolide Antibiotic{triangledown}

Stefanie Heller, Laurenz Kellenberger, and Stuart Shapiro*

Basilea Pharmaceutica AG, Basel, Switzerland

Received 16 January 2007/ Returned for modification 18 February 2007/ Accepted 15 March 2007

BAL19403 exemplifies a new family of macrolide antibiotics with excellent in vitro activity against propionibacteria. MICs indicated that BAL19403 was very active against erythromycin-resistant and clindamycin-resistant propionibacteria with mutations in the region from positions 2057 to 2059 (Escherichia coli numbering) of the 23S rRNA, although it is less active against those rare clinical isolates in which a methyltransferase, ErmX, confers macrolide and lincosamide resistance by dimethylation of the adenine moiety at position 2058. BAL19403 was predominantly bacteriostatic toward the propionibacteria, and population analyses indicated resistance selection frequencies for BAL19403 and the comparator drugs (erythromycin, clindamycin) in the range 10–8 to 10–9 for cutaneous propionibacteria with diverse antibiotic resistance profiles. On the basis of its antipropionibacterial activity and its high anti-inflammatory activity, BAL19403 represents a promising topical treatment for mild to moderate inflammatory acne vulgaris.

* Corresponding author. Mailing address: Microbiological Research, Basilea Pharmaceutica AG, Grenzacherstrasse 487, Postfach, CH-4005 Basel, Switzerland. Phone: (41 61) 606 13 49. Fax: (41 61) 606 11 12. E-mail: shapiro.stuart{at}basileapharma.com

{triangledown} Published ahead of print on 26 March 2007.

Antimicrobial Agents and Chemotherapy, June 2007, p. 1956-1961, Vol. 51, No. 6
0066-4804/07/$08.00+0     doi:10.1128/AAC.00062-07
Copyright © 2007, American Society for Microbiology. All Rights Reserved.



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