Tavaborole, a Novel Boron-Containing Small Molecule for the Topical Treatment of Onychomycosis, Is Noncarcinogenic in 2-Year Carcinogenicity Studies

被引:14
作者
Ciaravino, Vic [1 ]
Coronado, Dina [1 ]
Lanphear, Cheryl [2 ]
Shaikh, Imran [3 ]
Ruddock, William [3 ]
Chanda, Sanjay [1 ]
机构
[1] Anacor Pharmaceut Inc, Palo Alto, CA 94303 USA
[2] MPI Res Inc, Mattawan, MI USA
[3] ITR Labs Canada Inc, Baie Durfe, PQ, Canada
关键词
tavaborole; onychomycosis; antifungal; carcinogenicity; ANTIFUNGAL AGENT; ACIDS;
D O I
10.1177/1091581814545245
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Tavaborole, a cyclized boronic acid, has been approved by the Food and Drug Administration for the topical treatment of toenail onychomycosis. This novel, low-molecular-weight pharmaceutical compound has broad-spectrum antifungal activity against dermatophytes, yeasts, and molds responsible for the disease. Tavaborole was tested in 2-year carcinogenicity studies in mice (once daily dermal administration) and rats (once daily by oral gavage) as part of the extensive nonclinical safety program. There was no evidence of tavaborole-related neoplasms observed in either study. Based on the data gathered from these 2 carcinogenicity studies, tavaborole is considered noncarcinogenic.
引用
收藏
页码:419 / 427
页数:9
相关论文
共 16 条
[1]   Anti-infectives - Recent progress on the topical therapy of onychomycosis [J].
Alley, Michael R. K. ;
Baker, Stephen J. ;
Beutner, Karl R. ;
Plattner, Jacob .
EXPERT OPINION ON INVESTIGATIONAL DRUGS, 2007, 16 (02) :157-167
[2]  
Anacor Pharmaceuticals Inc, 2014, KERYDIN TAV TOP SOL
[3]   Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), for the potential treatment of onychomycosis [J].
Baker, Stephen J. ;
Zhang, Yong-Kang ;
Akama, Tsutomu ;
Lau, Agnes ;
Zhou, Huchen ;
Hernandez, Vincent ;
Mao, Weimin ;
Alley, M. R. K. ;
Sanders, Virginia ;
Plattner, Jacob J. .
JOURNAL OF MEDICINAL CHEMISTRY, 2006, 49 (15) :4447-4450
[4]   Boron-containing inhibitors of synthetases [J].
Baker, Stephen J. ;
Tomsho, John W. ;
Benkovic, Stephen J. .
CHEMICAL SOCIETY REVIEWS, 2011, 40 (08) :4279-4285
[5]  
Draize JH, 1944, J PHARMACOL EXP THER, V82, P377
[6]  
Groziak M P, 2001, Am J Ther, V8, P321, DOI 10.1097/00045391-200109000-00005
[7]  
Janssen, 2001, SPOR PACK INS
[8]   Systemic antifungal agents used to treat onychomycosis [J].
Katz, HI .
JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY, 1998, 38 (05) :S48-S52
[9]   Possible drug interactions in oral treatment of onychomycosis [J].
Katz, HI .
JOURNAL OF THE AMERICAN PODIATRIC MEDICAL ASSOCIATION, 1997, 87 (12) :571-574
[10]  
Novartis Pharmaceuticals Corporation, 2011, LAM PACK INS