Tavaborole, also known as AN-2690 (trade name Kerydin) is a topical antifungal medication for the treatment of onychomycosis, a fungal infection of the nail and nail bed. Tavaborole began its Phase 3 trials in December 2010 and was approved in July 2014. Tavaborole inhibits an essential fungal enzyme, Leucyl-tRNA synthetase, or LeuRS, required for protein synthesis. The inhibition of protein synthesis leads to termination of cell growth and cell death, eliminating the fungal infection. No treatment-related systemic side effects were observed in any of its clinical trials.
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Baker, Stephen J.; Akama, Tsutomu; Alley, Michael Richard Kevin; Benkovic, Stephen J.; Dipierro, Michael; Hernandez, Vincent S.; Hold, Karin M.; Kennedy, Isaac; Likhotvorik, Igor; Mao, Weimin; Maples, Kirk R.; Plattner, Jacob J.; Rock, Fernando; Sanders, Virginia; Stemphoski, Aaron M.; Yiannikouros, George Petros; Zegar, Siead; Zhang, Yong-Kang; Zhou, Huchen. Preparation of boron-containing small molecules and nucleosides for treating fungal infections. Assignee Anacor Pharmaceuticals, Inc., USA. WO 2007078340. (2007).
Baker, Stephen J.; Akama, Tsutomu; Alley, Michael Richard Kevin; Benkovic, Stephen J.; Dipierro, Michael; Hernandez, Vincent S.; Hold, Karin M.; Kennedy, Isaac; Likhotvorik, Igor; Mao, Weimin; Maples, Kirk R.; Plattner, Jacob J.; Rock, Fernando; Sanders, Virginia; Stemphoski, Aaron M.; Yiannikouros, George Petros; Zegar, Siead; Zhang, Yong-Kang; Zhou, Huchen. Preparation of boron-containing small molecules and nucleosides for treating fungal infections. Assignee Anacor Pharmaceuticals, Inc., USA. WO 2007078340. (2007).
Merchant, Rupa Sudhir; Merchant, Aditya Sudhir; Limbad, Piyushkumar Bhikhalal; Pansuriya, Akshay Madhubhai. A novel and improved process for the preparation of tavaborole and its intermediates. Assignee Halcyon Labs Private Limited, India. IN 201721039067. (2019).