Kaken’s drug discovery research focuses on such areas of strength as inflammation, immunity and allergies, in addition to its core competence of fungal infection disease. We invest substantial financial and human resources into such research activities with the aim of developing new drugs that are both effective and safe. To create new drugs that can compete in the world market, we maintain an active program of drug discovery research, spearheaded by outstanding research professionals and techniques refined over many years of experience in pharmaceutical development.
| Fiblast® Spray, a medicinal product of regenerative medicine, is the world's first product that commercializes recombinant human basic Fibroblast Growth Factor (bFGF), a member of the fibroblast growth factor family. bFGF exists in almost all tissues in the human body. Once a tissue is damaged by trauma, ischemia, etc., bFGF is released from the extracellular matrix and then acts on various cells and tissues to stimulate tissue regeneration. As bFGF has diverse functions, bFGF is characterized by its powerful abilities to stimulate both cellular proliferation and neovascularization. After obtaining exclusive licensing rights for recombinant human bFGF in Asia from Scios Inc. (U.S.) in 1988, Kaken continued its R&D efforts toward acquisition of marketing approval for the bFGF product with indications for pressure ulcers and other skin ulcers (burn ulcers and leg ulcers) and successfully introduced it under the trade name of Fiblast® Spray on the Japanese market in June 2001, marking the world's first commercialization of recombinant human bFGF. Having completed reexamination by the Japanese regulatory authorities in 2010, Fiblast® Spray has again confirmed its presence as a highly reliable drug.
In addition to its effectiveness in skin tissues, bFGF has also demonstrated the ability to stimulate the proliferation and regeneration of periodontal and bone tissues. In the field of dentistry, it has been confirmed that bFGF promotes proliferation of periodontal ligament cells and regeneration of cementum and alveolar bone. We have conducted three clinical trials in patients with periodontitis and found that bFGF is effective in regeneration of alveolar bone destroyed by periodontitis. In regard to bone tissue, bFGF has demonstrated its effectiveness in treating bone fractures by accelerating bone metabolism through both the direct effect of stimulating proliferation of osteoblast and the indirect effect of enhancing osteoclast function. Having completed two clinical trials, we are currently preparing for the next phase of development.
In addition to the fields in which we have conducted clinical trials, we are collaborating with universities and research institutions in Japan to further explore the possibilities of bFGF as a regenerative medicine in other fields.
In March 2005, Kaken acquired the worldwide rights to develop, manufacture and market bFGF. In December 2005, a license agreement was concluded with a Chinese pharmaceutical company for the development and marketing of Fiblast® Spray. In June 2007, a license agreement was reached with SUNSTAR INC. regarding the development and marketing of bFGF for dental applications in Europe and North America. In November 2009, a license agreement was concluded with OLYMPUS CORPORATION for the development and marketing of bFGF for wound healing in Europe and North America.
In collaboration with our overseas business partners, we will strive to increase the presence of bFGF on the global medical market by fully utilizing the wealth of technologies and expertise we have accumulated with regard to bFGF through our R&D efforts.
| The drug candidate KP-103 (efinaconazole), which was discovered through the outstanding antifungal research at Kaken, has the potential to be the world's first triazole compound for a topical medication for onychomycosis. This drug has high antifungal activity and is effective against a wide spectrum of fungi. Also, compared to other existing antifungal agents, its activity decreased only slightly even in the presence of keratin, the main component of nails. This means that the drug has superior nail penetrating properties, thereby suggesting that it will maintain its therapeutic effect in nails thickened by fungal infection or on the underside of such nails. KP-103 has also shown antifungal activity in various animal models of infections and, in particular, greater effectiveness than other treatment options in a guinea pig model for onychomycosis. While oral medications are currently taken as a standard therapy for patients suffering from persistent onychomycosis, KP-103 shows promise as a new treatment option by its featured topical approach.
In 2006, Kaken concluded a licensing agreement with Dow Pharmaceutical Sciences, Inc. (DPS), of the United States, for the development and marketing of KP-103 products in Europe and the Americas. After the acquisition of DPS in 2009 by Valeant Pharmaceuticals International, Inc., of Canada, Valeant has continued the joint development activities with Kaken. In two multinational pivotal studies (Phase III) in patients with mild to moderate onychomycosis of the toenails, this topical investigational drug (US development code: IDP-108) was found to be statistically superior to a placebo for all primary and secondary endpoints. The efficacy of this drug is competitive when compared to that of existing oral medications, and it has thus demonstrated its efficacy as a topical agent with fewer side effects.
In 2012, Kaken applied for marketing authorization for KP-103 in Japan, and the application is currently under investigation. We expect that the drug will receive approval in 2014, making it Japan's first topical medication for onychomycosis, and we are currently responding to investigations and preparing to market the drug accordingly. Valeant also submitted a marketing authorization application for this drug in the United States and Canada during 2012.
We will continue our efforts with overseas partners to acquire approval of this drug as a treatment for onychomycosis in the global market.