Infectious diseases have recently attracted considerable attention on the LeadDiscovery website. This is because the anti-infectives market is poised to experience considerable growth in the next few years, with a forecast market value that is expected to double in size to more than $44 billion by 2010. Fungal infection is particularly in need of new treatments since there is not a single rapidly fungicidal, non-toxic drug available. Against this need is an increasing market. During the 1990's, the US systemic antifungal market has grown 25% per year. Infections due to Candida account for about 80% of all major systemic fungal infections, and candida is now the fourth most prevalent organism found in bloodstream infections and is the most common cause of fungal infections in immunocompromised people. The frequency of nosocomial candidiasis has risen at least five-fold in the 1980s, making it one of the most common hospital-acquired infections. Although often a benign, self-limited problem, it may be associated with excess mortality of greater than 40% due to the development of candidiasis. The estimated health care cost of an episode of care for candidemia has been estimated to approximately $35,000 per Medicare patient. With roughly 30,000 patients falling victim to Candida nosocomial bloodstream infections per year, annual costs for just candidemia exceed $1bn.

The need for improved treatments of candidiasis has driven the development of a wealth of new targets and drug discovery platforms in antifungal R&D. As a result of these advances, the next generation of triazoles antifungals has emerged. This therapeutic class is reviewed in a further report highlight by us (click here to access). One molecule that receives special attention is CS-758. This novel triazole has been recently evaluated against experimental murine oropharyngeal candidiasis induced by Candida albicans with various susceptibilities to fluconazole. CS-758 exhibited potent in vitro activity against the strains used in this murine model including fluconazole-susceptible and fluconazole-resistant strains. CS-758 exhibited excellent efficacy against the infections induced by all the strains including a fluconazole-resistant strain. These results suggest that CS-758 is a promising compound for the treatment of oropharyngeal candidiasis including fluconazole-refractory infections.

Entry date February, 2003

Adapted from Kamai et al, Antimicrob Agents Chemother 2003 Feb;47(2):601-6.

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