The Discovery and Profile of Fluconazole

This paper was presented at the 16th National Congress of Chemotherapy, Florence, Italy, March 1988.

Summary

Fluconazole is a bis-triazolyl, difluorophenyl propyl alcohol derivative being developed for treatment of life-threatening and superficial fungal infections. The presence of a triazole and a difluorophenyl produces potent antifungal activity but replacement of the usual imidazole group by triazole leads to improved selectivity. Fluconazole is much less lipophilic than other azole antifungals and this leads to excellent penetration throughout the body, low protein-binding and water-solubility. Fluconazole is stable to metabolism resulting in excellent oral absorption and a long half-life. These properties have resulted in excellent efficacy and safety in a wide range of clinical situations.

Key words:

• triazole
• antifungal
• lipophilicity
• metabolic-stability
• clinical efficacy

Notes

This paper was presented at the 16th National Congress of Chemotherapy, Florence, Italy, March 1988.