キノロン薬開発の歴史と評価

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  • History and review of the development of quinolone antibiotics.

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Since its establishment in 1946, the Japanese Society of Chemotherapy (JSC) has contributed greatly to encouraging research and progress in chemotherapy through extensive exchange and dissemination of information in the field. One such activity in which the JSC has been and currently is involved is the development of synthetic antibacterial agents from nalidixic acid and pipemidic acid, leading to new quinolones. In 1962, nalidixic acid, the first agent of what to day are referred to as old quinolones, was discovered as an antibibacterial active against gram-negative bacteria. Since then, a series of old quinolones have been developed, but they have certain drawbacks, such as narrow antibiotic spectra, low recovery in urine, and relatively easy biotransformation. Subsequent work led to the birth of a new era with the introduction of norfloxacin as the first new quinolone in Japan in 1984 and then in many other countries throughout the world. This particular agent features clear differences from old quinolones in structure and activity, including the introduction of a fluorine atom into the prototype nucleus, resulting in much more potent antibacterial activity against gram-negative bacteria and a broad antibacterial spectrum covering even gram-positive bacteria. These features have led to extended indications for norfloxacin, to upper respiratory tract infections and superficial suppurative diseases, in addition to those of the old quinolones, urinary tract infections, intestinal infections, and otorhinological infections. Based on clinical studies planned and organized by JSC, a number of new quinolones have subsequently been developed, including ofloxacin. However, no drugs other than norfloxacin have yet been approved for pediatric use. The adverse reaction of arthropathy (joint and cartilage damage) predicted from studies in young animals have never materialized in clinical use. However, unexpected reactions, such as CNS reactions and phototoxicity, have been reported in clinical studies or post-marketing surveillance of the new quinolones. In this context, a newer quinolone, gatifloxacin is expected to reduce phototoxicity on the basis of recent studies. The JSC should continue to provide improved chemotherapeutic treatments required by our patients in the coming millennium through better understanding and public education in regard to infectious diseases as well as developing promising antibacterial agents, and for this same purpose, the JSC should also continue its extensive activities, including journal publishing, conferences and workshops, and interdisciplinary studies with related societies.

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