The Japanese experiences with hypoxia-targeting pharmacoradiotherapy: from hypoxic cell sensitisers to radiation-activated prodrugs.

摘要: Tumour hypoxia is a negative factor in cancer radiotherapy. In order to overcome the problem, various pharmacotherapies have been investigated as an adjunct The use of hypoxic cell sensitisers classical strategy, and many new compounds developed investigated. Development more efficient than those currently available seems difficult clinical studies prove efficacy existing are encouraged, especially combination with radiosurgery, intraoperative radiotherapy, interstitial irradiation, which single high dose radiation used. Following advent sensitisers, cytotoxins become available. Among them, tirapazamine has already gained success when combined cisplatin non-small lung cancer. beneficial effect needs be determined. As third-generation compound this field, antitumour prodrugs that activated by irradiation under conditions via one-electron reduction proposed. Prodrugs 5-fluorouracil 5-fluoro-2'-deoxyuridine shown vivo well vitro activity. Although evaluation not warranted due relatively low effect, strategy appears promising if prodrug design can applied potent agents shall future.