Postgraduate Research Institute of Science, Technology, Environment and Medicine, Limassol 3021, Cyprus.
Int J Mol Sci. 2023 Mar 4;24(5):4970. doi: 10.3390/ijms24054970.
The historical insights and background of the discovery, development and clinical use of deferiprone (L1) and the maltol-iron complex, which were discovered over 40 years ago, highlight the difficulties, complexities and efforts in general orphan drug development programs originating from academic centers. Deferiprone is widely used for the removal of excess iron in the treatment of iron overload diseases, but also in many other diseases associated with iron toxicity, as well as the modulation of iron metabolism pathways. The maltol-iron complex is a recently approved drug used for increasing iron intake in the treatment of iron deficiency anemia, a condition affecting one-third to one-quarter of the world's population. Detailed insights into different aspects of drug development associated with L1 and the maltol-iron complex are revealed, including theoretical concepts of invention; drug discovery; new chemical synthesis; in vitro, in vivo and clinical screening; toxicology; pharmacology; and the optimization of dose protocols. The prospects of the application of these two drugs in many other diseases are discussed under the light of competing drugs from other academic and commercial centers and also different regulatory authorities. The underlying scientific and other strategies, as well as the many limitations in the present global scene of pharmaceuticals, are also highlighted, with an emphasis on the priorities for orphan drug and emergency medicine development, including the roles of the academic scientific community, pharmaceutical companies and patient organizations.
具有 40 多年历史的去铁酮(L1)和麦芽酚铁复合物的发现、发展和临床应用的历史见解和背景,突出了源于学术中心的一般孤儿药开发计划的困难、复杂性和努力。去铁酮广泛用于治疗铁过载疾病中过多的铁,也用于许多与铁毒性相关的其他疾病,以及调节铁代谢途径。麦芽酚铁复合物是最近批准的用于增加铁摄入以治疗缺铁性贫血的药物,这种疾病影响世界上三分之一到四分之一的人口。揭示了与 L1 和麦芽酚铁复合物相关的药物开发的不同方面的详细见解,包括发明的理论概念;药物发现;新的化学合成;体外、体内和临床筛选;毒理学;药理学;以及剂量方案的优化。根据来自其他学术和商业中心以及不同监管机构的竞争药物,讨论了这两种药物在许多其他疾病中的应用前景。还强调了基础科学和其他策略,以及当前全球制药领域的许多限制,重点是孤儿药和急诊医学发展的优先事项,包括学术科学界、制药公司和患者组织的作用。