CICECO-Aveiro Institute of Materials, University of Aveiro, 3810-193 Aveiro, Portugal.
LAQV-Requimte, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.
J Med Chem. 2021 Feb 11;64(3):1260-1282. doi: 10.1021/acs.jmedchem.0c01292. Epub 2021 Feb 1.
Bisphosphonates, used for a long time in osteoporosis management, are currently the target of intensive research, from pre-formulation studies to more advanced stages of clinical practice. This review presents an overview of the contributions of this family of compounds to human health, starting with the chemistry and clinical uses of bisphosphonates. Following this, their pharmacology is described, highlighting administration-borne handicaps and undesirable effects. The last three sections of the review describe the research efforts that seek to curb delivery-related issues and expand bisphosphonate use. Innovative routes and strategies of administration, such as nano-encapsulation for oral intake or injectable cements for local or in-bone delivery are presented, as well as the latest results of case studies or preclinical studies proposing new therapeutic indications for the clinically approved bisphosphonates. Finally, a selection of anti-infectious bisphosphonate new drug candidates is shown, with focus on the molecules reported in the last two decades.
双膦酸盐类药物在骨质疏松症的长期管理中被广泛应用,目前是研究的热点,从制剂前研究到更先进的临床阶段。本综述概述了该类化合物对人类健康的贡献,从双膦酸盐的化学和临床用途开始。在此基础上,描述了它们的药理学特性,强调了给药相关的障碍和不良影响。综述的最后三个部分描述了旨在解决与给药相关问题并扩大双膦酸盐类药物应用的研究工作。介绍了创新性的给药途径和策略,如口服纳米封装或局部或骨内注射的可注射水泥,以及最新的案例研究或临床前研究结果,提出了临床批准的双膦酸盐类药物的新治疗适应症。最后,展示了一组抗感染双膦酸盐类新药候选物,重点是过去二十年报道的分子。