D'Acquarica Ilaria, Agranat Israel
Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, 00185 Rome, Italy.
Organic Chemistry, Institute of Chemistry, The Hebrew University of Jerusalem, Edmond J. Safra Campus, Jerusalem 9190401, Israel.
ACS Pharmacol Transl Sci. 2023 Jan 17;6(2):201-219. doi: 10.1021/acsptsci.2c00151. eCollection 2023 Feb 10.
Drug repurposing toward new medical uses and chiral switches are elements of secondary pharmaceuticals. The drug repurposing and chiral-switches strategies have mostly been applied independently in drug discovery. Drug repurposing has peaked in the search for therapeutic treatments of the Coronavirus Disease 2019 pandemic, whereas chiral switches have been overlooked. The current Perspective introduces the drug repurposing/chiral-switches combination strategy, overviewing representative cases of chiral drugs that have undergone this combination: ketamine, flurbiprofen, fenfluramine, and milnacipran. The deuterium-enabled chiral switches of racemic thalidomide analogs, a variation of the repurposing/chiral-switch combination strategy, is also included. Patenting and regulatory-exclusivity considerations of the combination strategy in the discovery of new medical uses are considered. The proposed combination creates a new synergy of its two elements, overcoming arguments against chiral switches, with better prospects for validation of patents and regulatory exclusivities. The combination strategy may be applied to chiral switches to paired enantiomers. Repurposing/chiral-switch drugs may be 'obvious-to-try'; however, their inventions may be unexpected and their patents nonobvious. Patenting repurposing/chiral-switch combination drugs is not 'evergreening', 'product hopping', and 'me-too'. The expected benefits and opportunities of the combined repurposing/chiral-switch strategy vis-à-vis its two elements are superior pharmacological properties, overcoming arguments against patent validities, challenges of chiral-switch patents, reduced expenses, shortened approval procedures, and higher expectations of regulatory exclusivities.
药物重新利用以实现新的医学用途以及手性转换是二次制药的要素。药物重新利用和手性转换策略在药物研发中大多是独立应用的。在寻找2019冠状病毒病大流行的治疗方法方面,药物重新利用已达到顶峰,而手性转换却被忽视了。本观点文章介绍了药物重新利用/手性转换组合策略,概述了经历过这种组合的手性药物的代表性案例:氯胺酮、氟比洛芬、芬氟拉明和米氮平。还包括外消旋沙利度胺类似物的氘启用手性转换,这是重新利用/手性转换组合策略的一种变体。考虑了在发现新医学用途中该组合策略的专利和监管独占性问题。所提出的组合创造了其两个要素的新协同效应,克服了对手性转换的反对意见,在专利和监管独占性验证方面有更好的前景。该组合策略可应用于对映体对的手性转换。重新利用/手性转换药物可能是“显而易见的尝试”;然而,它们的发明可能是意想不到的,其专利可能是非显而易见的。为重新利用/手性转换组合药物申请专利并非“专利常青”“产品跳跃”和“仿制药”。相对于其两个要素,重新利用/手性转换组合策略预期的益处和机会在于具有优越的药理特性,克服了对专利有效性的反对意见、手性转换专利的挑战、降低费用、缩短审批程序以及对监管独占性有更高期望。