Off-Patent Drug Repositioning
Off-Patent Drug Repositioning
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专利外药物重新定位
DOI：
10.1021/acs.jcim.0c00826
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发表时间：
2020-12-28
影响因子：
5.6
通讯作者：
Oprea, Tudor, I
中科院分区：
文献类型：
--
作者：
Avram, Sorin;Curpan, Ramona;Oprea, Tudor, I
药物重新定位旨在重复使用“老”药来治疗批准适应症以外的疾病(S)。物质成分专利和FDA的排他性可能会阻碍一些需要重新定位(重新调整用途)的药物立即可用。在这里，我们分析来自FDA橙皮书的数据，并使用当前市场上的专利有效性和排他性将药物分类为专利上(ONP)、专利外(OFP)和非市场(OFM)集。在没有一致接受的小分子定义的情况下，这些集合包括分子量在100到1250之间的有机分子和肽，从而分别产生237种ONP药物、320种OFM药物和996种OFP药物。我们讨论了这三类药物在初级分子性质、化学多样性、作用机制靶类和治疗领域方面的差异，并对OFP药物在不久的将来的丰富进行了评论。鉴于知识产权状况，在没有具体财产权的情况下，我们建议将药物列为优先事项，以改进重新定位战略：(1)OFP、(2)OFM和(3)ONP。
Drug repositioning aims to reuse "old" drugs to treat diseases outside their approved indication(s). Composition-of-matter patents and FDA exclusivities can hinder the immediate availability of some drugs to be repositioned (repurposed). Here, we analyze data from the FDA Orange Book and use current on-market patent validity and exclusivities to classify drugs into on-patent (ONP), off-patent (OFP), and off-market (OFM) sets. In the absence of an unanimously accepted definition for small molecules, these sets include organic molecules and peptides with molecular weight between 100 and 1250, which resulted in 237 ONP drugs, 320 OFM, and 996 OFP drugs, respectively. We discuss the differences between the three categories in terms of primary molecular properties, chemical diversity, mechanism-of-action target classes, and therapeutic areas and comment on the enrichment of OFP drugs in the near future. Given the intellectual property landscape, and in the absence of specific property rights, we suggest that drugs should be prioritized as follows, to improve the repositioning strategy: (i) OFP, (ii) OFM, and (iii) ONP, respectively.