靶点的选择在药物开发的激烈竞争中显得尤其重要。研究者们需要通过一些因素考虑靶点的科学有效性。这些因素包括针对这些靶点开发药物的公司数量、针对这些靶点的药物所处的临床阶段以及潜在的患者分层等。平衡这些因素是具有挑战性的,但可能会增加成功开发first-in-class或 best-in-class药物的机会。
12月16日,发表在Nature Reviews Drug Discovery上题为“Trial watch: Opportunities and challenges of the 2016 target landscape”的文章分析了2016年靶点“景观图”,共涉及661个靶点(备注:作者们分析的靶点仅包括人类蛋白)。其中,285个为经过验证的靶点(proven target,即有针对这一靶点的药物已经上市或者在注册或建议批准阶段。),376个为新靶点(novel target)。
图1 | Examination of the target landscape in 2016. a | Competition for all human protein targets with associated selective drugs. b | Competition level for proven targets only. c | Competition level for novel targets only.
图2 | d | Distribution of competition for novel targets by phase of development. e | Distribution of competition for proven targets by phase of development.
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