Page 75 - 《中国药房》2023年8期

专利视角下我国蛋白降解靶向嵌合体技术创新态势研究

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曹 倩 ，曹梦超（国家知识产权局专利局专利审查协作江苏中心，江苏 苏州 215163）
中图分类号 R914；G306 文献标志码 A 文章编号 1001-0408（2023）08-0961-07
DOI 10.6039/j.issn.1001-0408.2023.08.13

摘 要 目的 为我国蛋白降解靶向嵌合体（PROTAC）技术研究提供信息服务支撑，为相关药物研发机构的技术开发和专利布局
提供参考。方法 采用专利分析法，以HimmPat专利数据库为检索平台，对截至2022年2月向中国国家知识产权局专利局申请且
已公开的PROTAC技术相关专利申请进行检索，对其专利申请趋势、技术生命周期、主要申请人、技术来源国、技术主题及改进路
线等专利数据进行分析。结果与结论 本研究共纳入专利133件。PROTAC技术在我国开始进行专利申请的时间较晚，申请人数
量从2015年的2家发展到2020年的30家，申请量从2015年的2件增长到2020年的38件，年度专利申请量和申请人数量都处于快
速增长时期，但单个申请人年均申请量仍不足2件，表明该领域的研究仍处于技术的发展期早期；Arvinas、海思科、海创药业等申
请人的申请数量位居前列。国内申请量虽领先于国外来华申请量，但国内专利申请的平均简单同族申请量及平均简单同族国家
量仅为1.5，远低于国外来华申请量，反映出国内申请在“质”的层面仍有提升空间。PROTAC技术最初的改进主要集中在E3连接
酶配体和靶点、配体的选择，之后陆续出现新型 PROTAC 开发、连接子设计、配套方法等新的改进方向，表明专利申请主体在
PROTAC技术发展初期便已开始多赛道布局。建议我国PROTAC药物研发可重点从提高PROTAC药物的口服生物利用度、生物
安全性，克服潜在耐药性，探索理性设计及评估方法等方面进行考虑。
关键词 蛋白降解靶向嵌合体；专利分析；技术创新；药物研究

Research on technological innovation of PROTAC in China from the perspective of patent
CAO Qian，CAO Mengchao（Patent Examination Cooperation Jiangsu Center of the Patent Office，CNIPA，Jiangsu
Suzhou 215163， China）

ABSTRACT OBJECTIVE To provide information service support for research on proteolysis targeting chimera （PROTAC） in
China and provide reference for technical development and patent layout of relevant drug research and development institutions.
METHODS The patent analysis method was used to search the patent applications related to PROTAC technology that had been
applied to China National Intellectual Property Administration and had been issued before Feb. 2022， using the HimmPat patent
database as the search platform. The patent application trend， technology life cycle， main applicants， technology source countries，
technology themes， improvement routes and other patent data were analyzed. RESULTS & CONCLUSIONS A total of 133
patents were included in this study. The patent application for PROTAC technology started relatively late in China， with the number
of applicants increasing from 2 in 2015 to 30 in 2020， and the number of applications increasing from 2 in 2015 to 38 in 2020.
Both the annual patent application volume and the number of applicants were in a period of rapid growth， but the average annual
application volume of a single applicant was still less than 2， indicating that research in this field was still in the early stage of
technology development； the number of applications from Arvinas， Hisco， and Hinova Pharmaceutical Inc. ranked among the top.
Although the number of domestic applications led that of foreign applications in China， the average number of simple peer
applications and the average number of simple peer countries in domestic patent applications was only 1.5， which was far lower
than that of foreign applications in China， reflecting that there was still room for improvement in the “quality” level of domestic
applications. The initial improvements in PROTAC technology mainly focused on the selection of E3 ligands， targets and ligands，
and then new improvements such as new PROTAC development， linker design and matching methods emerged， indicating that the
patent applicant had started a multi-track layout in the early stages of the development of PROTAC technology. It is suggested that
the research and development of PROTAC drugs in China should focus on improving the oral bioavailability and biosafety of
PROTAC drugs， overcoming potential drug resistance， and exploring rational design and evaluation methods.
KEYWORDS proteolysis targeting chimera； patent analysis； technology innovation； drugs research

蛋白降解靶向嵌合体（proteolysis targeting chimera， 作为异双功能分子，由 3 部分组成，一端与 E3 连接酶结
PROTAC）是药物研发领域的一个新兴方向。PROTAC 合的配体连接，另一端与靶蛋白结合的配体连接，中间
为二者的连接子（linker） 。PROTAC 技术具有以下两
[1]
＊第一作者 副研究员。研究方向：医药化学领域专利实质审查
及知识产权政策。E-mail：56252581@qq.com 个主要优势：（1）PROTAC 只需具备与靶蛋白结合的活

中国药房 2023年第34卷第8期 China Pharmacy 2023 Vol. 34 No. 8 · 961 ·