成都先导与UPPTHERA签订基于DNA编码化合物库技术的新药研发合作协议

中国成都，2021年3月1日  成都先导药物开发股份有限公司（以下简称“成都先导”）宣布与UPPTHERA Inc.（以下简称“UPPTHERA”）达成新药研发合作，以期针对UPPTHERA关注的靶点发现全新结构的小分子化合物以及E3泛素连接酶。成都先导将利用其以DNA编码化合物库（DNA Encoded Library，以下简称DEL）的设计、合成及筛选为核心的先进技术平台为UPPTHERA筛选针对特定靶点的先导化合物，并将这些先导化合物排他性地转让UPPTHERA。基于此协议，成都先导将收到首付款及后续里程碑款，具体金额未被披露。

成都先导董事长兼首席执行官李进博士表示：

UPPTHERA首席执行官Siwoo Choi博士表示：

UPPTHERA是一家制药公司，总部位于韩国松岛。UPPTHERA的目标是使用蛋白降解靶向嵌合体（PROTAC）方法来解决尚未满足的医疗需求，而传统药物尚不能解决这些需求。UPPTHERA的产品线最初侧重于肺癌、心血管疾病和血液学癌症。UPPTHERA还使用其专有的E3连接酶平台设计PROTAC分子，以降解ER膜上的致病蛋白。

成都先导药物开发股份有限公司是一家从事新药研发的快速发展的生物技术公司，总部位于中国成都，在英国剑桥、美国休斯顿设有子公司，并于2020年4月在上海证券交易所科创板挂牌上市（股票名称：成都先导，股票代码：688222.SH）。成都先导为小分子新药发现与优化建立了一个国际领先的，以DNA编码化合物库的设计、合成和筛选（DEL），以及基于分子片段和三维结构信息的药物设计（FBDD/SBDD）为核心的技术平台。目前，公司基于数百种不同的骨架结构，已经完成10,000亿种结构全新、具有多样性和类药性的DNA编码化合物的合成，并且已有多个案例证实了其针对已知生物靶点和新兴生物靶点筛选苗头化合物的能力。

成都先导并购了坐落于英国剑桥的Vernalis公司，该公司是FBDD/SBDD技术的领先者。现在，成都先导拥有超过500人的科学家团队，并且能够提供一整套从靶基因到新药临床试验申请阶段的研发服务，覆盖范围包括重组蛋白表达纯化、结构生物学、计算化学与药物化学、生物化学和生物物理学、细胞生物学、体内药理学、药代动力学、药学研究等。

成都先导业务模式灵活，范围从基于单一功能的服务（FFS，如，蛋白表达与纯化，结构生物学，生物信息学，计算化学，药物化学，核酸及有机合成，分析化学，生物物理，细胞生物学，药代，药效等），DEL 筛选，DEL设计，合成及表征，整合式药物发现项目，风险分担项目，合资企业到项目转让许可。成都先导拥有大约20个内部新药项目，处于临床及临床前不同阶段。成都先导业务遍布北美、欧洲、亚洲、非洲及澳大利亚等，现已与多家国际著名制药公司、生物技术公司、化学公司、基金会以及科研机构建立合作，致力于新药的发现与应用。

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HitGen and UPPTHERA Enter Into Drug Discovery Research Collaboration

CHENGDU, China, March 1^st, 2021 

HitGen (688222.SH) today announced that it has entered into a drug discovery research collaboration with UPPTHERA Inc. to identify small molecule Hits against previous known-to-be undruggable targets and novel E3 ligase. HitGen will apply its platform technology, based on the design, synthesis and screening of DNA-encoded libraries (DEL) to discover compounds that bind to certain targets. The identified compounds will be exclusively licensed to UPPTHERA for further development. Under the terms of the agreement, HitGen will receive an undisclosed upfront payment, success fee, license/milestone fee from UPPTHERA.

“We are delighted to enter this collaboration with UPPTHERA, an emerging pharmaceutical venture company aiming for new drug development based on targeted protein degradation (TPD) technology. We look forward to working closely with UPPTHERA’s research teams to deliver novel small molecules to their programs, ” said Dr. Jin Li, Chairman of the Board and Chief Executive Officer of HitGen.

“HitGen’s DEL screening platform offers tremendous potential to identify a small molecule binder to UPPTHERA’s targets of interest”, said Dr. Siwoo Choi, Chief Executive Officer of UPPTHERA. “Our alliance enables us to discover and develop pipeline of novel therapeutics for diseases which traditional drugs have failed in the past.”

UPPTHERA is a pharmaceutical venture company headquartered in Songdo, South Korea. UPPTHERA aims to use Proteolysis Targeting Chimera (PROTAC) modality to solve unmet needs which have not been solved by traditional drug modalities. UPPTHERA’s pipeline is initially focused on, lung cancers, cardiovascular diseases, and hematologic cancers. UPPTHERA also uses its proprietary E3 ligase platform to design PROTAC molecules to degrade the disease-causing proteins on the ER membrane.

HitGen Inc. is a rapidly developing biotech company headquartered in Chengdu, China, with subsidiaries in Cambridge, UK and Houston, USA. It became a publicly listed company in Shanghai Stock Exchange in April 2020 (ticker code 688222.SH). HitGen has established a drug discovery research platform centered on the design, synthesis and screening of DNA encoded chemical libraries (DELs), fragment-based drug discovery (FBDD) and structure-based drug design (SBDD) technologies. HitGen's DELs currently contains more than 1 trillion novel, diverse, drug-like small molecules and macrocyclic compounds. These compounds are members of DELs synthesized from many hundreds of distinct chemical scaffolds, designed with tractable chemistry, and have yielded proven results for the discovery of small molecule leads against precedented and unprecedented classes of biological targets.

Through its acquisition of Cambridge UK based Vernalis R&D Ltd, a leader in FBDD/SBDD, HitGen now has a research team of over 500 scientists and offers a full set of research capabilities from recombinant protein expression and purification, structural biology, assay development, screening, DEL synthesis, nucleic acid and small molecule chemical synthesis, computational and medicinal chemistry, biochemistry and biophysics, cell biology, in vivo pharmacology, DMPK, CMC, etc., to enable drug discovery research from target gene to IND filing.

HitGen operates a flexible business model, ranging from a single capability-based fee for services (FFS，e.g., protein expression and purification, structural biology, bioinformatics, computational chemistry, medicinal chemistry, nucleic and organic chemistry, analytical chemistry, biophysics, PK, PD, etc.), DEL screening, DEL design, synthesis and characterization, integrated drug discovery projects, risk sharing projects, collaborative ventures to program out-licensing. HitGen has approximately 20 in-house drug discovery programs at different stages of research & development. HitGen is collaborating with pharmaceutical, biotech and chemical companies, foundations and research institutes in North America, Europe, Asia, Africa and Australia to enable the discovery and development of novel medicines and agrochemicals.

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