A Phase 1b/2 Study Evaluating the Activity of Tinengotinib (TT-00420) in Combination With Androgen Receptor Signaling Inhibitors (ARSIs) in Patients With Metastatic Castration Resistant Prostate Cancer (mCRPC)

The purpose of this study is to find out whether tinengotinib in combination with abiraterone acetate and prednisone or enzalutamide is a safe treatment that causes few or mild side effects in people with metastatic castration-resistant prostate cancer (mCRPC).

开始日期2024-06-04

申办/合作机构

Memorial Sloan Kettering Cancer Center

[+1]

CTIS2023-505660-11-00

/ Recruiting临床3期

A Phase III, Randomized, Controlled, Global Multicenter Study to Evaluate the Efficacy and Safety of Oral Tinengotinib versus Physician’s Choice in Subjects with Fibroblast Growth Factor Receptor (FGFR) altered, Chemotherapy- and FGFR Inhibitor-Refractory/Relapsed Cholangiocarcinoma (FIRST-308) - TT420C2308

开始日期2024-04-25

申办/合作机构

药捷安康（南京）科技股份有限公司初创企业

NCT06221774

/ Not yet recruiting临床1/2期IIT

An Open-Label, Multi-Cohort, Two-Stage, Phase Ib/II Clinical Study to Evaluate the Safety and Efficacy of TT-00420 Tablets Combined With Toripalimab Injection in Treating Advanced Urological Tumors

This Phase Ib/II clinical study is an open-label, multi-cohort, two-stage trial designed to assess the safety and efficacy of different doses of TT-00420 tablets in combination with Toripalimab injection for treating patients with advanced urological tumors. The study aims to evaluate the effectiveness of TT-00420 tablets at the optimal dose combined with Toripalimab in treating different types of advanced urological tumors.

开始日期2024-02-01

申办/合作机构

南京鼓楼医院

100 项与 Tinengotinib 相关的临床结果

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100 项与 Tinengotinib 相关的转化医学

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100 项与 Tinengotinib 相关的专利（医药）

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项与 Tinengotinib 相关的文献（医药）

2024-12-01·ANNALS OF ONCOLOGY

A Model for Decoding Resistance in Precision Oncology: Acquired Resistance to FGFR inhibitors in Cholangiocarcinoma

Article

作者: Qiang, X ; Borad, M ; Kambadakone, A R ; Shroff, R T ; Danysh, B P ; Flaherty, K T ; Leshchiner, I ; Martin, E E ; DiToro, D ; Lennerz, J K ; Saha, S K ; Lin, B ; Javle, M ; Chen, C T ; Iyer, R ; Sun, C ; Friboulet, L ; Harris, T ; Wang, H ; Li, L ; Reyes, S ; Cleary, J M ; Stone, J R ; Fan, J ; Gordan, J D ; Karasic, T ; Bensen, D C ; Iyer, S ; Kelley, R K ; Hoffman, I D ; Berchuck, J E ; Sootome, H ; Maurer, J ; Damjanov, N ; Baiev, I ; Goyal, L ; Peng, P ; Uboha, N V ; Wehrenberg-Klee, E ; Mody, K ; Parida, L ; Getz, G ; Walmsley, C ; Hollebecque, A ; Juric, D ; Nelson, K J ; Harris, W ; Majeed, U ; Zhang, K ; Zhu, A X ; Facchinetti, F ; Wu, F ; Vasseur, D ; Hirai, H ; Pinto, C

BACKGROUND:

Fibroblast growth factor receptor (FGFR) inhibitors have significantly improved outcomes for patients with FGFR-altered cholangiocarcinoma, leading to their regulatory approval in multiple countries. However, as with many targeted therapies, acquired resistance limits their efficacy. A comprehensive, multimodal approach is crucial to characterizing resistance patterns to FGFR inhibitors.

PATIENTS AND METHODS:

This study integrated data from six investigative strategies: cell-free DNA, tissue biopsy, rapid autopsy, statistical genomics, in vitro and in vivo studies, and pharmacology. We characterized the diversity, clonality, frequency, and mechanisms of acquired resistance to FGFR inhibitors in patients with FGFR-altered cholangiocarcinoma. Clinical samples were analyzed longitudinally as part of routine care across 10 institutions.

RESULTS:

Among 138 patients evaluated, 77 met eligibility, yielding a total of 486 clinical samples. Patients with clinical benefit exhibited a significantly higher rate of FGFR2 kinase domain mutations compared to those without clinical benefit (65% vs 10%, p<0.0001). We identified 26 distinct FGFR2 kinase domain mutations, with 63% of patients harboring multiple. While IC50 assessments indicated strong potency of pan-FGFR inhibitors against common resistance mutations, pharmacokinetic studies revealed that low clinically achievable drug concentrations may underly polyclonal resistance. Molecular brake and gatekeeper mutations predominated, with 94% of patients with FGFR2 mutations exhibiting one or both, whereas mutations at the cysteine residue targeted by covalent inhibitors were rare. Statistical genomics and functional studies demonstrated that mutation frequencies were driven by their combined effects on drug binding and kinase activity rather than intrinsic mutational processes.

CONCLUSION:

Our multimodal analysis led to a model characterizing the biology of acquired resistance, informing the rational design of next-generation FGFR inhibitors. FGFR inhibitors should be small, high-affinity, and selective for specific FGFR family members. Tinengotinib, a novel small molecule inhibitor with these characteristics, exhibited preclinical and clinical activity against key resistance mutations. This integrated approach offers a blueprint for advancing drug resistance research across cancer types.

2024-09-01·DRUGS IN R&D

Pharmacokinetics, Mass Balance, and Biotransformation of [14C]tinengotinib, A Novel Multi-target Kinase Inhibitor, in Healthy Subjects

Article

作者: Sun, Xiaofen ; Miao, Liyan ; Zhu, Yujia ; Sun, Caixia ; Ni, Shumao ; Fan, Jean ; Gu, Zheming ; Li, Lin ; Wang, Hui ; Peng, Peng ; Ma, Sheng ; Yu, Yingying ; Wu, Frank ; Yu, Zhenwen ; Zhang, Hua

BACKGROUND AND OBJECTIVE:

Tinengotinib, a novel multi-target small molecule kinase inhibitor, is currently undergoing phase II clinical trial in the USA and China. The purpose of this open-label study was to investigate the absorption, metabolism, and excretion of [¹⁴C]tinengotinib following a single oral dose in healthy subjects.

METHODS:

Six healthy male subjects received a single oral dose of [¹⁴C]tinengotinib capsules at 10 mg/100 µCi, and blood, urine, and feces samples were collected. Phenotyping experiments were further conducted to confirm the enzymes involved in its metabolism.

RESULTS:

Tinengotinib was rapidly absorbed in plasma with a time to peak drug concentration (T_max) of 1.0-4.0 h post-dose and a long terminal half-life (t_½) of 23.7 h. Blood-to-plasma radioactivity concentration ratios across timepoints ranged from 0.780 to 0.827, which indicated minimal association of radioactivity with blood cells. The mean cumulative excreted radioactivity was 99.57% of the dose, including 92.46% (68.65% as unchanged) in feces and 7.11% (0.28% as unchanged) in urine. In addition to unchanged tinengotinib, a total of 11 radioactive metabolites were identified in plasma, urine, and feces. The most abundant circulating radioactivity was the parent drug in plasma, which comprised 88.23% of the total radioactivity area under the concentration-time curve (AUC). Metabolite M410-3 was a major circulating metabolite, accounting for 5.38% of the parent drug exposure and 4.75% of the total drug-related exposure, respectively. All excreted metabolites accounted for less than 5.10% and 1.82% of the dose in feces and urine, respectively. In addition, no unique metabolites were observed in humans. Tinengotinib was metabolized mainly via CYP3A4.

CONCLUSIONS:

Overall, tinengotinib demonstrated a complete mass balance with limited renal excretion, no disproportionate blood metabolism, and slow elimination, primarily through the fecal route. The results of this study provide evidence to support the rational use of tinengotinib as a pharmacotherapeutic agent.

REGISTRATION:

ChinadrugTrials.org.cn identifier: CTR20212852.

2024-04-04·The oncologist

First-In-Human Phase I Study of Tinengotinib (TT-00420), a Multiple Kinase Inhibitor, as a Single Agent in Patients With Advanced Solid Tumors

Article

作者: Rodon, Jordi A ; Ni, Shumao ; Sun, Caixia ; Fan, Jean ; Meric-Bernstam, Funda ; Piha-Paul, Sarina A ; Xu, Binghe ; Mott, Frank ; Tsimberidou, Apostolia M ; Peng, Peng ; Levin, Wendy J ; Conley, Anthony P ; Ngo, Brenda ; Ru, Qinhua Cindy ; Fan, Ying ; Dumbrava, Ecaterina E ; Wang, Hui ; Hong, David S ; Karp, Daniel D ; Ajani, Jaffer A ; Fu, Siqing ; Javle, Milind M ; Wu, Frank ; Raghav, Kanwal ; Qiang, Xiaoyan

Abstract:

Purpose:

This first-in-human phase I dose-escalation study evaluated the safety, pharmacokinetics, and efficacy of tinengotinib (TT-00420), a multi-kinase inhibitor targeting fibroblast growth factor receptors 1-3 (FGFRs 1-3), Janus kinase 1/2, vascular endothelial growth factor receptors, and Aurora A/B, in patients with advanced solid tumors.

Patients and Methods:

Patients received tinengotinib orally daily in 28-day cycles. Dose escalation was guided by Bayesian modeling using escalation with overdose control. The primary objective was to assess dose-limiting toxicities (DLTs), maximum tolerated dose (MTD), and dose recommended for dose expansion (DRDE). Secondary objectives included pharmacokinetics and efficacy.

Results:

Forty-eight patients were enrolled (dose escalation, n = 40; dose expansion, n = 8). MTD was not reached; DRDE was 12 mg daily. DLTs were palmar-plantar erythrodysesthesia syndrome (8 mg, n = 1) and hypertension (15 mg, n = 2). The most common treatment-related adverse event was hypertension (50.0%). In 43 response-evaluable patients, 13 (30.2%) achieved partial response (PR; n = 7) or stable disease (SD) ≥ 24 weeks (n = 6), including 4/11 (36.4%) with FGFR2 mutations/fusions and cholangiocarcinoma (PR n = 3; SD ≥ 24 weeks n = 1), 3/3 (100.0%) with hormone receptor (HR)-positive/HER2-negative breast cancer (PR n = 2; SD ≥ 24 weeks n = 1), 2/5 (40.0%) with triple-negative breast cancer (TNBC; PR n = 1; SD ≥ 24 weeks n = 1), and 1/1 (100.0%) with castrate-resistant prostate cancer (CRPC; PR). Four of 12 patients (33.3%; HR-positive/HER2-negative breast cancer, TNBC, prostate cancer, and cholangiocarcinoma) treated at DRDE had PRs. Tinengotinib’s half-life was 28-34 hours.

Conclusions:

Tinengotinib was well tolerated with favorable pharmacokinetic characteristics. Preliminary findings indicated potential clinical benefit in FGFR inhibitor-refractory cholangiocarcinoma, HER2-negative breast cancer (including TNBC), and CRPC. Continued evaluation of tinengotinib is warranted in phase II trials.

项与 Tinengotinib 相关的新闻（医药）

2024-12-22

·医药魔方Invest

药捷安康完成赴港IPO备案

2024年12月20日，证监会对药捷安康（南京）科技股份有限公司（简称“药捷安康”）赴港IPO的上市备案予以确认。图片来源：证监会官网据悉，药捷安康拟发行不超过1.46亿股境外上市普通股并在港交所上市，34名股东拟将所持合计286,385,673股境内未上市股份转为境外上市股份，并在港交所上市流通。以下为“全流通”股东名称及转换数量：今年6月份，药捷安康曾递表港交所。招股书显示，药捷安康是一家以临床需求为导向、处于注册临床阶段的生物制药公司，专注于发现及开发肿瘤、炎症及心脏代谢疾病小分子创新疗法。凭借本身全面融合的内部研发系统，药捷安康已建立六款临床阶段候选产品及一款临床前阶段候选产品的管线。图片来源：药捷安康招股书（下同）其核心产品Tinengotinib(TT-00420)是一款有潜力成为全球首创药物、处于注册阶段、自主研发的独特多靶点激酶（「MTK」）抑制剂（主要靶向三个关键通路（即FGFR/VEGFR、JAK和Aurora激酶））。Tinengotinib有潜力治疗各种复发或难治、耐药实体瘤（包括胆管癌（「胆管癌」）、前列腺癌、乳腺癌、胆道系统癌症（「BTC」）和泛FGFR实体瘤）的未满足的临床需求。药捷安康计划首先在中国进行Tinengotinib用于治疗胆管癌的商业化。患有这种疾病的患者通常会寻求在少数以治疗胆管癌而闻名的医院接受治疗。考虑到容易接触到Tinengotinib的目标患者人群，其目前正准备成立内部商业团队。招股书显示，药捷安康已完成9轮融资，最后一轮D+轮融资后，其投后估值为45.9亿元。财务方面，2022年和2023年，药捷安康分别实现营收约12.4万元和118.1万元，对应年内亏损为2.5亿元和3.43亿元。药捷安康股权结构截至最后实际可行日期，药捷安康的执行董事兼董事会主席吴博士通过南京益镤及南京吉旻瑞直接及间接持有本公司已发行股本总额的约34.29%，为控股股东。其简历如下：吴永谦博士，61岁，为本公司董事长、执行董事兼首席执行官。其于2016年6月10日加入本公司，自此一直参与本公司的日常运营。吴博士自2016年11月18日起一直担任董事长。吴博士主要负责总体战略规划、业务方向和运营管理。吴博士拥有逾27年生物医药行业经验。于加入本公司前，吴博士于2011年加入四环医药控股集团有限公司（股份代号：0460）（「四环医药」，一家于联交所主板上市，从事药品研发、生产和销售的综合制药公司）。吴博士于2011年1月至2012年12月担任山东轩竹医药科技有限公司（「山东轩竹医药」，四环医药当时的一家全资附属公司）的项目管理高级副总裁，并于2013年1月至2016年5月担任山东轩竹医药的总经理，主要负责公司的整体管理和营运。其于2014年至2015年担任四环医药的首席科学家。彼亦曾于Boehringer Ingelheim Pharmaceuticals Inc.任职五年，负责免疫学及心血管药物的研究项目。此外，其于1996年11月至2005年6月受僱于Guilford Pharmaceuticals, Inc.。吴博士在业界及社会获授予多项证书及荣誉。彼于2008年至2010年担任著名的美国化学学会药物化学分会长期规划委员会委员。彼于2014年及2020年分别获任命为《中国新药杂志》及《药学进展》的编辑。彼为中国医药创新促进会首届（2015年至2019年）「药物研发专业委员会」委员。彼于2014年5月至2017年5月担任中山大学药学院的客座教授。吴博士于1985年7月取得中国南京大学化学学士学位。彼于1993年5月进一步取得美国韦恩州立大学哲学博士学位及于1994年1月至1995年12月获委任为美国布兰迪斯大学生物化学系博士后研究员。推荐阅读药捷安康递表港交所，估值为45.9亿元宇能制药IPO辅导验收，筹划赴北交所上市 Copyright © 2024 PHARMCUBE. All Rights Reserved. 欢迎转发分享及合理引用，引用时请在显要位置标明文章来源；如需转载，请给微信公众号后台留言或发送消息，并注明公众号名称及ID。免责申明：本微信文章中的信息仅供一般参考之用，不可直接作为决策内容，医药魔方不对任何主体因使用本文内容而导致的任何损失承担责任。

IPO财报高管变更

2024-12-09

·PRNewswire

2024 ESMO Asia: TransThera announces clinical data of tinengotinib in combination with atezolizumab (PD-L1) in biliary tract carcinoma (BTC)

NANJING, China and GAITHERSBURG, Md., Dec. 9, 2024 /PRNewswire/ -- TransThera Sciences Nanjing, Inc. (the " TransThera") announced the poster presentation at the 2024 European Society For Medical Oncology (ESMO) Asia Congress to discuss the clinical study of tinengotinib in combination with atezolizumab (Tecentriq®) in biliary tract carcinoma (BTC). Title: Tinengotinib (TT-00420) in Combination with Atezolizumab in Chinese Patients with Biliary Tract Carcinoma (BTC): Efficacy and Safety Results from a Phase Ib/II Study Poster number: 140P Immune-checkpoint inhibitor (ICI) combined with chemotherapy have been approved as first-line therapy for BTC. However, no standard of care has been established after first-line treatment and the survival of the patients is short, there is a huge unmet clinical need. Tinengotinib is a novel multi-kinase inhibitor. It may play a role of synergistic effect when combined with ICI. The efficacy and safety data of tinengotinib in combination with atezolizumab in Chinese BTC patients has been explored in a phase Ib/II study. Results: As of September 26, 2024, a total of 31 heavily pretreated advanced BTC patients were enrolled and treated with tinengotinib plus atezolizumab. 71.0% were priorly treated with at least one immunotherapy. Promising efficacy: A total of 20 intrahepatic cholangiocarcinoma patients were efficacy evaluable. The objective response rate (ORR) and disease control rate (DCR) were 25.0% and 80.0%, the median progression free survival (mPFS) reached 8.77 months and the 12-month overall survival (OS) rate was 70.1%. A total of 28 cholangiocarcinoma patients were efficacy evaluable. The ORR and DCR were 25.0% and 75.0%, the mPFS reached 5.72 months and the 12-month OS rate was 64.8%. All 31 BTC patients were efficacy evaluable. The ORR and DCR were 22.6% and 74.2%, the mPFS reached 4.11 months and the 12-month OS rate was 61.8%. Similar efficacy was observed regardless of prior ICI(s) therapy. Good safety and tolerability: No DLT was observed in the dose escalation phase. The combination therapy was generally well tolerated in heavily pre-treated BTC patients. These encouraging results suggest the combination therapy may have synergistic effect in treating some solid tumor such as BTC, and support the further exploration to evaluate the safety and efficacy of tinengotinib plus ICI in BTC patients who were previously treated with or without ICI therapy. About Tinengotinib Tinengotinib is an internally discovered, global phase III multi-kinase inhibitor that exerts antitumor effects by targeting FGFRs and VEGFRs, mitotic kinases Aurora A/B and Janus kinases (JAK). Ongoing clinical trials in the US and China have revealed the potential of tinengotinib to be efficacious in various solid tumors. It was granted the Orphan Drug Designation (ODD) and Fast Track Designation (FTD) by the FDA for the treatment of CCA, the Breakthrough Therapy Designation (BTD) by NMPA in China, the Orphan Drug Designation (ODD) for the treatment of biliary tract cancer by EMA. About TransThera TransThera is a clinical demand-oriented, registrational clinical-stage biopharmaceutical company focusing on discovering and developing innovative small molecule therapies for oncology, inflammatory and cardiometabolic diseases. Further aided by in-depth study of translational medicine and drug design, TransThera aims to develop first-in-class or best-in-class drug candidates strategically positioned to meet urgent clinical needs on a global scale. For more information, please visit Tecentriq® (atezolizumab) is a registered trademark of Genentech, a member of the Roche Group. Forward-looking statements This news contains forward-looking statements that involve risks, uncertainties, and assumptions. If risks or uncertainties ever materialize or the assumptions prove incorrect, our actual results may differ from those expressed or implied by such forward-looking statements. All statements other than statements of historical facts could be deemed forward-looking, including, but not limited to, any statement of the plans, strategies, and objectives of management for future operations, including but not limited to our clinical development and commercialization plans; any projections of financial information; any statements about historical results that may suggest trends for our business; any statements of expectation or belief regarding future events, potential markets or market size, technology developments, our product pipeline, clinical data, results or practices or the implications thereof, enforceability of our intellectual property rights, competitive strengths or our position within the industry; and any statements of assumptions underlying any of the items mentioned. SOURCE TransThera Sciences (Nanjing) Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

临床结果孤儿药快速通道临床3期免疫疗法

2024-09-05

·E药经理人

手握全球首创的Biotech闯关港股“胜算”几何？

港股或将迎来一批生物技术公司的上市潮。据东方财富Choice数据，2024年上半年，港股共有137家企业递表申请IPO，其中第二季度数量高于第一季度，并且在6月迎来一波高峰。具体来看，排队IPO的企业中，出现了“制药、生物科技与生命科学行业”“医疗保健设备与服务”板块扎堆复苏的迹象。对于国内的创新药企来说，不论上市与否、在哪里上市，被谈论最多、关注度最高的话题往往离不开两个关键词：手里还有多少钱？公司还值多少钱？而这些都共同指向一个评价维度：产品的创新性、稀缺性与成长性。对于尚未有产品上市销售的未盈利药企来说更是如此。不论是一级市场投资人的投资意愿，还是IPO成功后在二级市场的股价，都和这些因素紧密相关，开发具有高度差异化、高创新性的药物，已经成为衡量一家创新药企底色的重要标志。随着近来港交所递表的复苏，又有一批未盈利Biotech公司成为18A的预备队。在这之中，一家在2023年资本寒冬中逆风完成2.6亿元融资的Biotech公司被广泛关注。相比今天绝大部分以快速跟进为策略打造产品线、以中国为主要销售市场的18A公司和预备上市的公司不同，这家成立八年、手握全球首创药物、处于全球注册性临床阶段的Biotech，闯关港交所胜算有多大？ 01 挖潜FIC管线作为一家处于注册临床阶段的创新药公司，药捷安康目前尚未有产品获批上市。从业务上来看，药捷安康专注于发现及开发肿瘤、炎症及心脏代谢疾病小分子创新疗法，拥有6款临床阶段候选产品，以及1种临床前候选产品的管线。其招股书显示，核心产品Tinengotinib（TT-00420）是一款自主开发及研究、有潜质成为全球首创药物、处于注册临床阶段的独特MTK抑制剂，可靶向治疗若干耐药性、复发性或难治性肿瘤。Tinengotinib靶向三个关键信号通路，包括FGFR/VEGFR、JAK及Aurora。具体来看，通过靶向一种或多个通路，Tinengotinib可运用到不同的癌症类型，治疗不同的肿瘤人群。与FGFR的独特结合模式使Tinengotinib能够克服多克隆耐药突变，使其靶向FGFR驱动的癌症（如FGFR变异的胆管癌及泛FGFR实体瘤），而FGFR和其他几个关键通路的独特组合，又使其能够对其他的癌症类型（包括前列腺癌、乳腺癌及胆道系统肿瘤）有效。值得注意的是，Tinengotinib作为一款尚无任何参考开发路径的分子，目前没有其他MTK抑制剂具有相同的靶向组合及应用效果，研发过程需要付出巨大的努力和时间，需要沉下心来探索药物的疗效信号、研究生物学机制，不断重复从基础到临床（bench-to-bed）与从临床到基础（bed-to-bench）的过程，临床定位和开发难度可想而知。所幸Tinengotinib在临床上有所突破。这个产品目前已经在美国与中国相继开展胆管癌的注册性临床试验，也相继获得NMPA突破性治疗品种认定、FDA授予其治疗胆管癌的快速通道认定用于治疗胆管癌；获FDA授予用于治疗胆管癌的孤儿药认定；获EMA授予用于治疗胆道癌的孤儿药认定。招股书显示，截至2024年6月20日（最后实际可行日期），Tinengotinib共有8项临床试验在同步进行，其中，单药用于胆管癌的适应证正在美国、欧盟、英国、韩国等多地进行III期国际多中心临床试验，单药用于胆管癌的适应证正在中国进行II期关键性临床试验。从药捷安康给出的时间表来看，Tinengotinib用于胆管癌在国内的关键II期试验预计将于2025年下半年完成试验，国际多中心临床III期预计将于2026年下半年完成患者招募。按照披露时间表来看，Tinengotinib将优先在中国附条件批准，随后在全球其他地区获批。换言之，若临床试验与上市审批进展顺利，药捷安康最快将在一年后迎来首个商业化产品NDA。从一个创新分子成长为重磅炸弹药物，除了靶点选择（机制新）、分子结构差异（分子新）、临床定位（未满足需求）等等环节都要正确外，市场空间与成长性同样有着举足轻重的作用。作为进展最快的核心产品，Tinengotinib获批后的销售天花板也影响着投资者对药捷安康的态度。药捷安康以FGFR抑制剂经治耐药的胆管癌是目前全球进展最快的。说到FGFR，不免联想到EGFR，它们同属于受体酪氨酸激酶（RTKs）家族。正如三代EGFR-TKI奥希替尼克服了一二代EGFR-TKIs治疗进展后常见的耐药机制（T790M突变），极大地提高了患者的生存获益，Tinengotinib在针对晚期、经过多次治疗已经对FGFR抑制剂耐药的患者中，依然表现出良好的耐受性，并显示出抗肿瘤活性。从解决EGFR耐药到FGFR耐药，虽然靶点换了、适应证从非小细胞肺癌变成了胆管癌，研发进展最领先的公司也从跨国药企变成了来自中国的企业，但不变的是以明确的未满足临床需求为导向和致力于改善患者生存现状的追求。根据Frost&Sullivan报告，2023年全球胆管癌患者人数约为28万人，其中有25.2%的胆管癌患者观察到FGFR变异，7.4%的胆管癌患者观察到FGFR融合和重排。全球胆管癌药物市场规模预计到2026年将增长至31亿美元，2030年为54亿美元。中国的胆管癌药物市场规模预期在2026年将增长至55亿元。市场上有分析认为，胆管癌市场很小，没什么空间。但其实这是一种片面观点。有另一种声音指出，很多差异性较低的创新药在国内上市后价格较低，加之如果考虑纳入医保后，价格将更低。一些投资者是在这个维度下单纯从患者数量与国内的价格逻辑来计算，认为市场空间较小。而一旦产品具有明确的差异化，且有海外上市的机会，那将会遵循另一种药品定价逻辑：多个国产药物在海外上市后，定出高于中国价格约30倍的定价，如和黄医药的呋喹替尼在美国的价格是国内最新医保定价的24倍、君实生物的特瑞普利单抗在美国的价格是中国价格的33倍。可以说，利润空间都是非常大的。这也是如今中国生物医药企业面临的“必须走出国际化道路”的核心逻辑所在。药捷安康以全球首发的优势进入胆管癌细分市场，行业预测，会有较高的定价能力，享受高利润空间。加之若产品的全球III期试验成功，将会成为细分赛道的金标准，这一赛道的后来者若想参与竞争，需要与Tinengotinib开展头对头临床试验证明优效。这也意味着Tinengotinib将在相当长的一段时间内在细分赛道上有独占市场的潜力，这在中国目前的生物医药企业中是不多见的。同时，胆管癌只是Tinengotinib众多适应证之中的一个。药捷安康正在探索Tinengotinib在胆管癌之外的其他实体瘤适应证。针对治疗转移性去势抵抗性前列腺癌（mCRPC）、HER2-乳腺癌、胆道癌等适应证的研发，Tinengotinib均有管线进入临床II期，预计将于2024年Q4完成试验。这些大适应证的研发如果取得成功，基于胆管癌的定价权，将为Tinengotinib带来更加可观的产品收入。从这个角度上看，Tinengotinib不仅产品的创新和差异化强，未来商业化的想象空间也是巨大的。除核心产品Tinengotinib外，药捷安康也在推进肿瘤、炎症及心血管代谢疾病的多个临床项目。在肿瘤疾病领域，药捷安康正在推进两款在各自细分领域中具有同类最佳潜力的候选产品。TT-00973是潜在同类最佳的新型AXL/FLT3抑制剂，在抑制肿瘤细胞中AXL的磷酸化和激活方面具有高活性，使其有效治疗AXL的异常激活实体瘤。TT-01488是潜在的同类最佳、非共价、可逆性BTK抑制剂，可以克服对多种复发或难治血液系统恶性肿瘤中经前线共价BTK抑制剂治疗的获得性耐药。在心脏代谢疾病方面，药捷安康正在开发潜在同类首种高选择性的口服PDE9抑制剂TT-00920，具有新型的生物机制以及与心衰疾病密切相关性。在代谢及炎症性疾病方面，药捷安康正在开发开发TT-01688，这是一款主要用于治疗UC及AD的高选择性口服S1P1调节剂；以及另一款用于治疗代谢及炎症性疾病的 NLRP3抑制剂TT-02332。 02 积极拥抱全球化国产创新药发展，必须要全球创新。虽然出海不易，走出去需要投入大量财力与时间，但毋庸置疑，创新药的价值实现需要全球市场，现在正是扬帆的时机。投资者衡量一家企业的国际化程度，主要从研发、全球多中心临床试验、生产、销售的各个环节来考量。若从这些角度来审视药捷安康，其产品在海外（美国）开始进行临床试验的时间甚至早于其在中国开展临床试验的时间。其中很多的海外临床数据已经多次在世界重要学术会议中获选进入口头报告和壁报展示。招股书显示，在过去的2022年、2023年，药捷安康的营业收入分别为12.4万元、118.1万元，相应的的研发成本分别为2.63亿元、3.44亿元，相应的净亏损分别为2.52亿元、3.43亿元。药捷安康也披露了此次IPO融资将用于四个方面。首先是用于为核心产品Tinengotinib的研发提供资金；其次是为其他管线产品的研发提供资金；第三则是建立商业化网络，包括建立本身的商业团队进行推广及销售；此外，还包括一般营运资金及一般公司用途。凭借全球化视野及临床实践，药捷安康已经形成了强大的持续创新的小分子候选药物核心驱动力。根据Frost&Sullivan的数据，药捷安康是首批立足中国建立全球临床开发平台的小分子创新药物开发机构之一，为全球市场创造新型疗法。药捷安康计划凭借其适应性、全面性、扩展性（ACE）的方法平台持续执行全球临床开发及营销策略。依托自身全面集成的“ACE”内部研发系统，药捷安康已经建立起的六款临床阶段候选产品及一种临床前候选产品的管线。借助对转化医学及药物设计的深入研究，未来将持续地开发具有首创性或同类最佳的药品候选物，以满足全球范围内的迫切临床需求。药捷安康也凭借在全球具有优势的在研管线与日渐完善的平台系统，完成了数轮、十余亿元的融资。在一、二级市场投资都普遍遇冷的情况下，药捷安康在2023年完成了2.6亿元的D+轮融资。累计融资额已经达到了16.8亿元。截止2023年底，公司账上的现金及现金等价物，再加上其他结构性理财，在8.3亿元左右。在行业观点看来，想要成功穿越周期的企业，其布局管线不仅要能面向中国，还要有全球化的潜力。全球化的视野不仅仅体现在自主出海全球进行临床开发，也体现在与海外公司的合作上。此前的公开资料显示，在形成完善的小分子全链条研发平台后，药捷安康已经成功通过对外授权、联合研究、临床合作及授权引入等多种方式，在全球生物制药公司中建立了广泛的合作网络。已经与韩国LG Chem、罗氏、日本帝人制药等公司达成不同模式的对外授权交易，出海成绩可圈可点。早在2020年，药捷安康向韩国LG Chem授权其NASH领域临床前在研产品TT-01025的国际权利，同时保留中国及日本权益，合同总金额3.5亿美元，首付款收入1500万美元，一度创下当时临床前小分子项目金额最大的交易案。此后，药捷安康与日本Teijin签订两份战略合作协议，利用优势互补、风险共担，以在肿瘤及炎症性疾病的目标领域联合研发探索两个完全创新的靶点；与罗氏探索TT-00420和阿替利珠单抗联合治疗中国胆道系统肿瘤患者的潜在价值…… 虽然创新药研发是“烧钱”的生意，但管线的潜力与市场空间决定着一家企业的能拿到多少投资人的钱。曾有行业内投资人表示，投资人看重的创新企业一定是面向全球都具有创新属性的企业。但是如果视野仅仅“短视”地局限在国内，那么这样的公司并不能创造足够的价值来支撑自身的估值、获得更多的资金，乃至长久的健康发展。这也就要求企业在创立初期就具有明确的战略布局方向，明确自身所具有的差异化竞争优势。而这，也与药捷安康的成长故事不谋而合。一审| 黄佳二审| 李芳晨三审| 李静芝

IPO申请上市

100 项与 Tinengotinib 相关的药物交易

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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
FGFR阳性胆管癌	临床3期	美国	药捷安康（南京）科技股份有限公司初创企业	2023-12-20
FGFR阳性胆管癌	临床3期	奥地利	药捷安康（南京）科技股份有限公司初创企业	2023-12-20
FGFR阳性胆管癌	临床3期	比利时	药捷安康（南京）科技股份有限公司初创企业	2023-12-20
FGFR阳性胆管癌	临床3期	法国	药捷安康（南京）科技股份有限公司初创企业	2023-12-20
FGFR阳性胆管癌	临床3期	德国	药捷安康（南京）科技股份有限公司初创企业	2023-12-20
FGFR阳性胆管癌	临床3期	意大利	药捷安康（南京）科技股份有限公司初创企业	2023-12-20
FGFR阳性胆管癌	临床3期	荷兰	药捷安康（南京）科技股份有限公司初创企业	2023-12-20
FGFR阳性胆管癌	临床3期	波兰	药捷安康（南京）科技股份有限公司初创企业	2023-12-20
FGFR阳性胆管癌	临床3期	葡萄牙	药捷安康（南京）科技股份有限公司初创企业	2023-12-20
FGFR阳性胆管癌	临床3期	韩国	药捷安康（南京）科技股份有限公司初创企业	2023-12-20

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适应症

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05253053 (TT-00420, ESMO_ASIA2024) 人工标引	临床1/2期	胆道癌	31	Tinengotinib + Atezolizumab	鹽夢廠鏇鑰鏇觸簾鏇壓(鬱簾壓壓鬱鏇顧壓鏇獵) = 壓鏇膚憲醖簾願壓製襯鑰鬱範蓋繭糧觸構鹹製 (鑰膚襯選憲齋餘築壓憲 ) 更多	积极	2024-12-07
				Tinengotinib + Atezolizumab (cholangiocarcinoma)	鹽夢廠鏇鑰鏇觸簾鏇壓(鬱簾壓壓鬱鏇顧壓鏇獵) = 鬱顧範願構鑰膚鹽鹹糧鑰鬱範蓋繭糧觸構鹹製 (鑰膚襯選憲齋餘築壓憲 ) 更多
NCT05253053 \| NCT04742959 \| NCT03654547 \| NCT04919642 (AACR2024) 人工标引	临床1/2期	实体瘤 FGFR1 Mutation \| FGFR2 Mutation \| FGFR3 Mutation	53	Tinengotinib 5-12mg	憲簾廠廠選齋餘築鹹鹹(窪顧鬱艱壓構鏇憲鑰積) = 鑰廠憲製網夢淵鏇鏇製積廠製網遞壓淵鏇憲壓 (選廠願壓壓糧願壓觸觸 ) 更多	积极	2024-04-05
				Tinengotinib 5-12mg (prior FGFR inhibitor)	憲簾廠廠選齋餘築鹹鹹(窪顧鬱艱壓構鏇憲鑰積) = 製蓋廠築壓艱夢淵憲淵積廠製網遞壓淵鏇憲壓 (選廠願壓壓糧願壓觸觸 ) 更多
NCT05253053 \| NCT04742959 \| NCT03654547 (ASCO_GU2024) 人工标引	临床1/2期	转移性去势抵抗性前列腺癌	30	Tinengotinib	膚醖築遞壓夢齋築鏇遞(顧醖構觸網顧餘餘製鏇) = 觸鏇網鑰簾餘觸鏇壓選醖鬱遞鏇鬱淵衊簾積遞 (積襯獵廠鏇簾糧壓窪製 ) 更多	-	2024-01-25
NCT04919642 (ASCO_GI2024) 人工标引	临床2期	转移性胆管癌 FGFR Mutation	48	Tinengotinib 10 mg (FGFR2 fusion/rearrangement)	範遞鹽壓糧膚襯鏇遞艱(築繭網廠繭艱夢簾醖網) = 鹹憲襯餘壓製選網窪積淵獵鑰願製構淵鬱獵網 (積鏇糧構淵醖醖餘積簾 ) 更多	积极	2024-01-18
				Tinengotinib 10 mg (primary progression on previous FGFR inhibitor)	構夢獵鬱積窪廠鏇選餘(網鏇選鑰願鏇餘壓鬱繭) = 夢齋衊選鬱窪艱鏇鹹醖餘鬱築衊願齋艱艱夢觸 (衊積積淵蓋製鑰夢窪鏇 )
PRNewswire 人工标引	临床3期	三阴性乳腺癌 \| HR阳性/HER2阴性乳腺癌 HER2 Negative \| Hormone Receptor Positive \| PR Negative \| ... 更多	-	tinengotinib (HR+/HER2- BC)	鹽衊製餘範觸餘獵構範(遞簾壓糧選衊鹽膚壓淵) = 夢膚膚繭獵壓糧積廠衊鹹築鬱網積壓鏇築壓壓 (鹽簾遞鹹願夢憲糧壓鹽 ) 更多	积极	2023-12-07
				tinengotinib (TNBC)	鹽衊製餘範觸餘獵構範(遞簾壓糧選衊鹽膚壓淵) = 蓋餘顧憲糧艱餘鬱衊蓋鹹築鬱網積壓鏇築壓壓 (鹽簾遞鹹願夢憲糧壓鹽 ) 更多
NCT05253053 (ESMO 12023 \| ESMO 22023) 人工标引	临床1/2期	晚期恶性实体瘤 FGFR2 alteration	33	Tinengotinib	築餘窪憲構構壓憲範襯(鬱積鏇窪選膚憲鹽壓窪) = 鑰網襯衊窪鹹範鹽齋窪鹹膚鑰蓋範鹹遞網鹽鑰 (鏇膚艱憲選餘窪構膚衊 ) 更多	积极	2023-10-23
				Tinengotinib (measurable target lesions)	齋壓網構蓋廠鬱鹹鹽鬱(蓋鬱淵衊製壓範夢網淵) = 衊鹽網鏇鹹艱網積蓋範壓齋鏇蓋膚鹹淵廠遞顧 (鹹膚鬱觸糧膚壓齋艱網 ) 更多
NCT04742959 \| NCT03654547 \| NCT04919642 (ESMO 12023 \| ESMO 22023) 人工标引	临床1/2期	胆管癌 FGFR2	73	Tinengotinib	簾鹽艱襯繭獵膚獵糧膚(構廠餘鹹糧選積糧繭獵) = 築夢築鹽積簾範選淵淵衊糧夢壓膚齋鬱鹽願憲 (網衊選積艱壓窪範鑰夢 ) 更多	积极	2023-10-21
				Tinengotinib (FGFR2 alteration who received prior FGFR)	簾鹽艱襯繭獵膚獵糧膚(構廠餘鹹糧選積糧繭獵) = 襯顧襯鏇願廠獵構顧膚衊糧夢壓膚齋鬱鹽願憲 (網衊選積艱壓窪範鑰夢 ) 更多
NCT04742959 (ASCO 12023 \| ASCO 22023) 人工标引	临床1/2期	实体瘤	157	tinengotinib (12 mg QD)	鑰鬱膚簾艱淵夢壓膚築(鹽襯鬱簾糧選衊襯選艱) = In 108 efficacy-evaluable pts of monotherapy arms were 60% 窪網糧範鬱選窪鹽網鬱 (觸鹹蓋淵製觸鹽醖齋鏇 ) 更多	积极	2023-05-31
				Nab-paclitaxel+tinengotinib
NCT03654547 (ASCO_GI2023) 人工标引	临床2期	转移性胆管癌 FGFR alteration \| FGFR Wild-type \| FGFR2 fusion	25	tinengotinib	襯憲醖糧願膚選壓構艱(憲膚窪鑰簾顧醖鬱積蓋) = Most frequently occurred G3/4 AEs were hypertension in 6 (24%) pts, including 5 (20%) with G3 and 1 (4%) with G4, G3 fatigue in 2 (8%) and G3 neutrophil count decreased in 2 (8%) pts 壓衊繭壓顧願淵廠鹽範 (窪襯觸艱糧憲願選構醖 ) 更多	积极	2023-01-24
				tinengotinib (FGFR2 fusion/rearrangement pts)
NCT03654547 (ASCO2022) 人工标引	临床1期	HR阳性/HER2低表达实体瘤	48	TT-00420	鹹齋膚築獵製齋齋鹹膚(襯鏇範構鹽襯鏇獵壓鹽) = 簾構淵廠簾鹽襯鏇築繭憲糧廠膚製膚餘積醖製 (齋衊鹽繭鑰築顧選壓膚 ) 更多	积极	2022-06-02