A First-in-Human Study of Highly Selective FGFR2 Inhibitor, RLY-4008, in Patients with Intrahepatic Cholangiocarcinoma (ICC) and Other Advanced Solid Tumors

This is a Phase 1/2, open-label, FIH study designed to evaluate the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PDy), and antineoplastic activity of RLY-4008, a potent and highly selective FGFR2 inhibitor, in patients with unresectable or metastatic cholangiocarcinoma (CCA) and other solid tumors. The study consists of 4 parts: a dose escalation (Part 1), a dose expansion (Part 2), and an extension (Part 3) and a rollover (Part 4).

开始日期2020-09-02

申办/合作机构

Relay Therapeutics, Inc.

100 项与 Lirafugratinib 相关的临床结果

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100 项与 Lirafugratinib 相关的转化医学

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100 项与 Lirafugratinib 相关的专利（医药）

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项与 Lirafugratinib 相关的文献（医药）

2024-11-01·CLINICAL CANCER RESEARCH

Understanding and Overcoming Resistance to Selective FGFR Inhibitors across FGFR2-Driven Malignancies

Article

作者: Tselikas, Lambros ; André, Fabrice ; Nobre, Catline ; Loriot, Yohann ; Olaussen, Ken A. ; Hollebecque, Antoine ; Combarel, David ; Facchinetti, Francesco ; Friboulet, Luc ; Barbé, Rémy ; Michiels, Stefan ; Scoazec, Jean-Yves ; Bigot, Ludovic ; Smolenschi, Cristina ; Bahleda, Rastislav ; Italiano, Antoine ; Besse, Benjamin ; Brayé, Floriane ; Vasseur, Damien ; Ponce-Aix, Santiago

Abstract:

Purpose::

Understanding resistance to selective FGFR inhibitors is crucial to improve the clinical outcomes of patients with FGFR2-driven malignancies.

Experimental Design::

We analyzed sequential ctDNA, ± whole-exome sequencing, or targeted next-generation sequencing on tissue biopsies from patients with tumors harboring activating FGFR2 alterations progressing on pan-FGFR–selective inhibitors, collected in the prospective UNLOCK program. FGFR2::BICC1 Ba/F3 and patient-derived xenograft models were used for functional studies.

Results::

Thirty-six patients were included. In cholangiocarcinoma, at resistance to both reversible inhibitors (e.g., pemigatinib and erdafitinib) and the irreversible inhibitor futibatinib, polyclonal FGFR2 kinase domain mutations were frequent (14/27 patients). Tumors other than cholangiocarcinoma shared the same mutated FGFR2 residues, but polyclonality was rare (1/9 patients). At resistance to reversible inhibitors, 14 residues in the FGFR2 kinase domain were mutated—after futibatinib, only the molecular brake N550 and the gatekeeper V565. Off-target alterations in PI3K/mTOR and MAPK pathways were found in 11 patients, often together with on-target mutations. At progression to a first FGFR inhibitor, 12 patients received futibatinib or lirafugratinib (irreversible inhibitors), with variable clinical outcomes depending on previous resistance mechanisms. Two patients with TSC1 or PIK3CA mutations benefited from everolimus. In cell viability assays on Ba/F3 and in pharmacologic studies on patient-derived xenografts, irreversible inhibitors retained better activity against FGFR2 kinase domain mutations, with lirafugratinib active against the recalcitrant V565L/F/Y.

Conclusions::

At progression to FGFR inhibitors, FGFR2-driven malignancies are characterized by high intra- and interpatient molecular heterogeneity, particularly in cholangiocarcinoma. Resistance to FGFR inhibitors can be overcome by sequential, molecularly oriented treatment strategies across FGFR2-driven tumors.

2023-09-06·Cancer discovery

FGFR Inhibition: Understanding and Overcoming Resistance.

Communications

作者: Pal, Sumanta K ; Tripathi, Abhishek ; Li, Daneng

SUMMARY:

Facchinetti and colleagues provide key insights into the evolution of resistance to fibroblast growth factor receptor (FGFR) inhibitors, including the development of kinase domain mutations and activation of the PI3K-AKT signaling axis. In a separate study, Subbiah and colleagues report extensive preclinical data and initial clinical data for RLY-4008, an FGFR2-selective inhibitor that is poised to minimize toxicity and overcome resistance through greater potency and selectivity. See related article by Facchinetti et al., p. 1998 (5). See related article by Subbiah et al., p. 2012 (7).

2023-09-06·Cancer discovery

RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity acrossFGFR2Alterations and Resistance Mutations

Article

作者: Foster, Lindsey ; Taylor, Alexander M. ; Jen, Kai Yu ; Gunaydin, Hakan ; Sherwin, Cori Ann ; Hudson, Brandi M. ; Moustakas, Demetri T. ; Schmidt-Kittler, Oleg ; Houde, Damian J. ; Gerami-Moayed, Nastaran ; Casaletto, Jessica B. ; Schram, Alison M. ; Shaw, David E. ; Schönherr, Heike ; Touré, B. Barry ; Pal, Debjani ; Sharon, Dina A. ; O'Hearn, Patrick J. ; Valverde, Roberto ; Kamath, Suneel ; Ayaz, Pelin ; Ricard, Fabien ; Maglic, Dejan ; Goyal, Lipika ; Wolf, Beni B. ; Bergstrom, Donald A. ; Subbiah, Vivek ; Zhao, Songping ; Sahai, Vaibhav ; Watters, James ; Bruderek, Kamil

Abstract:

Oncogenic activation of fibroblast growth factor receptor 2 (FGFR2) drives multiple cancers and represents a broad therapeutic opportunity, yet selective targeting of FGFR2 has not been achieved. Although the clinical efficacy of pan-FGFR inhibitors (pan-FGFRi) validates FGFR2 driver status in FGFR2 fusion–positive intrahepatic cholangiocarcinoma, their benefit is limited by incomplete target coverage due to FGFR1- and FGFR4-mediated toxicities (hyperphosphatemia and diarrhea, respectively) and the emergence of FGFR2 resistance mutations. RLY-4008 is a highly selective, irreversible FGFR2 inhibitor designed to overcome these limitations. In vitro, RLY-4008 demonstrates >250- and >5,000-fold selectivity over FGFR1 and FGFR4, respectively, and targets primary alterations and resistance mutations. In vivo, RLY-4008 induces regression in multiple xenograft models—including models with FGFR2 resistance mutations that drive clinical progression on current pan-FGFRi—while sparing FGFR1 and FGFR4. In early clinical testing, RLY-4008 induced responses without clinically significant off-isoform FGFR toxicities, confirming the broad therapeutic potential of selective FGFR2 targeting.

Significance::

Patients with FGFR2-driven cancers derive limited benefit from pan-FGFRi due to multiple FGFR1–4-mediated toxicities and acquired FGFR2 resistance mutations. RLY-4008 is a highly selective FGFR2 inhibitor that targets primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs, suggesting it may have broad therapeutic potential.See related commentary by Tripathi et al., p. 1964.This article is featured in Selected Articles from This Issue, p. 1949

项与 Lirafugratinib 相关的新闻（医药）

2024-12-09

·GlobeNewswire-Health Care

Relay Therapeutics to Present Updated Clinical Data on RLY-2608 in HR+/HER2- Breast Cancer at 2024 San Antonio Breast Cancer Symposium

Company to host conference call on Wednesday, December 11, 2024 at 7am ETCAMBRIDGE, Mass., Dec. 09, 2024 (GLOBE NEWSWIRE) -- Relay Therapeutics, Inc. (Nasdaq: RLAY), a clinical-stage precision medicine company transforming the drug discovery process by combining leading-edge computational and experimental technologies, today announced that updated clinical data for RLY-2608 600mg BID + fulvestrant in patients with PI3Kα-mutated, HR+, HER2- locally advanced or metastatic breast cancer will be presented at the upcoming San Antonio Breast Cancer Symposium, taking place December 10-13, 2024. Details of the RLY-2608 + fulvestrant poster presentation are as follows:Abstract Title: PS7-01: Efficacy of RLY-2608, a mutant-selective PI3Kα inhibitor in patients with PIK3CA-mutant HR+HER2- advanced breast cancer: ReDiscover trialAbstract Number: SESS-2211Session: Concurrent Poster Spotlight Session 7: Targeting the ER and PI3K pathway: Novel drugs and combinationsDate/Time: Wednesday, December 11, 8:00-9:30 a.m. ET (7:00-8:30 a.m. CT) Conference Call InformationRelay Therapeutics will host a conference call to discuss these data on Wednesday, December 11, 2024 at 7:00 a.m. ET (6:00 a.m. CT). Registration and dial-in for the conference call and webcast may be accessed through Relay Therapeutics’ website under Events in the News & Events section through the following link: https://ir.relaytx.com/news-events/events-presentations. An archived replay of the webcast will be available following the event. The poster will be available at the start of the session on the company’s website at https://relaytx.com/publications/. About RLY-2608 RLY-2608 is the lead program in Relay Therapeutics’ efforts to discover and develop mutant selective inhibitors of PI3Kα, the most frequently mutated kinase in all cancers, with oncogenic mutations detected in about 14% of patients with solid tumors. RLY-2608 has the potential, if approved, to address more than 300,000 patients per year in the United States, one of the largest patient populations for a precision oncology medicine. Traditionally, the development of PI3Kα inhibitors has focused on the active, or orthosteric, site. The therapeutic index of orthosteric inhibitors is limited by the lack of clinically meaningful selectivity for mutant versus wild-type (WT) PI3Kα and off-isoform activity. Toxicity related to inhibition of WT PI3Kα and other PI3K isoforms results in sub-optimal inhibition of mutant PI3Kα with reductions in dose intensity and frequent discontinuation. The Dynamo® platform enabled the discovery of RLY-2608, the first known allosteric, pan-mutant, and isoform-selective PI3Kα inhibitor, designed to overcome these limitations. Relay Therapeutics solved the full-length cryo-EM structure of PI3Kα, performed computational long time-scale molecular dynamic simulations to elucidate conformational differences between WT and mutant PI3Kα, and leveraged these insights to support the design of RLY-2608. RLY-2608 is currently being evaluated in a first-in-human trial designed to treat patients with advanced solid tumors with a PIK3CA (PI3Kα) mutation. For more information on RLY-2608, please visit here. About Relay Therapeutics Relay Therapeutics is a clinical-stage precision medicine company transforming the drug discovery process by combining leading-edge computational and experimental technologies with the goal of bringing life-changing therapies to patients. As the first of a new breed of biotech created at the intersection of complementary techniques and technologies, Relay Therapeutics aims to push the boundaries of what’s possible in drug discovery. Its Dynamo® platform integrates an array of leading-edge computational and experimental approaches designed to drug protein targets that have previously been intractable or inadequately addressed. Relay Therapeutics’ initial focus is on enhancing small molecule therapeutic discovery in targeted oncology and genetic disease indications. For more information, please visit www.relaytx.com or follow us on Twitter. Cautionary Note Regarding Forward-Looking Statements This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995, as amended, including, without limitation, implied and express statements regarding Relay Therapeutics’ strategy, business plans and focus; the progress and timing of the clinical development of the programs across Relay Therapeutics’ portfolio; the expected therapeutic benefits and potential efficacy and tolerability of RLY-2608, both as a monotherapy and in combination with other agents, and its other programs, including lirafugratinib as well as the clinical data for RLY-2608; the interactions with regulatory authorities and any related approvals; the potential market opportunity for RLY-2608; the cash runway projection and the expectations regarding Relay Therapeutics’ use of capital, expenses and potential cost savings. The words “may,” “might,” “will,” “could,” “would,” “should,” “plan,” “anticipate,” “intend,” “believe,” “expect,” “estimate,” “seek,” “predict,” “future,” “project,” “potential,” “continue,” “target” and similar words or expressions, or the negative thereof, are intended to identify forward-looking statements, although not all forward-looking statements contain these identifying words. Any forward-looking statements in this press release are based on management's current expectations and beliefs and are subject to a number of risks, uncertainties and important factors that may cause actual events or results to differ materially from those expressed or implied by any forward-looking statements contained in this press release, including, without limitation, risks associated with: the impact of global economic uncertainty, geopolitical instability and conflicts, or public health epidemics or outbreaks of an infectious disease on countries or regions in which Relay Therapeutics has operations or does business, as well as on the timing and anticipated results of its clinical trials, strategy, future operations and profitability; the delay or pause of any current or planned clinical trials or the development of Relay Therapeutics’ drug candidates; the risk that the preliminary or interim results of its preclinical or clinical trials may not be predictive of future or final results in connection with future clinical trials of its product candidates and that interim and early clinical data may change as more patient data become available and are subject to audit and verification procedures; Relay Therapeutics’ ability to successfully demonstrate the safety and efficacy of its drug candidates; the timing and outcome of its planned interactions with regulatory authorities; and obtaining, maintaining and protecting its intellectual property. These and other risks and uncertainties are described in greater detail in the section entitled “Risk Factors” in Relay Therapeutics’ most recent Annual Report on Form 10-K and Quarterly Report on Form 10-Q, as well as any subsequent filings with the Securities and Exchange Commission. In addition, any forward-looking statements represent Relay Therapeutics' views only as of today and should not be relied upon as representing its views as of any subsequent date. Relay Therapeutics explicitly disclaims any obligation to update any forward-looking statements. No representations or warranties (expressed or implied) are made about the accuracy of any such forward-looking statements. Contact:Megan Goulart617-322-0814mgoulart@relaytx.com Media:Dan Budwick1AB973-271-6085dan@1abmedia.com

临床研究

2024-12-06

·生物制药小编

无意开发的管线，卖给了韩国药企

近日，Relay Therapeutics与Elevar Therapeutics达成一项全球许可协议。 Relay以7500万美元+4.25亿美元商业里程碑付款+10%的分层特许权使用费将其RLY-4008的全球独家开发和商业化权益出售给Elevar，此后Elevar将负责lirafugratinib在全球范围内的研发和商业化。把RLY-4008卖掉后，目前Relay仅剩下一条临床阶段管线了。反正是卖出去了 RLY-4008是一种高选择性的FGFR2不可逆口服小分子抑制剂，是公司最快的管线，已经推进到NDA准备阶段。但是即便如此，把RLY-4008成功卖出去应该是Relay能想到的最好的方案了。去年10月，Relay曾宣布暂停对RLY-4008的开发，公开的官方原因是美国政府推行的《通货膨胀削减法案》。因为IRA而停止开发，这似乎是一个说不太通的理由。因为在此之前，RLY-4008展现的临床数据还算积极，在70mg剂量组中，RLY-4008的客观缓解率达到了88%，并且所有获得缓解的患者仍持续呈现缓解状态，部分缓解的患者肿瘤缩小至少30%。该临床数据公布后，公司股价还应声上涨23.75%。不过当时也有读者留言，或许是因为RLY-4008的临床数据并不如表面积极，因此找了个理由停止。不论如何，Relay好歹是把RLY-4008卖出去了，至少拿到了首付款。出变故的管线 Relay是一家AI药物发现公司，成立于2016年，2020年在纳斯达克交易市场上市。 Relay创立了一个基于分子动力学模拟技术平台Dynamo，来发现处于动态变化突变蛋白结合口袋，对难以成药靶点进行开发。 Relay曾有三条进入临床的管线，分别为FGFR2抑制剂RLY-4008、SHP2抑制剂RLY-1971、以及PI3Kα抑制剂RLY-2608。然而，在经历了一系列的变故后，目前仅剩RLY-2608这一条临床阶段管线在研。 2023年10月，Relay宣布暂停一款临床前管线CDK2抑制剂RLY-2139的开发。 RLY-1971则是在今年7月被基因泰克无故退货，里程碑付款泡汤。目前，RLY-1971已不在Relay研发管线之中，大概率已经被彻底放弃了。仅剩的一条临床阶段管线RLY-2608也没令人省心，去年AACR会议上公布的临床I期有效性不佳，导致公司股价暴跌36%，还在盘中交易触发了熔断机制。目前看来Relay并不缺钱，截至2024年9月30日，Relay帐上趴着的现金、现金等价物、投资等价物8.396亿美元，预计足以支持公司运营至2027年下半年。不过为了节省开支，今年以来，Relay已经宣布了两轮裁员，共计影响了15%的员工。 Relay采取的融资途径也十分明确，基本都是趁着每一次积极临床数据公布进行股票公开发行。 2022年，Relay公布的RLY-4008初步临床试验数据后，Relay趁势公开发行1100万股普通股，总金额约为3亿美元。今年9月，RLY-2608+fulvestrant公布了治疗HR+/HER2-乳腺癌的I/II期中期数据后，Relay又趁势公开发行2亿美元的普通股。参考出处 https://www.stocktitan.net/news/RLAY/relay-therapeutics-and-elevar-therapeutics-announce-exclusive-global-ujtspmggqb7y.html https://endpts.com/relay-licenses-lirafugratinib-to-elevar-for-75m/ /

AACR会议临床1期引进/卖出

2024-12-05

·医药速览

昨夜，聚焦韩国！5亿美金，一韩国药企从美药企Relay囊获在研口服小分子药

昨夜，Relay Therapeutics 决定将一种针对罕见癌症的资产开发工作，交寄给韩国药企 Elevar Therapeutics。双方签署了价值高达5亿美元的许可协议，Relay Therapeutics将获得7500万美元的里程碑付款，以及高达4.25亿美元的潜在商业里程碑付款和特许权使用费。根据该协议，Elevar 将获得一种用于治疗实体瘤的研究性口服小分子药物——lirafugratinib（RLY-4008）的全球独家开发和商业化权利。 Lirafugratinib 是一种成纤维细胞生长因子受体2（FGFR2）抑制剂，已在胆管癌（CCA）及其他FGFR2改变的实体瘤治疗中展现出潜力。总部位于韩国的Elevar Therapeutics，将负责lirafugratinib的所有后续活动，包括新药批准（NDA）提交、以及该药物在全球范围内的商业化，特别是在FGFR2驱动的胆管癌（CCA）和其他FGFR2改变的实体瘤中的应用。值得注意的是，lirafugratinib 已获得FDA的突破性疗法和孤儿药标签，这为其未来的开发和商业化提供了有力支持。早在2023年10月，Relay Therapeutics 曾因《通货膨胀削减法案》的影响而暂停了在CCA中将lirafugratinib推向市场的计划。随着新数据的出现，显示该候选药物可能适用于罕见胆管癌以外的其他癌症，公司的策略发生了转变。目前，lirafugratinib 正在全球范围内进行1/2期试验，研究对象为FGFR2突变肿瘤患者，包括FGFR2融合CCA的关键队列，该队列旨在支持加速批准并已完全入组。 Elevar Therapeutics 收购lirafugratinib，将使Relay Therapeutics 能够专注于PI3Kα，及明年启动的一项乳腺癌试验。在经历了两轮裁员、7月失去罗氏这个关键合作伙伴后，与韩国药企的这次交易交易，无疑将为Relay Therapeutics 带来一丝喘息的机会。对Elevar Therapeutics 来说，也算是提供了一个宝贵的机会，通过开发和商业化lirafugratinib，在罕见癌症治疗领域取得突破。参考消息： https://endpts.com/relay-licenses-lirafugratinib-to-elevar-for-75m/ 免责声明本文旨在行业资讯和知识分享，无任何商业用途。文章仅代表作者观点，不代表本站立场。往期推荐 1.刚刚！信迪利单抗（信达生物）与呋喹替尼（和黄医药）的联合疗法获批上市，适用于子宫内膜癌 2.2024医药公司市值回顾：两极分化！礼来领跑，辉瑞、默克等面临挑战 3.九源基因港股上市，首日大跌 4.强生裁员赔偿细节公开！7年拿40万赔偿，相当慷慨！ 5.Cell子刊丨中山大学团队揭示lncRNA调控核仁朊病毒样蛋白质液-固相转变的新机制往期链接 “小小疫苗”养成记 | 医药公司管线盘点人人学懂免疫学 | 人人学懂免疫学（语音版）综述文章解读 | 文献略读 | 医学科普 | 医药前沿笔记 PROTAC技术 | 抗体药物 | 抗体药物偶联-ADC 核酸疫苗 | CAR技术 | 化学生物学温馨提示医药速览公众号目前已经有近12个交流群（好学，有趣且奔波于医药圈人才聚集于此）。进群加作者微信（yiyaoxueshu666）或者扫描公众号二维码添加作者，备注“姓名/昵称-企业/高校-具体研究领域/专业”，此群仅为科研交流群，非诚勿扰。简单操作即可星标⭐️医药速览，第一时间收到我们的推送 ①点击标题下方“医药速览” ②至右上角“...” ③点击“设为星标

引进/卖出疫苗并购突破性疗法孤儿药

100 项与 Lirafugratinib 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
晚期恶性实体瘤	临床2期	美国	Relay Therapeutics, Inc.	2020-09-02
晚期恶性实体瘤	临床2期	澳大利亚	Relay Therapeutics, Inc.	2020-09-02
晚期恶性实体瘤	临床2期	法国	Relay Therapeutics, Inc.	2020-09-02
晚期恶性实体瘤	临床2期	德国	Relay Therapeutics, Inc.	2020-09-02
晚期恶性实体瘤	临床2期	中国香港	Relay Therapeutics, Inc.	2020-09-02
晚期恶性实体瘤	临床2期	意大利	Relay Therapeutics, Inc.	2020-09-02
晚期恶性实体瘤	临床2期	荷兰	Relay Therapeutics, Inc.	2020-09-02
晚期恶性实体瘤	临床2期	新加坡	Relay Therapeutics, Inc.	2020-09-02
晚期恶性实体瘤	临床2期	韩国	Relay Therapeutics, Inc.	2020-09-02
晚期恶性实体瘤	临床2期	西班牙	Relay Therapeutics, Inc.	2020-09-02

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临床结果

适应症

分期

评价

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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


NCT04526106 (REFOCUS, Corporate Publications) 人工标引	临床1/2期	实体瘤 FGFR2 fusions \| FGFR2 amplifications \| FGFR2 mutations	84	Lirafugratinib (patients with FGFR2 fusions)	膚艱繭網壓網製願網鬱(蓋艱衊獵鏇糧襯憲簾糧) = 齋餘壓鹽齋網鏇鬱憲構窪醖築範範鏇醖顧積鬱 (觸齋醖獵膚構鑰壓觸夢 )	积极	2023-10-12
				Lirafugratinib (patients with breast cancer across all FGFR2 alterations, 10 of whom had HR+/HER2- breast cancer)	膚艱繭網壓網製願網鬱(蓋艱衊獵鏇糧襯憲簾糧) = 顧願淵鹹觸憲壓夢觸遞窪醖築範範鏇醖顧積鬱 (觸齋醖獵膚構鑰壓觸夢 )
NCT04526106 (ReFocus, ASCO2023) 人工标引	临床1/2期	实体瘤 \| 胆管癌	75	RLY-4008 (FGFRi-naïve CCA f/r)	廠膚糧範鹽鏇選顧鑰構(鹹範襯顧蓋簾鬱構網齋) = 70 mg QD 獵艱憲餘鏇製糧醖齋廠 (鏇鏇鹽廠醖簾壓夢糧獵 ) 更多	积极	2023-05-26
				RLY-4008 (Prior-FGFRi CCA f/r)
AACR2023	临床1/2期	-	-	RLY-4008 (fasted)	餘獵構蓋遞艱淵廠襯構(製遞構衊築鹽築醖鑰鏇) = 網糧鹹鹽鹽齋簾壓構鹹艱觸鹽襯蓋蓋壓襯壓醖 (顧觸廠鹽範窪鏇獵範鑰 )	-	2023-04-04
				RLY-4008 with food	餘獵構蓋遞艱淵廠襯構(製遞構衊築鹽築醖鑰鏇) = 憲廠遞積顧網獵製蓋醖艱觸鹽襯蓋蓋壓襯壓醖 (顧觸廠鹽範窪鏇獵範鑰 )
NCT04526106 (ReFocus, ESMO_ASIA2022)	临床1/2期	FGFR2融合或重排的胆管癌	38	RLY-4008	積衊觸艱簾獵鏇構築鹹(壓構選艱簾淵鹽選鬱獵) = majority of responses ongoing 鹽襯構襯廠鏇構網窪遞 (獵願襯築構範蓋範膚繭 )	-	2022-12-04
NCT04526106 (ReFocus, ESMO2022) 人工标引	临床1/2期	胆管癌一线 FGFR2-fusion/FGFR2rearrangement	195	RLY-4008 20-200 mg QD or BID (RP2D (70 mg QD))	鬱選淵鬱製齋蓋顧選夢(齋膚廠窪膚衊鑰襯獵構) = 願簾簾窪遞窪範齋鏇齋觸遞繭範觸簾積願襯獵 (淵夢鹽積窪鏇蓋築製顧, 56.6 ~ 96.2) 更多	积极	2022-09-11
				RLY-4008 20-200 mg QD or BID (All dose levels)	鬱選淵鬱製齋蓋顧選夢(齋膚廠窪膚衊鑰襯獵構) = 範積襯獵窪衊繭鹹簾淵觸遞繭範觸簾積願襯獵 (淵夢鹽積窪鏇蓋築製顧, 40.8 ~ 73.7) 更多
NCT04526106 (ReFocus, AACR2021) 人工标引	临床1/2期	实体瘤 \| FGFR2融合或重排的胆管癌 FGFR2 Mutation	45	RLY-4008	構憲選築繭鏇簾壓積齋(鑰淵餘獵鹹襯齋鹹夢壓) = AEs occurring in >20% of pts include stomatitis (49%), palmar-plantar erythrodysesthesia (PPE, 38%), dry mouth (29%), and nail toxicities (22%), majority of which were ≤Gr 2. 膚獵齋鬱鹽衊艱觸蓋鬱 (膚窪壓願鑰簾範夢築鏇 ) 更多	积极	2021-12-01
				RLY-4008 (FGFRi-naïve, FGFR2-fusion+ CCA)