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

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

NCT05948475 / Recruiting临床3期

A Phase III, Randomized, Controlled, Global Multicenter Study to Evaluate the Efficacy and Safety of Oral Tinengotinib VS Physician's Choice in Subjects With FGFR-altered, Chemotherapy- and FGFR Inhibitor-Cholangiocarcinoma

This study is 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

开始日期2023-12-20

申办/合作机构

药捷安康（南京）科技股份有限公司初创企业

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）

2024-04-04·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 ; Mott, Frank ; Xu, Binghe ; 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 ; Javle, Milind M ; Fu, Siqing ; 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.

2023-02-01·Molecular cancer therapeutics

Tinengotinib (TT-00420), a Novel Spectrum-Selective Small-Molecule Kinase Inhibitor, Is Highly Active Against Triple-Negative Breast Cancer

Article

作者: Li, Guoyu ; Wu, Di ; Qiang, Xiaoyan ; Hu, Chao ; Yu, Qi ; Li, Lin ; Peng, Peng ; Sourd, Laura ; Wang, Dong ; Wu, Frank ; Marangoni, Elisabetta ; Ni, Shumao

Abstract:

Triple-negative breast cancer (TNBC) is a highly heterogeneous cancer lacking actionable targets. Using a phenotypic screen of TNBC cells, we discovered a novel multiple kinase inhibitor tinengotinib (TT-00420) that strongly inhibited Aurora A/B, FGFR1/2/3, VEGFRs, JAK1/2, and CSF1R in biochemical assays. Exposure to tinengotinib specifically inhibited proliferation across all subtypes of TNBC in vitro and in vivo, while leaving luminal breast cancer cells intact. Incubation of HCC1806 with tinengotinib led to dose-dependent downregulation of genes essential for TNBC cell growth and proliferation. Studies revealed that the potential mechanism of action of tinengotinib involved, predominantly, inhibition of Aurora A or B kinase activity, while inhibition of other pathways contributed to suppression of potency and activity. In vitro treatment of TNBC cell lines or in vivo administration in a syngeneic model with tinengotinib resulted in up-regulation of CXCL10 and 11 or diminished tumor-associated macrophage (TAM) infiltration. Tinengotinib represents a novel combinatorial inhibitory mechanism to treat TNBC. The phase I trial of tinengotinib was completed (ClinicalTrials.gov identifier: NCT03654547).

2022-08-01·Cellular oncology (Dordrecht)

Novel protein kinase inhibitor TT-00420 inhibits gallbladder cancer by inhibiting JNK/JUN-mediated signaling pathway

Article

作者: Yang, Mao ; Peng, Peng ; Li, Weijian ; Zhang, Dadong ; Liu, Liguo ; He, Yongning ; Tang, Shijie ; Geng, Yajun ; Li, Yongsheng ; Jiang, Xiaoqing ; Chen, Luonan ; Zhang, Rui ; Liu, Yingbin ; Qiang, Xiaoyan ; Zou, Lu ; Miao, Huijie ; Qiu, Shimei ; Wu, Ying ; Wang, Zeyu ; Liu, Ke ; Li, Yang ; Zhao, Yuhao ; Li, Maolan ; Li, Zhizhen ; Liu, Yun ; Feng, Feiling ; Wang, Ziyi ; Shao, Ziyu ; Chen, Chen ; Wu, Frank ; Xiang, Dongxi

PURPOSE:

This study aimed to investigate the efficiency of our chemically synthesized TT-00420, a novel spectrum-selective multiple protein kinase inhibitor, in cultured cells and animal models of gallbladder cancer (GBC) and explore its potential mechanism.

METHODS:

Multiple GBC models were established to assess the anti-tumor efficiency, toxicity, and pharmacokinetics of TT-00420. Integrated transcriptomic, proteomic and phosphoproteomic analysis was conducted to identify potential downstream effectors of TT-00420. Western blotting, qRT-PCR, nuclear-cytoplasm separation, and immunofluorescence were performed to confirm the multi-omic results and explore the molecular mechanism of TT-00420. Immunohistochemistry was used to detect FGFR1 and p-FGFR1 expression levels in GBC samples. Autodock software was utilized to investigate the potential binding mode between the TT-00420 and the human FGFR1.

RESULTS:

We found that TT-00420 exerted potent growth inhibition of GBC cell lines and multiple xenograft models. Treatment of mice with 15 mg/kg TT-00420 via gavage displayed a half-life of 1.8 h in the blood and rapid distribution to the liver, kidneys, lungs, spleen, and tumors at 0.25 h, but no toxicity to these organs over 2 weeks. Multi-omic analysis revealed c-Jun as a potential downstream effector after TT-00420 treatment. Mechanistically, TT-00420 showed rigorous ability to block FGFR1 and its downstream JNK-JUN (S63/S73) signaling pathway, and induce c-Jun S243-dependent MEK/ERK reactivation, leading to FASLG-dependent tumor cell death. Finally, we found that FGFR1 and p-FGFR1 expression was elevated in GBC patients and these levels correlated with decreased patient survival.

CONCLUSIONS:

TT-00420 shows potent antitumor efficacy and may serve as a novel agent to improve GBC prognosis.

项与 Tinengotinib 相关的新闻（医药）

2024-04-18

·药渡Daily

【药渡药闻报告-创新药篇】-2024年第14期/总第135期

全球药物批准/研发动态01全球新药批准情况根据药渡数据统计分析，本次统计周期（2024.04.06-04.12）全球（不含中国）共有4个新药获批上市。其中，BLA批准1个，新适应症批准3个。与上个统计周期相比，本次减少2个批准新药。4月11日，艾伯维（AbbVie）银屑病治疗药物Skyrizi（Risankizumab）获MFDS的批准，用于治疗对标准疗法反应不足或不耐受的成年人（18岁及以上）的中度至重度手足脓疱型银屑病。作为一种维持疗法，Skyrizi在牛皮癣患者中表现出高度的皮肤改善和持续改善，每12周给药一次150毫克剂量，每年四次。Skyrizi在中度至重度斑块状银屑病和银屑病关节炎中显示出显著疗效，将为手掌脓包病患者提供新的治疗选择。4月11日，AstraZeneca的Fasenra®（Benralizumab）获得FDA批准，用于治疗6至11岁嗜酸性粒细胞表型严重哮喘患者的附加维持治疗。Benralizumab于2017年首次被批准作为治疗12岁及以上严重嗜酸性粒细胞性哮喘（SEA）的附加维持治疗。Benralizumab的这一额外适应症得到了TATE的证据支持：Benralizumab达到了主要终点，证明6至11岁SEA儿童的药代动力学（PK）和药效学（PD）与先前试验中观察到的一致。Benralizumab目前在美国被批准作为6岁及以上SEA患者的附加维持治疗。全球（不含中国）新药批准情况（部分）02全球新药申报进展根据药渡数据统计分析，本次统计周期（2024.04.06-04.12）全球（不含中国）共有2个新药申报上市。其中，NDA申报进展2个。与上次统计周期相比，本次减少2个NDA/BLA申报。4月8日，Stealth宣布FDA接受Elamipretide用于治疗Barth综合征的新药申请。该NDA得到了SPIBA-001 III期自然病程对照研究的积极数据和TAZPOWER第2部分基线对照试验的额外支持疗效和安全性数据的支持。Elamipretide于2017年获得快速通道资格认定，2018年获得孤儿药资格认定，2020年获得罕见儿科疾病认定。NDA/BLA申报情况根据药渡数据统计分析，本次统计周期（2024.04.06-04.12）全球（不含中国）共有9个药物获监管机构特殊资格认定。其中，化学药5个，生物药4个。与上次统计周期相比，本次增加8个获监管机构特殊资格认定的药物。4月7日，迪哲医药宣布FDA授予其首款自主研发的新型肺癌靶向药舒沃哲®突破性疗法认定，用于一线治疗携带表皮生长因子受体（EGFR）20号外显子插入（exon20ins）突变的晚期非小细胞肺癌（NSCLC）患者。舒沃哲®于2023年8月在中国通过优先审评首发上市是目前全球唯一获批针对EGFR exon20ins突变型晚期NSCLC的小分子TKI。4月9日，同宜医药宣布自主研发的第二代Bi-XDC双配体偶联药物CBP-1019已经获得FDA孤儿药资格认定，用于治疗食管癌。这是CBP-1019继去年9月获得FDA孤儿药资格认定用于治疗胰腺癌后的又一次认可。连续获得两个适应症的孤儿药资格认定将有助于CBP-1019在美国的注册申报、临床开展及商业化进程加速推进。特殊资格认定情况（部分）03全球新药研发进展根据药渡数据统计分析，本次统计周期（2024.04.06-04.12）全球（不含中国）新药临床研发状态更新共计54条，涉及肿瘤、血液和淋巴疾病、遗传代谢病、精神疾病、皮肤病以及眼部疾病等共计11个领域。其中，肿瘤领域临床进展更新居各领域之首，涉及化学药18条，生物药8条，细胞疗法1条，疫苗2条。4月8日，三叶草生物公布其二价RSV候选疫苗SCB-1019 I期临床试验首批年轻成年人群组获得积极初步数据：SCB-1019诱导的RSV-A和RSV-B中和滴度水平显著提高，分别达到约6,600 IU/mL（提高6.4倍）和约46,000IU/mL（提高12倍）。老年人群入组I期临床试验也已顺利如期推进，初步数据将于2024年下半年公布。4月12日，药捷安康宣布在2024年AACR上公开Tinengotinib针对携带FGFR1-3变异晚期泛实体瘤（单药）的最新研究成果并入选突破性研究。Tinengotinib针对多种癌症都有疗效信号，包括胆管癌、乳腺癌、前列腺癌、尿路上皮癌、结肠癌及头颈癌，疗效为BOR 33.3%，DCR 88.2%，mPFS 6.90个月。Tinengotinib已获得FDA孤儿药认证及快速通道资格认证， EMA孤儿药认证；NMPA批准纳入突破性治疗品种名单。全球新药研发进展详情（部分）04全球医药交易事件本次统计周期（2024.04.06-04.12）全球（含中国）医药交易时间共计21起，涉及药物权益转让、公司并购等多起交易事件。全球医药交易时间汇总表（部分）国内药物批准/研发动态国内药物批准/研发动态01国内新药批准情况根据药渡数据统计分析，本次统计周期（2024.04.06-04.12）国内共有6个新药获NMPA批准上市。其中，BLA批准2个，新适应症批准2个，新剂型批准2个。与上次统计周期相比，本次增加3个NMPA批准新药。4月7日，君实生物宣布，由公司自主研发的抗PD-1单抗药物特瑞普利单抗注射液（拓益®）联合阿昔替尼用于中高危的不可切除或转移性肾细胞癌患者的一线治疗新适应症上市申请于近日获得NMPA批准。这是特瑞普利单抗在中国获批的第八项适应症，也是我国首个获批的肾癌免疫疗法。此次新适应症的获批主要基于RENOTORCH研究（NCT04394975）的数据结果，这是我国首个晚期肾癌免疫治疗的关键III期临床研究。4月11日，三生制药宣布NMPA已于4月2日批准重组人血小板生成素注射液（特比澳®）新适应症，用于治疗儿童或青少年的持续性或慢性原发免疫性血小板减少症（ITP）。此前特比澳®已获批成人实体瘤化疗后血小板减少症（CIT）和成人原发免疫性血小板减少症（ITP）适应症。目前，重组人血小板生成素注射液是中国ITP指南推荐首选的二线治疗药物。中国新药批准情况（部分）02国内新药临床默示许可进展根据药渡数据统计分析，本次统计周期（2024.04.06-04.12）国内共有38个新药获临床默示许可，涉及53个受理号。其中，化学药20个，治疗用生物制品18个。与上个统计周期相比，本次减少17个临床默示许可获批受理号。本周国内新药临床默示许可进展（部分）03国内新药申报进展根据药渡数据统计分析，本次统计周期（2024.04.06-04.12）国内共有8个新药申报上市，涉及14个受理号。其中，化学药4个，治疗用生物制品3个，预防用生物制品1个。与上个统计周期相比，本次增加2个新药申报上市受理号。国内新药申报上市情况（部分）根据药渡数据统计分析，本次统计周期（2024.04.06-04.12）国内共有37个新药申报临床，涉及56个受理号。其中，化学药17个，治疗用生物制品19个，预防用生物制品1个。与上个统计周期相比，本次增加20个临床申报受理号。国内新药临床申报情况（部分）根据药渡数据统计分析，本次统计周期（2024.04.06-04.12）国内共有2个药物获NMPA特殊资格认定。其中，化学药1个，生物药1个。与上个统计周期相比，本次增加1个获监管机构特殊资格认定的药物。4月9日，中国国家药监局药品审评中心（CDE）官网公示，百利天恒申报的注射用BL-B01D1拟纳入突破性治疗品种，针对适应症为既往经PD-1/PD-L1单抗治疗且经至少两线化疗（至少一线含铂）治疗失败的复发性或转移性鼻咽癌患者。公开资料显示，BL-B01D1是一款EGFR×HER3双特异性抗体偶联药物（ADC）。该产品治疗鼻咽癌的III期临床研究目前正在进行中。BL-B01D1是一种基于双特异性拓扑异构酶抑制剂的ADC，可同时靶向作用于表皮生长因子受体和人表皮生长因子受体3（EGFR×HER3），二者在大多数上皮性肿瘤中高度表达。BL-B01D1已经开展了多个I期临床研究。肿瘤评估数据显示，该产品已经在12种肿瘤中均有强烈的有效性信号，且在II期推荐剂量（RP2D）下具有良好的安全性。其中针对非小细胞肺癌及晚期或转移性鼻咽癌表现出突破性疗效。NMPA特殊资格认定情况（部分）04国内新药研发进展根据药渡数据统计分析，本次统计周期（2024.04.06-04.12）国内新药临床研发状态更新共计11条，涉及肿瘤、遗传代谢病和皮肤病等共计6个领域。其中，化学药3个，生物药8个。4月8日，康方生物研发的PD-1/CTLA-4双特异性抗体开坦尼®（卡度尼利单抗注射液）联合奥沙利铂和卡培他滨用于一线治疗不可手术切除的局部晚期复发或转移性胃或胃食管结合部（G/GEJ）腺癌的III期临床研究（AK104-302/COMPASSION-15）的期中分析阳性结果在2024年AACR上以口头报告（Oral）的形式重磅发布。COMPASSION-15研究是全球首个PD-1/CTLA-4双特异性抗体联合化疗一线治疗胃癌的III期临床研究。研究结果显示，卡度尼利联合方案对比化疗可大幅度延长患者的总生存获益和降低死亡风险，对于肿瘤治疗客观缓解和远期生存的获益非常突出。即使对于PD-L1低表达人群也具有同样优异的疗效，有望弥补当下PD-1单抗一线治疗PD-L1低表达胃癌疗效有限的短板，为晚期胃癌患者提供更为全面高效的免疫治疗方案。国内新药研发进展情况（部分）05国内新药研发领域政策法规动态本周无新药研发领域政策法规发布。06国内新药研发领域热点新闻迈威生物，下一个Biotech盈利新星？医药市场波谲云诡，无数Biotech企业都在试图从白热化的竞争中脱颖而出。然而，迈威生物却以半年涨幅高达150%，成为资本市场“最靓的仔”。近日，迈威生物公布2023年财报：实现总营收1.28亿元，同比激增361.03%，再次被推至市场聚光灯下。然而，面对激烈的市场竞争，迈威生物能否保持强劲的发展势头？其研发的创新药又能否成功‘出海’，成为公司扭亏为盈的关键？这些都是市场关注的焦点。更多资讯，请阅读原文咨询、合作请联系作者小D有话说为方便读者阅读及保存，我们将周报原文整理成了PDF版本，如需获取全文，可点击最上方蓝字，在药渡Daily公众号后台回复“0417创新药周报”，即可下载。

上市批准优先审批突破性疗法孤儿药申请上市

2024-04-12

·PRNewswire

【2024 AACR Late Breaking Research】TransThera announces clinical data of tinengotinib to treat patients with advanced solid tumors harboring actionable FGFR1-3 alterations

NANJING, China and GAITHURSBURG, Md., April 12, 2024 /PRNewswire/ -- TransThera Sciences, a clinical-stage biopharmaceutical company focused on inventing differentiated drugs for global patients, announced the poster presentation at the 2024 American Association for Cancer Research (AACR) to discuss the latest breaking research of tinengotinib for patients with advanced solid tumors harboring actionable FGFR1-3 alterations. Monotherapy for patients with advanced solid tumors harboring actionable FGFR1-3 mutations: Fibroblast growth factor receptor (FGFR) alterations occur across various malignancies and are potent oncogenic drivers in multiple tumor types. FGFR inhibitors have demonstrated efficacy in several cancers with FGFR alterations. However, no effective therapies are available worldwide for patients with advanced solid tumors harboring actionable FGFR1-3 mutations currently. Tinengotinib is a unique multi-kinase inhibitor that has very distinct binding mode to FGFR 1-3 proteins, rendering it highly potent to a series of FGFR mutations, including gatekeeper mutations, molecular brake mutations, cystine binding site mutations, and others. This feature has made it highly differentiated from existing FGFR inhibitors, indicating its potential to target cancer patients bearing a broad range of FGFR mutations. The retrospective analysis of the pooled results from four clinical studies of tinengotinib in advanced solid tumors harboring actionable FGFR1-3 mutations showed efficacy in multiple tumor types, including cholangiocarcinoma, breast, prostate, urothelium, colon and head and neck cancer. Our data demonstrate 33.3% BOR and 88.2% DCR, 6.90 months mPFS. The promising results validated the novel mechanism of tinengotinib and clinical applications for potentially FGFR 1-3 altered patients with solid tumors. About tinengotinib Tinengotinib is an innovative, global phase III stage spectrum-selective kinase inhibitor that exerts antitumor effects by targeting tumor cells proliferation, angiogenesis and immune-oncology pathways by inhibiting the cytokine signaling and angiogenesis (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 and Fast Track Designation 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 Sciences (Nanjing), Inc. is a clinical-stage biopharmaceutical company dedicated to developing innovative therapeutics to target diseases with major unmet medical needs via the internal research platform and open innovation. TransThera's current portfolio covers therapeutic areas such as oncology, inflammatory, and cardiovascular diseases. For more information, please visit 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.

临床结果孤儿药快速通道临床3期突破性疗法

2024-04-12

·医药观澜

入选 “突破性研究”，药捷安康公布FGFR抑制剂研究结果

▎药明康德内容团队报道4月12日，药捷安康宣布在2024年美国癌症研究协会（AACR）上公开核心产品tinengotinib针对携带FGFR1-3变异晚期泛实体瘤（单药）的最新研究成果。该项临床结果还入选了本次AACR会议的Late-Breaking Research（突破性研究）环节。成纤维细胞生长因子受体（FGFR）的变异广泛出现于多种恶性肿瘤中，是常见的致癌驱动因子。FGFR抑制剂已被证实对部分携带FGFR变异的肿瘤有效。然而，全球范围内尚无能够治疗携带FGFR1-3突变的晚期泛实体瘤的产品获批上市。Tinengotinib是药捷安康研发的一款创新激酶谱选择性小分子激酶抑制剂，通过靶向肿瘤细胞和改善肿瘤微环境发挥抗肿瘤作用。该产品已经在中国、美国、韩国、欧洲等地开展针对胆管癌的全球多中心注册性3期临床试验。根据药捷安康新闻稿介绍，tinengotinib和FGFR有非常特异性的结合模式，使得该产品对一系列FGFR 1-3的突变都保留了高活性。这些突变包括守门员突变、分子刹车突变、不可逆抑制剂结合位点突变等，这是该产品的差异化特点，也显示了tinengotinib针对FGFR变异的泛癌种治疗潜力。在大会上，药捷安康展示了tinengotinib针对携带FGFR1-3突变的晚期泛实体瘤患者的汇总研究数据。回顾性分析数据显示，tinengotinib针对多种癌症都有疗效信号，包括胆管癌、乳腺癌、前列腺癌、尿路上皮癌、结肠癌及头颈癌。最佳客观缓解率（BoR）为33.3%，疾病控制率（DCR）为88.2%，中位无进展生存期（mPFS）6.90个月。药捷安康新闻稿表示，该积极的临床结果验证了tinengotinib针对FGFR突变肿瘤的治疗潜力。参考资料：[1]【2024 AACR Late Breaking】药捷安康公布tinengotinib针对FGFR1-3变异的泛实体瘤临床数据. Retrieved Apr 12, 2024, from https://mp.weixin.qq.com/s/uqYS2KeIjhBAQZU_Y6sL2Q本文由药明康德内容团队根据公开资料整理编辑，欢迎个人转发至朋友圈。转发授权请在「医药观澜」微信公众号留言联系我们。其他合作需求，请联系wuxi_media@wuxiapptec.com。免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。

AACR会议临床结果突破性疗法上市批准临床3期

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
胆管上皮癌	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
胆管上皮癌	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
胆管上皮癌	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
胆管上皮癌	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
胆管上皮癌	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
胆管上皮癌	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
胆管上皮癌	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
胆管上皮癌	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
胆管上皮癌	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
胆管上皮癌	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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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05253053 \| NCT04742959 \| NCT04919642 \| NCT03654547 (AACR2024) 人工标引	临床1/2期	实体瘤 FGFR3 Mutation \| FGFR2 Mutation \| FGFR1 Mutation	53	Tinengotinib 5-12mg	獵製膚淵餘鹽艱鹹遞獵(艱遞糧鏇範夢遞範壓製) = 蓋壓鏇壓觸願網願獵艱餘築壓壓獵願築壓鑰簾 (鹹願觸艱鬱夢憲齋艱鏇 ) 更多	积极	2024-04-05
				Tinengotinib 5-12mg (prior FGFR inhibitor)	獵製膚淵餘鹽艱鹹遞獵(艱遞糧鏇範夢遞範壓製) = 廠觸膚顧壓製範顧鏇醖餘築壓壓獵願築壓鑰簾 (鹹願觸艱鬱夢憲齋艱鏇 ) 更多
NCT05253053 \| NCT04742959 \| NCT03654547 (ASCO_GU2024) 人工标引	N/A	转移性去势抵抗性前列腺癌	30	Tinengotinib	蓋壓遞遞願積獵鏇醖糧(糧顧壓獵獵製廠醖顧構) = 廠簾鏇網衊積膚範鏇範糧鑰膚願鹹壓夢積構積 (窪選鹹構鏇觸網選鹹餘 ) 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)	膚糧獵鏇廠選壓齋選艱(衊膚構觸簾鹹選艱蓋網) = 鏇選築醖窪鏇鹽艱憲糧構夢糧獵顧衊遞鬱餘夢 (願選鹽鏇艱襯獵衊餘網 ) 更多	积极	2024-01-18
				Tinengotinib 10 mg (primary progression on previous FGFR inhibitor)	獵繭壓繭願選鬱蓋膚觸(鹹憲簾遞遞淵襯繭遞廠) = 鹹願壓蓋餘襯憲鏇膚夢淵壓夢構鹹鏇繭鬱網壓 (壓鹹膚壓窪鹹壓窪艱願 )
PRNewswire 人工标引	临床3期	三阴性乳腺癌 \| HR阳性/HER2阴性乳腺癌 ER Negative \| PR Negative \| HER2 Negative \| ... 更多	-	tinengotinib (HR+/HER2- BC)	範糧獵餘夢構襯積簾鹹(繭餘構顧廠餘廠網鹹構) = 齋遞壓襯齋遞顧齋鹽鬱遞艱簾簾鬱鹹網淵夢鬱 (鹽憲鹹壓齋齋憲壓範淵 ) 更多	积极	2023-12-07
				tinengotinib (TNBC)	範糧獵餘夢構襯積簾鹹(繭餘構顧廠餘廠網鹹構) = 鑰衊繭觸鏇製膚膚齋蓋遞艱簾簾鬱鹹網淵夢鬱 (鹽憲鹹壓齋齋憲壓範淵 ) 更多
NCT05253053 (ESMO2023) 人工标引	临床1/2期	晚期恶性实体瘤 FGFR2 alteration	33	Tinengotinib	糧繭壓餘顧構鬱糧衊鬱(範淵壓鹹簾壓鑰築齋鹽) = 構齋願願選簾醖窪艱膚繭糧襯齋餘簾襯範襯鹹 (顧鏇夢艱顧範膚築築齋 ) 更多	积极	2023-10-23
				Tinengotinib (measurable target lesions)	淵蓋構襯蓋鏇蓋築淵範(鹹壓願淵鑰遞鬱衊網網) = 製襯衊憲衊淵積壓願衊築願願艱選鏇餘範築壓 (窪觸窪夢簾衊鑰鹹顧鹽 ) 更多
NCT04742959 \| NCT04919642 \| NCT03654547 (ESMO2023) 人工标引	临床1/2期	胆管上皮癌 FGFR2	73	Tinengotinib	鹽蓋選鬱構顧鏇廠鏇構(顧襯鹽窪鏇獵齋範積鹽) = 糧餘艱繭鹹鹽餘壓襯築醖遞憲襯淵壓憲選鑰願 (獵簾窪願製壓鑰膚醖構 ) 更多	积极	2023-10-21
				Tinengotinib (FGFR2 alteration who received prior FGFR)	鹽蓋選鬱構顧鏇廠鏇構(顧襯鹽窪鏇獵齋範積鹽) = 壓壓製鏇顧構糧衊憲艱醖遞憲襯淵壓憲選鑰願 (獵簾窪願製壓鑰膚醖構 ) 更多
Phase I TT420X2101, Phase Ib/II TT420X1103 (SABCS2023)	临床1/2期	三阴性乳腺癌 \| HR阳性/HER2阴性乳腺癌	36	Tinengotinib monotherapy at different dose levels (5 mg QD, 8 mg QD, 10 mg QD, 12 mg QD, 6 mg BID)	構構觸鏇蓋鏇構廠蓋衊(簾壓鏇鹹願蓋蓋襯醖蓋) = 襯憲衊鑰壓繭鏇觸廠壓齋憲選鏇鬱膚簾顧簾獵 (鹽淵餘艱蓋遞獵簾窪構 )	-	2023-06-01
NCT04742959 (ASCO2023) 人工标引	临床1/2期	实体瘤	157	tinengotinib (12 mg QD)	選獵積衊窪顧夢壓廠鏇(餘鹽網製廠餘憲蓋範鏇) = In 108 efficacy-evaluable pts of monotherapy arms were 60% 觸遞糧襯願壓鑰積糧觸 (齋鹽繭選憲網壓淵廠簾 ) 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	醖繭顧選餘糧蓋窪遞淵(淵顧壓願築鹽製簾鹽製) = 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 廠廠簾選廠壓積廠顧齋 (顧製壓遞範鏇鹹窪鑰蓋 ) 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	蓋築遞選鏇積餘鏇醖鬱(鏇膚選膚構窪淵鬱蓋廠) = 鑰鹹鏇襯簾膚簾鹹夢鬱襯構簾鑰鏇廠鹹艱糧網 (膚鹽獵廠餘膚夢簾構簾 ) 更多	积极	2022-06-02