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更新于：2026-06-15
Tasurgratinib
他舒格替尼
更新于：2026-06-15
概要
基本信息
药物类型 小分子化药 |
别名 Tasurgratinib Succinate、他舒替尼、琥珀酸他舒格替尼 + [5] |
作用方式 拮抗剂 |
作用机制 FGFR1拮抗剂(成纤维细胞生长因子受体-1拮抗剂)、FGFR2拮抗剂(成纤维细胞生长因子受体-2拮抗剂)、FGFR3拮抗剂(成纤维细胞生长因子受体-3拮抗剂) |
在研适应症 |
非在研适应症 |
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2024-09-24), |
最高研发阶段(中国)申请上市 |
特殊审评孤儿药 (日本) |
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结构/序列
分子式C32H37N5O6 |
InChIKeyIBHOLSBDZMIPPT-UHFFFAOYSA-N |
CAS号1622204-21-0 |
关联
10
项与 他舒格替尼 相关的临床试验JPRN-jRCT2031210043
Multicenter investigator-initiated phase II trial of E7090 in patients with advanced or recurrent solid tumor with fibroblast growth factor receptor (FGFR) gene alteration - FORTUNE trial
NCT04962867
Multicenter Investigator-initiated Phase II Trial of E7090 in Patients With Advanced or Recurrent Solid Tumor With Fibroblast Growth Factor Receptor (FGFR) Gene Alteration (FORTUNE Trial)
JPRN-JapicCTI-205429
An Open-label Phase 1b Study of E7090 Monotherapy and in Combination With Other Anticancer Agents in Subjects With Estrogen Receptor Positive (ER+) and Human Epidermal Growth Receptor 2 Negative (HER2-) Recurrent/Metastatic Breast Cancer
100 项与 他舒格替尼 相关的临床结果
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100 项与 他舒格替尼 相关的转化医学
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100 项与 他舒格替尼 相关的专利（医药）
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16
项与 他舒格替尼 相关的文献（医药）2026-05-01Gan to kagaku ryoho. Cancer & chemotherapy
[FGFR2 Fusion Gene-Positive Solid Tumors].
Article
作者: Kawakatsu, Shoji ; Baba, Taisuke ; Kurimoto, Keisuke ; Yamada, Mihoko ; Ebata, Tomoki ; Watanabe, Nobuyuki ; Onoe, Shunsuke ; Mizuno, Takashi ; Sunagawa, Masaki ; Kokuryo, Toshio
Fibroblast growth factor receptors (FGFR) are tyrosine kinases that regulate cellular responses including proliferation, survival, and migration. FGFR fusion genes arose from chromosomal translocations or deletions, lead to ligand-independent constitutive signal activation and contribute to carcinogenesis and cancer progression. FGFR2 fusion genes are identified in 7.4-13.6% of intrahepatic cholangiocarcinoma and 3.6% of perihilar cholangiocarcinoma. They are also reported in colorectal, prostate, and breast cancers, though at lower frequencies. Diagnosis methods are RT-PCR, RNA sequencing, FISH, and NGS. Comprehensive genomic profiling (CGP) tests are available clinically. Three FGFR inhibitors are currently approved. Pemigatinib (approved in 2021) demonstrated a response rate of 35.5%, futibatinib (approved in 2023) showed a response rate of 42%, and tasurgratinib (approved in 2024) achieved a response rate of 30.2%. The most common adverse event is hyperphosphatemia. Alopecia, diarrhea, nail disorders, and retinal detachment are also required attention. Polyclonal on-target resistance to pan-FGFR inhibitors and increasing of FGFR2 kinase domain resistance mutations based on treatment history has been reported. Novel therapeutics, such as highly selective FGFR2 inhibitors and next-generation inhibitors, are developed and are expected to improve prognosis for patients with FGFR2 fusion-positive solid tumors.
2025-12-01Oncology and Therapy
Sequential Fibroblast Growth Factor Receptor Inhibition in Intrahepatic Cholangiocarcinoma: Navigating an Evolving Landscape of Resistance and Opportunity—A Case Report and Current Opinion
Article
作者: Yamaguchi, Hironori ; Sasanuma, Hideki
Fibroblast growth factor receptor (FGFR)2 rearrangements define a distinct molecular subset of intrahepatic cholangiocarcinoma (iCCA) with therapeutic potential using FGFR inhibitors. However, acquired resistance invariably limits long-term efficacy, posing a significant clinical challenge. Sequential targeting with different FGFR inhibitors is an emerging strategy, yet robust evidence, particularly for third-line and beyond, is scarce, and a consensus on optimal sequencing and patient selection remains unreached. Here, we report a case of FGFR2-rearranged iCCA where the patient achieved a radiographic partial response (PR) to tasurgratinib (a third-line FGFR inhibitor) following prior progression on pemigatinib and futibatinib. This case underscores the sustained dependency on the FGFR pathway and highlights the potential clinical utility of rationally sequenced FGFR-targeted therapy even after multiple lines of treatment. More broadly, this report serves as a basis for a current opinion on the evolving landscape of sequential FGFR inhibition in iCCA. We delve into the complexities of acquired resistance, dissect the arguments for and against prolonged FGFR pathway blockade, explore the impact of co-occurring genomic alterations, discuss the controversies, research priorities, and the urgent need for a balanced perspective to guide future clinical practice and trial design in this rapidly advancing but still uncertain field.
2025-11-08JAPANESE JOURNAL OF CLINICAL ONCOLOGY
Tasurgratinib (E7090) for cholangiocarcinoma with fibroblast growth factor receptor 2 fusions/rearrangements: a multicenter, open-label, Phase 2 study
Article
作者: Ikeda, Masafumi ; Duan, Huaxin ; Yan, Sheng ; Kuwahara, Takamichi ; Nakai, Yousuke ; Satoh, Taroh ; Nakada, Takuya ; Meng, Zhiqiang ; Funasaka, Setsuo ; Shen, Lin ; Furuse, Junji ; Komatsu, Yoshito ; Morizane, Chigusa ; Ma, Xuelei ; Ikezawa, Hiroki ; Cui, Tongjian ; Ueno, Makoto ; Zhao, Haitao ; Sasaki, Takashi ; Nagano, Hiroaki
Abstract:
Background:
This Phase 2 study (NCT04238715) evaluated the efficacy/safety of tasurgratinib 140 mg daily in patients with cholangiocarcinoma (CCA) and fibroblast growth factor receptor (FGFR) 2 fusions/rearrangements.
Methods:
Eligible Japanese and Chinese patients who had surgically unresectable, advanced, or metastatic CCA and had received ≥1 prior gemcitabine-based combination chemotherapy regimen were included and treated with oral tasurgratinib 140 mg daily. The primary endpoint was objective response rate (ORR); the study was considered successful if the lower limit of the ORRs 90% CI was >15%. Secondary endpoints included duration of response and safety. FGFR2 fusions/rearrangements were confirmed by fluorescence in situ hybridization performed in central laboratories. Tumor responses were measured every 8 weeks by Response Evaluation Criteria in Solid Tumors version 1.1 per independent imaging review.
Results:
Sixty-three patients were treated; 23 (37%) had received 1 prior regimen, all others had received ≥2. By the data cutoff date (15 March 2023), the ORR was 30.2% (two-sided 90% CI: 20.7–41.0). The median duration of response for responders was 5.6 months (95% CI: 3.7–9.3; range: 1.0+ to 14.8+). Sixty-one patients (97%) had ≥1 treatment-related treatment-emergent adverse event; 18 patients (29%) had ≥1 grade ≥3 treatment-related treatment-emergent adverse events. Four patients (6%) had a fatal adverse event, none were considered treatment-related. Tasurgratinib had promising antitumor activity in patients with CCA harboring FGFR2 fusions or rearrangements after ≥1 prior gemcitabine-based chemotherapy regimen.
Conclusions:
The primary endpoint (ORR) met the study’s predefined success criteria. Tasurgratinib had a manageable safety profile consistent with previous reports and the known pharmacological profile of FGFR inhibitors.
100 项与 他舒格替尼 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| FGFR2融合或重排的胆管癌 | 日本 | 2024-09-24 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 胆管癌 | 申请上市 | 中国 | 2026-02-10 | |
| 胆管癌 | 申请上市 | 中国 | 2026-02-10 | |
| 复发性实体肿瘤 | 临床2期 | 日本 | 2021-06-15 | |
| 转移性胆管癌 | 临床2期 | 中国 | 2020-01-22 | |
| 转移性胆管癌 | 临床2期 | 日本 | 2020-01-22 | |
| ER阳性/HER2阴性乳腺癌 | 临床1期 | 日本 | 2020-10-09 | |
| ER阳性乳腺癌 | 临床1期 | 日本 | 2020-10-09 | |
| 晚期恶性实体瘤 | 临床1期 | 日本 | 2014-10-28 | |
| 不能切除的胆道癌 | 临床申请批准 | 中国 | 2026-06-12 | |
| 不能切除的胆道癌 | 临床申请批准 | 中国 | 2026-06-12 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 46 | (Group A: FGFR1-3 fusion) | 廠醖簾鏇糧衊網鑰鹽蓋(製襯壓鹹築繭製餘製鹽) = 衊衊遞憲蓋遞衊憲簾製 積蓋網簾齋鏇窪願觸鹽 (鹽衊簾獵選壓艱鑰壓積, 3.7 ~ 50.7) 更多 | 积极 | 2025-05-30 | ||
(Group B: FGFR1-3 sensitive mutations to tasurgratinib determined by MANO methods) | 廠醖簾鏇糧衊網鑰鹽蓋(製襯壓鹹築繭製餘製鹽) = 鬱蓋鑰衊糧膚糧蓋蓋窪 積蓋網簾齋鏇窪願觸鹽 (鹽衊簾獵選壓艱鑰壓積, 5.7 ~ 44.0) 更多 | ||||||
临床1期 | 32 | 顧糧壓膚憲鏇鑰顧憲廠(窪繭選遞醖壓衊壓觸鬱) = 獵餘膚遞夢鹽憲觸積衊 廠壓積觸鏇觸鹹廠網襯 (顧衊鹹顧獵夢膚廠壓蓋 ) 更多 | 积极 | 2024-05-24 | |||
顧糧壓膚憲鏇鑰顧憲廠(窪繭選遞醖壓衊壓觸鬱) = 壓構遞遞鹹襯鑰襯憲醖 廠壓積觸鏇觸鹹廠網襯 (顧衊鹹顧獵夢膚廠壓蓋 ) 更多 | |||||||
临床2期 | FGFR2融合或重排的胆管癌 FGFR2 gene fusion | 63 | tasurgratinib 140 mg | 觸夢憲獵糧餘廠憲簾繭(築壓積憲遞簾襯遞鬱構) = 範積簾簾襯鏇願窪遞遞 膚鏇鑰艱顧積構醖獵憲 (簾艱範蓋築鑰製觸築衊 ) 更多 | 积极 | 2024-01-19 | |
临床1期 | 16 | (Cholangiocarcinoma harboring FGFR2 gene fusion) | 網簾構憲顧糧製廠鬱齋(淵鑰構壓願顧築憲壓艱) = reported in 2 out of 16 patients (13%); they were increased AST, lipase increased and retinopathy 獵膚憲憲憲鹹範淵鹹願 (遞構膚夢蓋鬱網糧積淵 ) 更多 | 积极 | 2020-02-04 | ||
(Gastric cancer harboring FGFR2 gene amplification or FGFR2 protein high expression) | |||||||
临床1期 | 24 | 窪艱鹹鹹夢觸鏇鹹鬱構(築願夢醖鹽淵鹽繭簾襯) = No DLT were observed up to the 140-mg dose; one patient in the 180-mg cohort experienced a DLT (increased aspartate aminotransferase/alanine aminotransferase, grade 3) 鹹襯衊鬱淵顧鬱網鹹獵 (糧繭艱製顧顧簾製窪襯 ) | 积极 | 2020-02-01 | |||
临床1期 | 40 | 襯顧遞淵鑰餘選網糧鹹(醖範觸夢淵選鑰窪鹽淵) = 鑰餘鹽鑰衊顧範餘膚鹹 艱糧顧顧網構築網廠築 (簾淵蓋繭鏇衊夢積淵顧 ) | 积极 | 2017-07-01 |
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