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更新于：2026-04-25
GSK-3052230
更新于：2026-04-25
概要
基本信息
在研机构- |
最高研发阶段暂停临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评- |
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结构/序列
Sequence Code 150418
Sequence Code 1117836251
关联
4
项与 GSK-3052230 相关的临床试验NCT01868022
Multi-arm, Non-randomized, Open-Label Phase IB Study to Evaluate GSK3052230 in Combination With Paclitaxel and Carboplatin, or Docetaxel or as Single Agent in Subjects With Solid Malignancies and Deregulated FGF Pathway Signaling
NCT01604863
Multi-Center, Open-Label Phase 1B Study to Evaluate the Safety and Tolerability of HGS1036 in Combination With Paclitaxel and Carboplatin, Cisplatin and Etoposide, or Docetaxel in Subjects With Advanced Solid Malignancies
NCT01244438
An Open-Label Phase 2 Pilot Study Evaluating the Activity and Safety of FP 1039 in Subjects With Advanced and/or Recurrent Endometrial Cancers With Specific FGFR2 Mutations
100 项与 GSK-3052230 相关的临床结果
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100 项与 GSK-3052230 相关的转化医学
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100 项与 GSK-3052230 相关的专利（医药）
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8
项与 GSK-3052230 相关的文献（医药）2020-04-01Investigational new drugs3区 · 医学
A phase Ib study of GSK3052230, an FGF ligand trap in combination with pemetrexed and cisplatin in patients with malignant pleural mesothelioma
3区 · 医学
Article
作者: López, Pilar Garrido ; Vasquez, James ; Morgensztern, Daniel ; Mitrica, Ionel ; Orlov, Sergey ; Fennell, Dean A ; Gadgeel, Shirish ; Wang, Xiaowei ; Viteri, Santiago ; Baker-Neblett, Katherine ; Kindler, Hedy L ; Zauderer, Marjorie G ; Kostorov, Vladimir ; Levchenko, Evgeny ; Trigo, José ; DeYoung, M Phillip ; Bellovin, David I ; Yan, Li ; van Brummelen, Emilie M J ; Dómine, Manuel ; Schellens, Jan H M ; Vansteenkiste, Johan F
Background Fibroblast growth factors (FGFs) have a fundamental role in cancer. Sequestering FGFs with GSK3052230 (FP-1039) blocks their ability to activate FGFRs while avoiding toxicities associated with small molecule inhibitors of FGFR, including hyperphosphatemia and retinal, nail, and skin toxicities. Methods A multicenter, open-label, phase Ib study evaluated weekly GSK3052230 added to pemetrexed/cisplatin in patients with treatment-naive, unresectable malignant pleural mesothelioma. Doses were escalated according to a 3 + 3 design, followed by cohort expansion at the maximum tolerated dose (MTD). Endpoints included safety, overall response rate, progression-free survival, and pharmacokinetics. Results 36 patients were dosed at 10, 15, and 20 mg/kg doses of GSK3052230. Three dose-limiting toxicities were observed at 20 mg/kg and one at 15 mg/kg. The MTD was defined as 15 mg/kg and used for cohort expansion. The most common treatment-related adverse events (AEs) were nausea (56%), decreased appetite (36%), infusion reactions (36%), decreased neutrophil counts (36%), and fatigue (33%). The confirmed ORR was 39% (95% CI: 23.1-56.5) (14/36 PRs) and 47% had stable disease (17/36), giving a disease control rate of 86%. At 15 mg/kg GSK3052230 (n = 25), the ORR was 44% (95% CI: 24.4-65.1), and the median PFS was 7.4 months (95% CI: 6.7-13.4). Four patients had disease control for over 1 year, and three were still ongoing. Conclusion At 15 mg/kg weekly, GSK3052230 was well tolerated in combination with pemetrexed/cisplatin and durable responses were observed. Importantly, AEs associated with small molecule inhibitors of FGFR were not observed, as predicted by the unique mechanism of action of this drug.
2019-10-01Lung cancer (Amsterdam, Netherlands)2区 · 医学
An open-label phase IB study to evaluate GSK3052230 in combination with paclitaxel and carboplatin, or docetaxel, in FGFR1-amplified non-small cell lung cancer
2区 · 医学
Article
作者: Vasquez, James ; Baker-Neblett, Katherine ; Orlov, Sergey ; Delgado, Ignacio ; Wang, Xiaowei ; DeYoung, M Phillip ; Morgensztern, Daniel ; Shomova, Marina ; Burdaeva, Olga ; Trigo, José ; Karaseva, Nina ; Garrido, Pilar ; Lassen, Ulrik ; Felip, Enriqueta ; Dómine, Manuel ; Yan, Li ; Paik, Paul K ; Lara, Primo ; Mitrica, Ionel
OBJECTIVES:
GSK3052230 (FP-1039) is a soluble fusion protein that acts as ligand trap sequestering fibroblast growth factors (FGFs) involved in tumor growth and angiogenesis, while sparing the hormonal FGFs. Because of this selectivity, the molecule is predicted to avoid toxicities associated with small molecule inhibitors of FGFR, including hyperphosphatemia and retinal, nail, and skin toxicities. Herein we report the results of a phase 1b study where GSK3052330 was administered with standard of care chemotherapy in FGFR1-amplified squamous non-small cell lung cancer (sqNSCLC) patients.
METHODS AND METHODS:
Eligible patients with stage IV or recurrent metastatic sqNSCLC harboring FGFR1 gene amplification received escalating doses of GSK3052230 in combination with paclitaxel and carboplatin at the starting doses 200 mg/m2 and AUC of 6, respectively, in the first line setting (Arm A) or docetaxel 75 mg/m2 in second line (Arm B). The primary endpoints of the study were safety and tolerability, to identify a maximum tolerated dose (MTD), and to assess overall response rate (ORR) based on investigator assessment.
RESULTS:
Twenty-nine patients were enrolled into the study, including 20 patients on Arm A and 9 patients on Arm B. There were no dose limiting toxicities in either Arm and the MTD was not reached. The most common adverse events (AEs) were compatible with the chemotherapy backbone used in each Arm, including neutropenia, alopecia, nausea, arthralgia, asthenia, diarrhea and peripheral neuropathy. The overall response rate and median progression-free survival were 47% and 5.5 months, respectively, for Arm A and 0% and 4.6 months, respectively, for Arm B.
CONCLUSION:
GSK3052230 is a novel FGFR pathway inhibitor, which is well tolerated in combination with chemotherapy. Importantly, AEs associated with small molecule inhibitors of FGFR were not observed, as predicted by the unique mechanism of action of this drug.
2016-06-28Oncotarget
Inhibition of FGF/FGFR autocrine signaling in mesothelioma with the FGF ligand trap, FP-1039/GSK3052230
Article
作者: Tunstead, James ; Sherk, Christian ; Fricko, Maggie ; Minthorn, Elisabeth ; Barnette, Mary ; Alsaid, Hasan ; Skedzielewski, Tina ; Jucker, Beat M. ; Kumar, Rakesh ; DeYoung, M. Phillip ; Ganji, Gopinath ; Blackwell, Christina ; Hoang, Bao
Fibroblast growth factor (FGF) ligand-dependent signaling has a fundamental role in cancer development and tumor maintenance. GSK3052230 (also known as FP-1039) is a soluble decoy receptor that sequesters FGFs and inhibits FGFR signaling. Herein, the efficacy of this molecule was tested in models of mesothelioma, a tumor type shown to express high levels of FGF2 and FGFR1. GSK3052230 demonstrated antiproliferative activity across a panel of mesothelioma cell lines and inhibited growth of tumor xenografts in mice. High expression of FGF2 and FGFR1 correlated well with response to FGF pathway inhibition. GSK3052230 inhibited MAPK signaling as evidenced by decreased phospho-ERK and phospho-S6 levels in vitro and in vivo. Additionally, dose-dependent and statistically-significant reductions in tumor vessel density were observed in GSK3052230-treated tumors compared to vehicle-treated tumors. These data support the role of GSK3052230 in effectively targeting FGF-FGFR autocrine signaling in mesothelioma, demonstrate its impact on tumor growth and angiogenesis, and provide a rationale for the current clinical evaluation of this molecule in mesothelioma patients.
100 项与 GSK-3052230 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 |
|---|---|---|---|---|
| 复发性子宫内膜癌 | 临床2期 | - | 2011-01-01 | |
| 恶性胸膜间皮瘤 | 临床1期 | 美国 | 2013-10-09 | |
| 恶性胸膜间皮瘤 | 临床1期 | 比利时 | 2013-10-09 | |
| 恶性胸膜间皮瘤 | 临床1期 | 丹麦 | 2013-10-09 | |
| 恶性胸膜间皮瘤 | 临床1期 | 荷兰 | 2013-10-09 | |
| 恶性胸膜间皮瘤 | 临床1期 | 俄罗斯 | 2013-10-09 | |
| 恶性胸膜间皮瘤 | 临床1期 | 西班牙 | 2013-10-09 | |
| 恶性胸膜间皮瘤 | 临床1期 | 英国 | 2013-10-09 | |
| 转移性非鳞状非小细胞肺癌 | 临床1期 | 美国 | 2013-10-09 | |
| 转移性非鳞状非小细胞肺癌 | 临床1期 | 比利时 | 2013-10-09 |
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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1期 | 非小细胞肺癌 FGFR1 Amplification | 29 | 蓋鏇鏇製襯醖築襯憲鏇(構構鏇廠餘簾壓襯夢築) = the MTD was not reached. 獵製製網襯構淵壓網醖 (衊膚觸艱夢積網構觸鏇 ) 更多 | 积极 | 2019-10-01 | ||
临床1期 | 65 | (5 mg/kg GSK3052230 + Paclitaxel + Carboplatin: Arm A) | 醖鏇鏇鹹鏇鑰鏇衊繭願 = 餘餘製顧獵積壓齋壓憲 憲積積觸鬱衊憲願鹹襯 (夢鹹壓簾獵憲餘鏇鹹簾, 積醖網膚簾鬱醖襯鑰鏇 ~ 鬱窪願夢鏇窪構築簾鏇) 更多 | - | 2019-02-11 | ||
(10 mg/kg GSK3052230 + Paclitaxel + Carboplatin: Arm A) | 醖鏇鏇鹹鏇鑰鏇衊繭願 = 獵廠築顧膚襯鬱夢鏇積 憲積積觸鬱衊憲願鹹襯 (夢鹹壓簾獵憲餘鏇鹹簾, 構鏇廠顧憲憲繭鏇遞鏇 ~ 艱鏇鑰鏇製獵襯選鑰壓) 更多 | ||||||
临床1期 | 24 | 選廠窪顧糧醖壓遞構獵(觸廠築顧餘觸鏇構鏇衊) = 壓鑰鹽網餘糧糧製艱鬱 艱選鏇繭窪繭範網憲範 (膚鹽醖願遞蓋願鬱廠製 ) | - | 2016-05-20 | |||
選廠窪顧糧醖壓遞構獵(觸廠築顧餘觸鏇構鏇衊) = 餘鑰壓蓋淵鏇選鬱觸築 艱選鏇繭窪繭範網憲範 (膚鹽醖願遞蓋願鬱廠製 ) | |||||||
临床1期 | 39 | 鬱鹹齋獵膚膚蓋艱積壓(獵鏇鏇鹹積鹹範鏇範醖) = reported at doses of 0.75 mg/kg (urticaria), 1 mg/kg (intestinal perforation and neutropenia), and 16 mg/kg (muscular weakness). 襯鏇憲網餘網鏇壓鹹衊 (憲淵觸願製簾鬱積鏇鹹 ) | 积极 | 2016-03-01 | |||
临床1期 | 34 | 遞夢壓鬱餘簾鬱憲鹽襯(繭繭鹽壓選選範廠遞襯) = 鏇製積鑰壓繭鬱鑰艱淵 願餘醖壓觸遞範壓獵齋 (遞壓繭觸憲餘選遞壓蓋 ) | - | 2015-09-09 |
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