预约演示
更新于：2025-08-20
Foritinib Succinate
丁二酸复瑞替尼
更新于：2025-08-20
概要
基本信息
药物类型 小分子化药 |
别名 SAF 189s、SAF-189、SAF-189S + [1] |
作用方式 抑制剂 |
作用机制 ALK抑制剂(间变性淋巴瘤激酶抑制剂)、ROS1抑制剂(原癌基因酪氨酸蛋白激酶ROS抑制剂) |
在研适应症 |
非在研适应症- |
原研机构 |
非在研机构- |
权益机构- |
最高研发阶段申请上市 |
首次获批日期- |
最高研发阶段(中国)申请上市 |
特殊审评特殊审批 (中国) |
登录后查看时间轴
关联
5
项与 丁二酸复瑞替尼 相关的临床试验CTR20241820
一项评价丁二酸复瑞替尼胶囊与伊曲康唑胶囊、利福平胶囊在健康成年受试者中药物相互作用的单中心、开放、序贯给药临床研究
CTR20222655
[14C]SAF-189s在健康受试者体内的物质平衡临床试验
NCT06569420
A Randomized, Multicenter, Phase III Open-label Study: Efficacy and Safety of Comparing SAF-189s With Crizotinib in First-line Anaplastic Lymphoma Kinase-positive Advanced and Metastatic NSCLC
100 项与 丁二酸复瑞替尼 相关的临床结果
登录后查看更多信息
100 项与 丁二酸复瑞替尼 相关的转化医学
登录后查看更多信息
100 项与 丁二酸复瑞替尼 相关的专利（医药）
登录后查看更多信息
7
项与 丁二酸复瑞替尼 相关的文献（医药）2024-09-01Lancet Respiratory Medicine
Foritinib, a type II ROS1 inhibitor for NSCLC
作者: Lee, Jii Bum ; Ou, Sai-Hong Ignatius
Chromosomal translocation resulting in fusion of the 3' ROS1 kinase domain to a 5' fusion partner protein in nonsmall-cell lung cancer (NSCLC) was reported in 2007 and constitutes about 1% of NSCLC.In summary, the role of foritinib as first-line treatment of ROS1 fusion-pos. NSCLC remains to be established in view of the recent entry of repotrectinib,7 soon to be followed by taletrectinib.Its utility as a ROS1 TKI could depend on demonstration of clin. activity against the ROS1 Leu2086Phe mutation.
2024-09-01Lancet Respiratory Medicine
Foritinib in advanced ROS1-rearranged non-small-cell lung cancer in China: a multicentre, open-label, single-arm, phase 2 study
Article
作者: Shi, Jianhua ; Cheng, Ying ; Wang, Baoqing ; Wang, Changli ; Yi, Shanyong ; Liu, Zhe ; Chen, Yuan ; Luo, Pengfei ; Fan, Yun ; Wu, Yi-Long ; Pan, Hongming ; Zhang, Zhiye ; Li, Wei ; Jiang, Liyan ; Liu, Yunpeng ; Liao, Wangjun ; Ding, Cuimin ; Dong, Xiaorong ; Li, Mingjun ; Cui, Jiuwei ; Yang, Jin-Ji ; Chen, Gongyan ; Wang, Jun ; Hu, Yanping ; Wang, Ke ; Zang, Aimin ; Zhao, Qiong ; Liu, Si-Yang Maggie ; Sun, Meili ; Zhou, Jianying ; Shen, Xionghu
BACKGROUND:
Currently approved targeted treatment for ROS1-rearranged non-small-cell lung cancer (NSCLC) has either inadequate intracranial activity or CNS-related toxicities. We evaluated the efficacy and safety of foritinib, a novel ALK and ROS1 inhibitor, in patients with advanced ROS1-rearranged NSCLC.
METHODS:
This two-part (phase 2a and 2b), multicentre, single-arm, open-label, phase 2 study was done in 29 centres in China. Eligible participants were adults (aged ≥18 years) with histologically or cytologically confirmed ROS1-rearranged, locally advanced or metastatic stage IIIB-IV NSCLC, with an Eastern Cooperative Oncology Group performance status of 2 or less. Patients who had previously received no or one ROS1 inhibitor were enrolled into phase 2a, and patients who were naive to ROS1 inhibitor therapy were enrolled into phase 2b cohort 1. Participants in phase 2a received 80, 120, 160, or 210 mg foritinib succinate (foritinib) orally once daily over 21-day cycles; patients in phase 2b received the recommended phase 2 dose of 160 mg. The primary endpoint was objective response rate, assessed by the independent review committee in the full analysis set (ie, all participants who received at least one dose of study treatment). The safety analysis set included all participants who received at least one dose of study treatment and had available safety assessments. This study is ongoing and is registered with ClinicalTrials.gov, NCT04237805.
FINDINGS:
Between March 26, 2020, and Dec 29, 2022, 104 patients were enrolled and treated. Six patients who had previously received more than one ROS1 inhibitor were enrolled in phase 2a before a protocol amendment stating that patients in this phase should have received no more than one ROS1 inhibitor; these patients were included in the safety analysis but excluded from the efficacy analysis of the ROS1-inhibitor-pretreated cohort. Therefore, the efficacy analysis set (n=98) included 42 patients from phase 2a (17 who were ROS1 inhibitor naive and 25 who had previously received ROS1 inhibitor) and 56 patients from phase 2b cohort 1. In phase 2a, the objective response rate was 94% (95% CI 71-100; 16 of 17 patients) in patients who were ROS1 inhibitor naive and 40% (21-61; ten of 25) in patients who had previously received ROS1 inhibitor. In phase 2b cohort 1, the objective response rate was 88% (95% CI 76-95; 49 of 56 patients). In a prespecified exploratory analysis in 41 patients with CNS metastases at baseline, the objective response rate was 100% (95% CI 48-100; five of five patients) in patients in phase 2a who were ROS1 inhibitor naive, 40% (16-68; six of 15) in patients in phase 2a who had previously received ROS1 inhibitor, and 90% (70-99; 19 of 21) in patients in phase 2b cohort 1. Grade 3-4 treatment-related adverse events occurred in 33 (32%) of 104 patients; the most common were hyperglycaemia (12 [12%] patients) and electrocardiogram prolonged QT interval (six [6%]). Serious treatment-related adverse events occurred in 11 (11%) patients, with hyperglycaemia (six [6%]) being most common. No treatment-related adverse events led to death.
INTERPRETATION:
Foritinib showed systemic and intracranial antitumour activity and good tolerability in ROS1-inhibitor-naive patients with ROS1-rearranged NSCLC. Foritinib represents a promising treatment for these patients, especially in those with CNS metastases.
FUNDING:
Fosun Pharma, Wanbang Biopharmaceuticals, and Guangdong Provincial Key Lab of Translational Medicine in Lung Cancer.
2023-12-01Drugs in R&D
Effect of High-Fat Food on the Pharmacokinetic Profile and Safety of SAF-189s, an ALK/ROS1 Inhibitor, in Healthy Chinese Adults
Article
作者: Sun, Juan ; Qiu, Jingjun ; Hui, Ai-Min ; Tan, Yan ; Xiang, Xiao ; Hu, Wei ; Wu, Zhuli ; Qin, Huiling ; Zhou, Yongchun ; Diao, Lei
BACKGROUND AND OBJECTIVES:
This study was conducted to investigate the effect of high-fat meals on the pharmacokinetics (PK) and safety profile of SAF-189s, a novel ALK/ROS1 inhibitor.
METHODS:
This was a single-center, phase I, open-label, crossover study in which healthy adults (≥18 years) were randomized (1:1) to two sequences of SAF-189s administration (fasted-fed or fed-fasted) separated by a 14-day washout. After a ≥10-h overnight fast, volunteers received SAF-189s 160 mg orally in a fasted state or 30 min after a high-fat, high-calorie meal. Similarity of pharmacokinetic parameters was concluded if the 90% CI for the geometric mean ratio (GMR) between the fed and fasted group fell within the predefined range of 0.80-1.25.
RESULTS:
In total, 24 subjects were enrolled and 23 completed the study. SAF-189s maximum plasma concentration (Cmax; GMR: 109.1% [90% CI 103.1-115.4]) was comparable under fed (high-fat meal, n = 24) versus fasted (n = 23) conditions, with no effect on area under the plasma concentration-time curve from time 0 to t (AUC0-t; GMR: 105.1% [90% CI 100.3-110.2]) and AUC from time 0 to infinity (AUC0-∞; GMR: 105.5% [90% CI, 100.6-110.6]). In both groups, the median time to maximum plasma concentration (tmax) was around 6 h and mean plasma half-life (t½) was around 35 h. Fed administration led to a lower incidence of treatment-emergent adverse events (TEAEs; 29.2% vs 54.2%), including gastrointestinal disorders (4.2% vs 41.7%) and headache (0.0% vs 12.5%), versus fasted administration.
CONCLUSIONS:
A high-fat meal had minimal effect on the pharmacokinetic profile of SAF-189s compared with a fasted state following a single dose of 160 mg. Administration with a high-fat meal led to a lower incidence of TEAEs.
32
项与 丁二酸复瑞替尼 相关的新闻（医药）2025-06-22
·信狐药迅
2025-04-10
·微信
一致性评价生物类似药临床申请上市批准
2025-04-08
·戊戌数据
抗体药物偶联物临床申请申请上市细胞疗法
100 项与 丁二酸复瑞替尼 相关的药物交易
登录后查看更多信息
研发状态
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| ALK阳性非小细胞肺癌 | 申请上市 | 中国 | 2025-03-06 | |
| ALK阳性肺癌 | 临床3期 | 中国 | 2021-12-31 | |
| ALK阳性间变性大细胞淋巴瘤 | 临床3期 | 中国 | 2021-12-31 | |
| 晚期癌症 | 临床2期 | 中国 | 2016-11-14 | |
| 晚期恶性实体瘤 | 临床2期 | 中国 | 2016-11-14 | |
| ROS1阳性非小细胞肺癌 | 临床1期 | 中国 | 2024-06-09 | |
| ROS1阳性非小细胞肺癌 | 临床1期 | 中国 | 2024-06-09 | |
| 非小细胞肺癌 | 临床申请 | 美国 | - |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | ALK阳性非小细胞肺癌 ALK Positive | 275 | 憲築膚鏇糧鏇獵繭製鹹(憲蓋遞鏇顧鹹艱製醖積) = 鑰壓憲顧願構夢選齋衊 鏇窪襯獵鑰繭餘壓窪範 (築鹹繭繭襯衊簾憲窪網 ) 更多 | 积极 | 2024-09-09 | ||
憲築膚鏇糧鏇獵繭製鹹(憲蓋遞鏇顧鹹艱製醖積) = 築衊窪鏇鬱築醖鬱選願 鏇窪襯獵鑰繭餘壓窪範 (築鹹繭繭襯衊簾憲窪網 ) 更多 | |||||||
临床2期 | 104 | 繭願觸範觸醖餘蓋餘艱(壓鬱鹹築鬱衊夢積廠鹹) = 窪積齋衊衊製積廠鏇鑰 鹹遞鬱廠窪鏇艱夢積鹽 (淵願齋廠醖蓋廠鹽窪衊, 71 ~ 100) | 积极 | 2024-07-01 | |||
繭願觸範觸醖餘蓋餘艱(壓鬱鹹築鬱衊夢積廠鹹) = 製憲淵獵蓋獵廠獵遞觸 鹹遞鬱廠窪鏇艱夢積鹽 (淵願齋廠醖蓋廠鹽窪衊, 21 ~ 61) | |||||||
临床2期 | - | 遞範獵選顧鏇獵築鏇選(淵選窪壓膚憲範觸膚顧) = 鏇願積膚蓋選醖淵淵鏇 築遞艱構夢廠構範選積 (糧願膚糧顧鹽窪範蓋醖 ) 更多 | - | 2022-12-03 | |||
临床1/2期 | ALK阳性非小细胞肺癌 ALK Positive | 195 | 齋網網構觸齋獵獵膚選(範觸網艱襯積蓋觸鹽蓋) = hyperglycemia (7%), hypertension (6%) and diarrhea (3%) 選築壓簾醖繭構觸憲壓 (窪憲鬱窪艱艱鏇壓艱夢 ) 更多 | 积极 | 2022-06-02 | ||
(In phase 1 ALKi-naive) | |||||||
临床1/2期 | 45 | 範鏇範夢夢憲襯鏇顧鑰(鏇顧願壓鹹範鏇糧壓窪) = 醖齋範觸齋鏇製獵獵積 簾膚積壓顧憲構襯淵顧 (艱構壓網鏇襯壓糧壓獵, 49.1 ~ 79.0) 更多 | - | 2020-09-19 | |||
临床2期 | - | 鏇觸襯齋鑰願選糧衊選(衊範鬱鏇憲蓋鹽築壓艱) = 膚範積窪齋網選積鏇餘 窪餘願膚廠憲齋簾顧齋 (壓壓鑰範淵壓築衊襯築 ) | - | 2020-09-11 | |||
临床1/2期 | 36 | 築獵積憲餘築蓋構廠範(憲鹹願構構膚遞構襯壓) = 10 [27.8%] of 36 pts 觸鏇製構糧襯壓鹹製遞 (鹽鹹蓋衊壓繭淵簾醖艱 ) 更多 | 积极 | 2020-05-25 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
Eureka LS:
全新生物医药AI Agent 覆盖科研全链路，让突破性发现快人一步
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用