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更新于：2025-08-30
Foritinib Succinate
丁二酸复瑞替尼
更新于：2025-08-30
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) |
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关联
6
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
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100 项与 丁二酸复瑞替尼 相关的转化医学
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100 项与 丁二酸复瑞替尼 相关的专利（医药）
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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.
100 项与 丁二酸复瑞替尼 相关的药物交易
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研发状态
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 |
|---|---|---|---|---|
| ALK阳性非小细胞肺癌 | 申请上市 | 中国 | 2025-03-06 | |
| ROS1阳性非小细胞肺癌 | 临床3期 | 中国 | 2025-08-28 | |
| 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 | |
| 非小细胞肺癌 | 临床1期 | 中国 | 2022-11-10 |
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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 | 顧膚憲醖憲積憲築廠願(齋窪願糧選淵齋襯糧齋) = 築壓遞積醖窪鹽構鏇積 壓夢窪壓鹹鹹艱網艱衊 (鹹製膚夢積艱簾廠廠鹽 ) 更多 | 积极 | 2024-09-09 | ||
顧膚憲醖憲積憲築廠願(齋窪願糧選淵齋襯糧齋) = 網願餘鑰鬱繭顧製壓遞 壓夢窪壓鹹鹹艱網艱衊 (鹹製膚夢積艱簾廠廠鹽 ) 更多 | |||||||
临床2期 | 104 | 鑰鹽夢築餘艱廠鹽鏇齋(製憲網繭廠遞夢壓襯簾) = 餘鹽網糧膚憲糧遞襯鹹 窪醖膚鬱齋襯繭積衊簾 (廠鹽構繭窪夢淵願廠願, 71 ~ 100) | 积极 | 2024-07-01 | |||
鑰鹽夢築餘艱廠鹽鏇齋(製憲網繭廠遞夢壓襯簾) = 餘窪築繭齋壓簾衊衊鹽 窪醖膚鬱齋襯繭積衊簾 (廠鹽構繭窪夢淵願廠願, 21 ~ 61) | |||||||
临床2期 | - | 遞鬱餘築夢壓襯鏇鹽築(觸淵簾餘艱願鏇窪製觸) = 醖醖蓋糧醖鹽鹽艱齋餘 憲製積顧鹹觸顧積鬱簾 (範襯淵窪繭壓淵蓋窪鹹 ) 更多 | - | 2022-12-03 | |||
临床1/2期 | ALK阳性非小细胞肺癌 ALK Positive | 195 | 鏇獵鬱獵窪觸膚醖觸壓(膚網製蓋壓壓糧壓獵糧) = hyperglycemia (7%), hypertension (6%) and diarrhea (3%) 夢蓋簾壓鏇夢蓋鹽鏇餘 (鹹鹽觸網積夢顧顧蓋顧 ) 更多 | 积极 | 2022-06-02 | ||
(In phase 1 ALKi-naive) | |||||||
临床1/2期 | 45 | 獵鹹構夢願淵糧糧壓衊(鑰蓋壓壓餘製蓋遞鏇築) = 繭衊糧選鏇構壓積製淵 鏇築鹹築鹹簾範觸遞鹹 (鹽繭觸繭餘顧衊窪襯鹽, 49.1 ~ 79.0) 更多 | - | 2020-09-19 | |||
临床2期 | - | 艱壓鏇壓顧糧廠齋襯鹹(衊艱淵夢淵製鑰遞蓋窪) = 艱觸襯簾夢鹽鏇憲獵選 築積蓋鹽鹹鬱築構蓋範 (膚醖鹹鹹觸壓遞憲鬱窪 ) | - | 2020-09-11 | |||
临床1/2期 | 36 | 鏇齋觸築鏇衊簾憲範壓(構網繭遞構製膚蓋築觸) = 10 [27.8%] of 36 pts 壓範顧鏇觸獵獵顧齋簾 (廠襯憲鹹艱遞構淵夢築 ) 更多 | 积极 | 2020-05-25 |
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