WXFL10203614(WXFL10203614) - 药物靶点：JAK1_在研适应症：类风湿关节炎，活动性中度克罗恩病，活动性重度克罗恩病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

WXFL 10203614、WXFL-10203614、WXFL10203614

靶点

JAK1

作用机制

JAK1抑制剂(酪氨酸蛋白激酶JAK1抑制剂)

治疗领域

免疫系统疾病皮肤和肌肉骨骼疾病遗传病与畸形+ [1]

在研适应症

类风湿关节炎活动性中度克罗恩病活动性重度克罗恩病+ [3]

非在研适应症-

原研机构

无锡福欣医药研究开发有限公司

在研机构

无锡福祈制药有限公司

无锡福欣医药研究开发有限公司

非在研机构-

最高研发阶段临床3期

首次获批日期-

最高研发阶段(中国)临床3期

特殊审评-

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关联

12

项与 WXFL10203614 相关的临床试验

CTR20242140 / Recruiting临床2期

评价WXFL10203614片治疗中重度活动性克罗恩病（CD）安全性和有效性的多中心、剂量探索Ⅱ期临床研究

主要目的： (1)初步评价WXFL10203614片治疗中重度活动性CD的有效性和安全性； (2)探索WXFL10203614片治疗中重度活动性CD的最佳剂量。次要目的：评价WXFL10203614片在中重度活动性CD患者中的群体药代动力学特征。

开始日期2024-10-25

申办/合作机构

无锡福祈制药有限公司

CTR20242280 / Recruiting临床1期

[14C]WXFL10203614在中国成年健康男性受试者体内的吸收、代谢和排泄研究

本试验旨在评价中国成年男性健康受试者单剂量口服[14C] WXFL10203614的吸收、代谢和排泄，揭示受试物在人体内的药代动力学整体特征，为药物的临床合理使用提供参考。主要目的 1.定量分析受试者单次口服[14C]WXFL10203614后排泄物中的总放射性，获得人体放射性排泄率数据和主要排泄途径； 2.获得受试者口服[14C]WXFL10203614后人血浆、尿液和粪便的放射性代谢物谱，鉴定主要代谢产物，确定代谢途径及消除途径。 3.定量分析受试者单次口服[14C]WXFL10203614后全血和血浆中的总放射性，并考察全血和血浆中总放射性的分配情况。次要目的 1.采用已验证的液相色谱串联质谱联用法（LC-MS/MS）定量分析血浆中WXFL10203614及其代谢产物（如适用）的浓度，获得血浆中WXFL10203614及其代谢产物（如适用）的药动学参数。观察[14C]WXFL10203614单次给药后受试者的安全性。

开始日期2024-09-19

申办/合作机构

无锡福欣医药研究开发有限公司

CTR20242142 / Recruiting临床2期

评价WXFL10203614片治疗中重度活动性溃疡性结肠炎（UC）安全性和有效性的多中心、剂量探索Ⅱ期临床研究

主要目的： (1)初步评价WXFL10203614片治疗中重度活动性UC的有效性和安全性； (2)探索WXFL10203614片治疗中重度活动性UC的最佳剂量。次要目的：评价WXFL10203614片在中重度活动性UC患者中的群体药代动力学特征。

开始日期2024-09-13

申办/合作机构

无锡福祈制药有限公司

100 项与 WXFL10203614 相关的临床结果

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100 项与 WXFL10203614 相关的转化医学

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100 项与 WXFL10203614 相关的专利（医药）

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2

项与 WXFL10203614 相关的文献（医药）

Frontiers in pharmacology

Safety, tolerability and pharmacokinetics of WXFL10203614 in healthy Chinese subjects: A randomized, double-blind, placebo-controlled phase Ⅰ study

Article

作者: Zhang, Zhiwei ; Wang, Jiakun ; Xu, Jianguo ; Que, Linling ; Shi, Yunfei ; Huang, Kai ; He, Qing ; Ding, Ying ; Qian, Zhenzhong ; Gu, Xianghong ; Qin, Wei ; Chen, Yuanxin ; Chu, Nannan

Objective: This study was conducted to investigate the safety, tolerability and pharmacokinetics (PK) of WXFL10203614 after single and multiple oral doses in healthy Chinese subjects.Methods: A single-center, randomized, double-blind, placebo-controlled phase Ⅰ study was performed on healthy Chinese subjects. In the single-dose study, Subjects were randomized into 7 dose levels of WXFL10203614 (1 mg group, n = 2; 2, 5, 10, 17, 25 and 33 mg groups with placebo, 8 subjects per group, 2 of them given placebo). In the multiple-dose study, subjects received 5 or 10 mg WXFL10203614 once daily (QD), 5 mg twice daily (BID) or placebo for 7 consecutive days. Safety, tolerability and PK of WXFL10203614 were all assessed.Results: A total of 592 subjects were screened, 50 subjects were enrolled in the single-dose study and 30 in the multiple-dose study. All adverse events (AEs) were mild or moderate and resolved spontaneously. No Serious Adverse Events (SAEs) or deaths were reported during the study. WXFL10203614 was absorbed rapidly after dosing with Tmax of 0.48–0.98 h, Cmax, AUC0-t and AUC0-∞ were all increased in a dose-related manner over the range of 1–33 mg. Renal excretion was the major route of elimination of WXFL10203614. Steady-state PK parameters (Cmax,ss, AUC0-t,ss and AUC0-∞,ss) were elevated after once-daily administration of 5–10 mg WXFL10203614 and non- and weak drug accumulations were observed, whereas moderate drug accumulation occurred in the 5 mg BID group.Conclusion: WXFL10203614 exhibited good safety, tolerability and favorable PK profiles in healthy Chinese subjects, supporting further clinical development in patients with rheumatoid arthritis.Clinical Trials Registration Number:http://www.chinadrugtrials.org.cn/index.html, #CTR20190069 and CTR20200143.

Frontiers in pharmacology

The effect of food on the pharmacokinetics of WXFL10203614, a potential selective JAK1 inhibitor, in healthy Chinese subjects

Article

作者: Huang, Kai ; Chu, Nannan ; Wang, Jiakun ; He, Qing ; Gu, Xianghong ; Qian, Zhenzhong ; Qin, Wei ; Xu, Jianguo ; Shi, Yunfei ; Zhang, Zhiwei ; Ding, Ying ; Que, Linling

Objective: This study was performed to investigate the effect of food on the pharmacokinetics (PK) of WXFL10203614 in healthy Chinese subjects.Methods: This was a randomized, open-label, single-dose, two-treatment (fed vs fasted), two-period, two-sequence, crossover study. 14 eligible subjects were averagely randomized into 2 sequences and then received 10 mg WXFL10203614 under fasted or fed condition. In each period, the blood samples were collected from 0 h (pre-dose) and serially up to 72 h post-dose, and plasma concentrations were detected using the high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method. The effect of food on the PK profile and safety of WXFL10203614 were assessed.Results: 70 subjects were screened, and 14 subjects (10 male and 4 female) were enrolled and completed the study. Under the fasted condition, WXFL10203614 was absorbed rapidly with a Tmax of 0.98 h. The absorption rate was slower, Tmax delayed by 2.98 h, and the Cmax decreased by 16.3% when WXFL10203614 administered after the high-fat and high-calorie diet, other PK parameters were not affected. The 90% confidence intervals (CIs) for the ratio (fed/fasted) of geometric means of the Cmax, AUC0-t and AUC0-∞ were 0.73–1.01, 0.90–1.03 and 0.90–1.03, indicating that the high-fat and high-calorie diet might impact the absorption process of WXFL10203614. Although the Cmax was slightly decreased, there was no significant difference in the Cmax under fasted and fed conditions. Thus, it was not considered clinically significant owing to the small magnitude of changes in Cmax. All Treatment-emergent adverse events (TEAEs) were mild and resolved spontaneously without treatment.Conclusion: Food had no clinically relevant effects on drug system exposure of WXFL10203614. It was well tolerated under fasted and fed conditions in healthy Chinese subjects, so WXFL10203614 could be administered orally with or without food.Clinical Trial Registration: http://www.chinadrugtrials.org.cn/index.html, identifier CTR20191636.

1

项与 WXFL10203614 相关的新闻（医药）

2024-02-23

·米内网

【瞩目】中药1类新药获批！240亿市场风云再起

精彩内容近日，NMPA官网显示，卓和药业的中药1.1类创新药九味止咳口服液获批上市，用于治疗急性支气管炎风热咳嗽证。米内网数据显示，2022年中国三大终端六大市场止咳祛痰平喘中成药销售额超过240亿元。中药1.1类创新药九味止咳口服液来源于邹学熹教授临床经验方，具有宣肺止咳之功效，用于治疗急性支气管炎风热咳嗽证，处方由矮地茶、枇杷叶、麻黄、苦杏仁、薄荷、陈皮、竹茹、鱼腥草和炙甘草组成。该药品的上市为急性气管-支气管炎咳嗽患者提供了又一种治疗选择。止咳祛痰平喘中成药是家庭药箱中的常备药品。米内网数据显示，2022年中国三大终端六大市场（统计范围见文末）止咳祛痰平喘中成药销售额超过240亿元，大幅增长19.29%。中国三大终端六大市场止咳祛痰平喘中成药销售情况（单位：万元）来源：米内网格局数据库经过疫情的洗礼，止咳祛痰平喘中成药市场重回增长轨道。米内网数据显示，2023H1中国城市实体药店终端止咳祛痰平喘中成药销售额超过60亿元，大幅增长55.43%。产品TOP20中，京都念慈菴蜜炼川贝枇杷膏、急支糖浆、铁皮枫斗颗粒位列前三，10个独家品种上榜。2023H1中国公立医疗机构终端止咳祛痰平喘中成药销售额超过80亿元，大幅增长53.57%。其中，止咳祛痰平喘中成药TOP5品牌分别为扬子江海燕药业的苏黄止咳胶囊、上海凯宝药业的痰热清注射液、贵州健兴药业的肺力咳合剂、康隆药业的强力枇杷露、太极集团的急支糖浆。卓和药业集团股份有限公司于2017年成立于无锡市锡山区，除了中药1.1类创新药，公司有2款化药1类创新药注射用WXWH0075（抗感染）、WXFL10203614片（治疗溃疡性结肠炎）已获批临床。资料来源：米内网数据库、NMPA注：米内网《中国三大终端六大市场药品竞争格局》，统计范围是：城市公立医院和县级公立医院、城市社区中心和乡镇卫生院、城市实体药店和网上药店，不含民营医院、私人诊所、村卫生室，不含县乡村药店；上述销售额以产品在终端的平均零售价计算。本文为原创稿件，转载请注明来源和作者，否则将追究侵权责任。投稿及报料请发邮件到872470254@qq.com稿件要求详询米内微信首页菜单栏商务及内容合作可联系QQ：412539092●温馨提示●因为微信公众号修改了推送规则，最近很多读者反映没有及时看到推文。把米内网设为“星标”，就能每天与我们不见不散啦，具体操作如下：【分享、点赞、在看】点一点不失联哦

上市批准

100 项与 WXFL10203614 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
类风湿关节炎	临床3期	中国	无锡福欣医药研究开发有限公司	2023-08-31
活动性中度克罗恩病	临床2期	中国	无锡福祈制药有限公司	2024-10-25
活动性重度克罗恩病	临床2期	中国	无锡福祈制药有限公司	2024-10-25
活动性中度溃疡性结肠炎	临床2期	中国	无锡福祈制药有限公司	2024-09-13
活动性重度溃疡性结肠炎	临床2期	中国	无锡福祈制药有限公司	2024-09-13
特应性皮炎	临床2期	中国	无锡福祈制药有限公司	2024-08-14

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临床结果

适应症

分期

评价

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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


CTR20190069 \| CTR20200143 (Pubmed) 人工标引	临床1期	-	80	WXFL10203614	夢壓餘製築積觸壓鹽鬱(繭鏇簾衊鏇繭積齋襯獵) = All adverse events (AEs) were mild or moderate and resolved spontaneously. 積獵顧獵齋廠夢醖鬱簾 (壓鬱膚餘製廠鹹襯願鑰 )	积极	2022-11-04