预约演示
更新于：2025-07-19
Culmerciclib
库莫西利
更新于：2025-07-19
概要
基本信息
药物类型 小分子化药 |
别名 TQB 3616、TQB-3616、TQB3616 |
作用方式 抑制剂 |
作用机制 CDK2抑制剂(细胞周期蛋白依赖性激酶2抑制剂)、CDK4抑制剂(细胞周期蛋白依赖性激酶4抑制剂)、CDK6抑制剂(细胞周期蛋白依赖性激酶6抑制剂) |
在研适应症 |
非在研适应症 |
原研机构 |
在研机构 |
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- |
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结构/序列
分子式C24H27FN8 |
InChIKeyLLFOBMRPWNABCB-UHFFFAOYSA-N |
CAS号2004705-28-4 |
关联
18
项与 库莫西利 相关的临床试验CTR20244912
评价TQB3912片联合氟维司群注射液±TQB3616胶囊在局部晚期或转移性HR阳性、HER2阴性乳腺癌受试者中的有效性和安全性的Ib/II期临床试验
NCT06702618
Evaluation of the Efficacy and Safety of TQB3616 Capsules Combined With Hormonal Therapy in a Phase II Clinical Trial for Cyclin-dependent Kinases 4 and 6（CDK4/6)Inhibitor-Resistant, Hormone Receptor(HR)-Positive, Human Epidermal Growth Factor Receptor 2(HER2)-Negative Recurrent/Metastatic Breast Cancer
NCT06662773
Phase I Clinical Trial Evaluating Drug Drug Interactions of TQB3616 Capsules
100 项与 库莫西利 相关的临床结果
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100 项与 库莫西利 相关的转化医学
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100 项与 库莫西利 相关的专利（医药）
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5
项与 库莫西利 相关的文献（医药）2025-02-01Frontiers of Medicine
TRIM4 modulates the ubiquitin-mediated degradation of hnRNPDL and weakens sensitivity to CDK4/6 inhibitor in ovarian cancer
Article
作者: Shen, Yuhong ; Wang, Yiwei ; Guan, Xin ; Zhou, Tianyu ; Zhu, Chongying ; Che, Xiaoxia ; Feng, Weiwei ; Ruan, Yiyin ; Shen, Lifei ; Liu, Hua
Ovarian cancer is the most lethal malignancy affecting the female reproductive system. Pharmacological inhibitors targeting CDK4/6 have demonstrated promising efficacy across various cancer types. However, their clinical benefits in ovarian cancer patients fall short of expectations, with only a subset of patients experiencing these advantageous effects. This study aims to provide further clinical and biological evidence for antineoplastic effects of a CDK4/6 inhibitor (TQB4616) in ovarian cancer and explore underlying mechanisms involved. Patient-derived ovarian cancer organoid models were established to evaluate the effectiveness of TQB3616. Potential key genes related to TQB3616 sensitivity were identified through RNA-seq analysis, and TRIM4 was selected as a candidate gene for further investigation. Subsequently, co-immunoprecipitation and GST pull-down assays confirmed that TRIM4 binds to hnRNPDL and promotes its ubiquitination through RING and B-box domains. RIP assay demonstrated that hnRNPDL binded to CDKN2C isoform 2 and suppressed its expression by alternative splicing. Finally, in vivo studies confirmed that the addition of siTRIM4 significantly improved the effectiveness of TQB3616. Overall, our findings suggest that TRIM4 modulates ubiquitin-mediated degradation of hnRNPDL and weakens sensitivity to CDK4/6 inhibitors in ovarian cancer treatment. TRIM4 may serve as a valuable biomarker for predicting sensitivity to CDK4/6 inhibitors in ovarian cancer.
2025-01-01Frontiers in Pharmacology
The food effect on the pharmacokinetics of TQB3616 capsule in Chinse healthy subjects: a randomized, open-label, single-center, two-period, two-sequence crossover phase I clinical trial.
Article
作者: Yang, Haimiao ; Liu, Zhengzhi ; Zhou, Yanan ; Dai, Jun ; Zhang, Lei ; Wang, Yanli ; Cheng, Yang ; Zhang, Hong ; Deng, Qiaohuan ; Ren, Qing
Purpose:
The purpose of this study was to evaluate the food effect on the pharmacokinetics of TQB3616 capsule in Chinse healthy subjects.
Methods:
The subjects were randomly allocated to two distinct sequences in a 1:1 ratio. During each treatment periods, subjects ingested a single oral dose of 180 mg TQB3616 capsule administered with 240 mL of warm water under fasted and fed conditions. To avoid carryover effects, a 19 days washout period was strictly implemented between treatment periods. Blood samples were collected in accordance with the study protocol, and the plasma concentration of TQB3616 was measured using a fully validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. Safety evaluations were performed continuously throughout the duration of the trial.
Results:
Following the administration of TQB3616 capsules under both fasted and fed conditions, the geometric mean ratios of Cmax, AUC0-t, and AUC0- __-mml:math xmlns:mml="http://www.w3.org/1998/Math/MathML"-__∞
Conclusion:
A pharmacokinetic study conducted on healthy volunteers, who received a single 180 mg dose of TQB3616 capsules under fasting and fed conditions, demonstrated clinically significant effects of food on the drug's bioavailability. Compared with fasted, postprandial administration delayed median Tmax by 1 h while increasing total systemic exposure and peak concentration. Additionally, postprandial dosing was associated with reduced incidence of gastrointestinal adverse reactions. These data support the recommendation that TQB3616 capsules be administered with food to maximize therapeutic bioavailability while improving gastrointestinal tolerability profile.
Clinical Trial Registration:
http://www.chinadrugtrials.org.cn, identifier, CTR20210354; clinicaltrials.gov, identifier, NCT05344729.
2024-07-01Bioorganic & medicinal chemistry letters
Discovery and preclinical evaluations of TQB3616, a novel CDK4-biased inhibitor
Article
作者: Yang, Shuqun ; Liu, Yingchun ; Chen, Chen ; Chan, Chi-Chung ; Lin, Ruibin ; Chen, Shuhui ; Xia, Yuanfeng ; Xu, Xiongbin ; Ren, Bingjie ; Jiang, Wen ; Zhu, Xiaoyu ; Song, Baohui ; Tian, Xin ; Li, Jian ; Zhu, Yusong ; Li, Wei ; Zhang, Xiquan ; Xu, Zhaobing ; Hu, Lihong ; Yang, Ling ; Ding, Charles Z
Among small-molecule CDK4/6 inhibitors (palbociclib, ribociclib, and abemaciclib) approved for metastatic breast cancers, abemaciclib has a more tolerable adverse effects in clinic. This is attributable to preferential inhibition of CDK4 over CDK6. In our search for a biased CDK4 inhibitor, we discovered a series of pyrimidine-indazole inhibitors. SAR studies led us to TQB3616 as a preferential CDK4 inhibitor. TQB3616 exhibited improvements in both enzymatic and cellular proliferation inhibitory potency when tested side-by-side with the FDA approved palbociclib and abemaciclib. TQB3616 also possessed favorable PK profile in multiple species. These differentiated properties, together with excellent GLP safety profile warranted TQB3616 moving to clinic. TQB3616 entered into clinical development in 2019 and currently in phase III clinical trials (NCT05375461, NCT05365178).
100 项与 库莫西利 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 |
|---|---|---|---|---|
| HR阳性/HER2阴性乳腺癌 | 申请上市 | 中国 | 2024-07-19 | |
| HER2 阴性乳腺癌 | 临床3期 | 中国 | 2023-03-30 | |
| HR阳性乳腺癌 | 临床3期 | 中国 | 2022-03-18 | |
| HR阳性HER2阴性淋巴结阳性乳腺癌 | 临床3期 | 中国 | 2022-03-18 | |
| HEGF2阴性乳腺癌 | 临床3期 | 中国 | 2022-03-18 | |
| 去分化脂肪肉瘤 | 临床2期 | 中国 | 2022-07-29 | |
| 局部晚期非小细胞肺癌 | 临床2期 | 中国 | 2021-08-18 | |
| 非小细胞肺癌 | 临床2期 | 中国 | 2021-08-12 | |
| 小细胞肺癌 | 临床2期 | 中国 | 2021-08-12 | |
| 晚期乳腺癌 | 临床2期 | 中国 | 2021-02-04 |
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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1期 | - | 16 | TQB3616 capsule under fasted conditions | 齋觸繭淵廠夢網衊獵鑰(繭夢齋餘繭願遞鹽願顧) = 積衊築範衊鏇積範襯蓋 鑰壓膚鹽窪艱遞鬱顧齋 (選遞獵網顧網艱憲觸蓋 ) 更多 | 积极 | 2025-01-01 | |
临床3期 | HR阳性/HER2阴性乳腺癌 Hormone Receptor Positive | HER2 Negative | - | 憲築膚網製獵糧鑰簾獵(齋構構觸餘襯願廠積壓) = 鏇製醖衊顧鬱築鑰繭糧 淵製網積鏇憲窪蓋築衊 (壓簾範壓窪鑰餘窪襯廠 ) 更多 | 积极 | 2024-09-27 | ||
对照组 | 憲築膚網製獵糧鑰簾獵(齋構構觸餘襯願廠積壓) = 遞醖築餘鹽鬱觸製夢構 淵製網積鏇憲窪蓋築衊 (壓簾範壓窪鑰餘窪襯廠 ) 更多 | ||||||
临床2期 | 26 | 鏇蓋觸膚遞鹹壓選範觸(襯夢遞醖獵衊廠糧糧衊) = 鏇艱鹽觸繭淵顧窪鬱齋 鑰築餘餘繭膚鑰範鹹鏇 (膚膚鏇鑰遞網襯簾築鹽, 40.0% ∼79.9%) 更多 | 积极 | 2024-09-14 | |||
临床2期 | 111 | (1st-, 2nd-line BC (100% Chinese) + 1st-line) | 獵製衊衊築憲糧膚選願(夢構廠壓顧壓憲糧艱網) = 顧衊鹽壓窪築繭醖艱簾 鹹艱襯醖選糧糧醖艱鏇 (糧壓醖簾餘觸網淵鹹遞 ) 更多 | 优效 | 2024-01-01 | ||
(1st-, 2nd-line BC (100% Chinese) + 2nd-line) | 獵製衊衊築憲糧膚選願(夢構廠壓顧壓憲糧艱網) = 壓壓夢範鹽製艱鬱範範 鹹艱襯醖選糧糧醖艱鏇 (糧壓醖簾餘觸網淵鹹遞 ) 更多 |
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