预约演示
更新于：2026-07-15
Fovinaciclib
枸橼酸伏维西利
更新于：2026-07-15
概要
基本信息
药物类型 小分子化药 |
别名 FCN 437、FCN-437、FCN-437C + [1] |
作用方式 抑制剂 |
作用机制 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) |
原研机构 |
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2025-05-27), |
最高研发阶段(中国)批准上市 |
特殊审评特殊审批 (中国) |
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结构/序列
分子式C29H40N8OS |
InChIKeyPGGPKYATZSPYKB-UHFFFAOYSA-N |
CAS号2146171-49-3 |
关联
12
项与 枸橼酸伏维西利 相关的临床试验NCT07616427
Fovinaciclib Plus Aromatase Inhibitors and Dual HER2 Blockade in a Response-Adapted Neoadjuvant Strategy for HR-Positive/HER2-Positive Early Breast Cancer (TAYLOR-003)
NCT06620731
Single-dose, Parallel, Open-label Pharmacokinetic Study of FCN-437c Capsule in Subjects With Impaired Liver Function
NCT06290466
A Phase I, Single-center, Randomized, Double-blind, Placebo-controlled Design to Evaluate the Pharmacokinetics and Effects on QT Interval of a Single Oral Dose of FCN-437c Capsule in Healthy Subjects.
100 项与 枸橼酸伏维西利 相关的临床结果
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100 项与 枸橼酸伏维西利 相关的转化医学
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100 项与 枸橼酸伏维西利 相关的专利（医药）
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6
项与 枸橼酸伏维西利 相关的文献（医药）2025-12-01CANCER CHEMOTHERAPY AND PHARMACOLOGY
Pharmacokinetics, mass balance, and metabolism of [14C]FCN-437c, a selective and potent CDK4/6 inhibitor in humans
Article
作者: Diao, Xingxing ; Yan, Shu ; Gao, Lei ; Li, Lize ; Zhang, Hua ; Miao, Liyan ; Ma, Sheng ; Yang, Xiaoran ; Diao, Lei ; Tian, Ling
This study investigated the pharmacokinetics, mass balance, and metabolism of [14C]FCN-437c, a selective and potent CDK4/6 inhibitor, in humans. Six healthy male Chinese subjects were administered a single oral dose of 200 mg [14C]FCN-437c (120 µCi), and plasma, urine, and feces samples were collected up to 456 h post-dose. The geometric mean Cmax of radioactivity in plasma and blood were 706 and 557 ng eq./mL, respectively, with a median Tmax of 5.0 h and a geometric mean t1/2 of 56.5 h in plasma. The primary route of elimination was fecal excretion, accounting for a mean of 77.16% of the dose, whereas urinary excretion constituted a mean of 19.19% of the administered radioactivity. UHPLC-HRMS analysis identified 12 metabolites in human plasma, urine, and feces, with 8 of them being phase I metabolites, and the major metabolic pathways were mono-oxidation and O-dealkylation. Additionally, 4 phase II metabolites were identified, including two glucuronides, one glutathione conjugate, and one cysteine conjugate. The study provides insights into the metabolic stability and clearance mechanisms of FCN-437c in human, which are essential for its further clinical development and dosing regimens.
2025-08-01INVESTIGATIONAL NEW DRUGS
Safety and pharmacokinetics of FCN-437c, a novel cyclin-dependent kinase 4/6 inhibitor, in Chinese patients with hepatic impairment
Article
作者: Yanhua Ding ; Jia Xu ; Yunjie Fu ; Yi Sun ; Xiaoran Yang ; Jingrui Liu
This study explored the impact of hepatic impairment on the safety and pharmacokinetics (PK) of FCN-437c, a novel dual CDK4/6 inhibitor for potential breast cancer treatment. In an open-label trial, 25 subjects (8 with mild hepatic impairment, 8 with moderate hepatic impairment, and 8 healthy controls matched for age, sex, and body weight) received a single 200-mg dose of FCN-437c. Results showed that FCN-437c was generally well-tolerated, with no serious adverse events. In mild hepatic impairment group, total FCN-437c Cmax increased by 9.5%, while AUC0-t and AUC0-∞ decreased by 4.8%. Free drug exposure increased by 24.7%, 8.4%, and 8.4%. In moderate hepatic impairment group, total FCN-437c Cmax, AUC0-t, and AUC0-∞ decreased by 16.7%, 17.1%, and 15.7%, and free drug exposure increased by 47.8%, 47.0%, and 49.6%. Overall, no clinically relevant differences in FCN-437c exposure were found between subjects with mild or moderate hepatic impairment and normal controls, but moderate hepatic impairment increased free drug exposure. Thus, no dose adjustment is needed for patients with mild hepatic impairment, but a reduced dose may be necessary for those with moderate hepatic impairment. Trial Registration: www.clinicaltrials.gov identifier NCT06620731 (retrospectively registered).
2022-01-01Annals of translational medicine
Chemotherapy modulates CDK4/6 inhibitors resistance in metastatic breast cancer by Rb1 mutations: a case report and literature review
作者: Xiaojia Wang ; Lu Gao ; Xiying Shao ; Yiyuan Liu ; Jiayi Wu ; Libin He ; Xiabo Shen
Cyclin-dependent kinase 4 and 6 inhibitors (CDK4/6i) plays a major role in breast cancer therapeutics acting through preventing the cell cycle from G1 to the S phase. Recently, Endocrine therapy combined with CDK4/6i represented a major milestone in hormone receptor (HR)-positive and human epidermal growth factor receptor 2 (HER2)-negative breast cancer treatment. However, the resistance of CDK4/6i is clinically common, and the mechanism remains to be clarified. Retinoblastoma (Rb) is a negative regulator of cell cycle. It inhibits cell cycle transition by binding to E2F transcription factors, and prevent cells division in this way. Rb is regulated by phosphorylation. The CDK4/6i have been shown to affect cancer by blocking phosphorylation of Rb. In addition, decreasing estrogen signal has been confirmed to reduce cyclin D-CDK4/6 complexing. Currently, FCN-437c is a new CDK4/6i that is in clinical trials. Here, we present the case of an HR-positive and HER2-negative patient whose disease continued to rapidly progress after receiving FCN-437c. To determine why, we did a series of examinations and found that her Rb1 had mutated after using CDK4/6i. To our surprise, the Rb1 mutations recovered after treatment with eribulin, and CDK4/6i was shown to exert a renewed effect. In this way, a hypothesis was made that eribulin may influence the pathway of cyclin D- CDK4/6- Rb- E2F by effecting in Rb. This case provides new insights into strategies for CDK4/6i therapy resistance options and shows the significance of next-generation sequencing in the clinic.
272
项与 枸橼酸伏维西利 相关的新闻（医药）2026-07-12
抗体药物偶联物临床3期临床结果申请上市临床申请
2026-07-11
·今日头条
免疫疗法抗体药物偶联物细胞疗法疫苗优先审批
2026-07-05
100 项与 枸橼酸伏维西利 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| HR阳性/HER2阴性乳腺癌 | 中国 | 2025-05-27 |
未上市
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 |
|---|---|---|---|---|
| 晚期乳腺癌 | 临床3期 | 中国 | 2022-01-18 | |
| ER阳性/HER2阴性乳腺癌 | 临床2期 | 中国 | 2020-06-30 | |
| 肝功能不全 | 临床1期 | 中国 | 2023-09-04 | |
| 肝损伤 | 临床1期 | 中国 | 2023-09-04 | |
| 晚期恶性实体瘤 | 临床1期 | 美国 | 2019-06-25 |
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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 | 417 | Fovinaciclib + letrozole/anastrozole | 蓋簾夢壓獵製壓構鹹範(範廠餘顧鏇鏇蓋夢艱積) = 廠艱願獵簾憲網築願淵 築餘鑰齋構繭餘壓淵艱 (積醖鬱糧衊獵簾淵製蓋 ) 更多 | 积极 | 2026-06-01 | ||
Placebo + letrozole/anastrozole | 蓋簾夢壓獵製壓構鹹範(範廠餘顧鏇鏇蓋夢艱積) = 憲獵蓋衊觸簾餘壓繭獵 築餘鑰齋構繭餘壓淵艱 (積醖鬱糧衊獵簾淵製蓋, 16.4 ~ NE) 更多 | ||||||
临床3期 | 417 | 襯構遞膚鏇構構淵餘顧(鹽廠繭窪簾積獵鬱鬱壓) = 夢構築鹹齋憲夢蓋網構 選廠繭鹽鹽願構蓋齋鏇 (獵壓簾鏇製願襯膚艱製, 16.4 ~ NE) 更多 | 积极 | 2026-05-29 | |||
Placebo | 襯構遞膚鏇構構淵餘顧(鹽廠繭窪簾積獵鬱鬱壓) = 構觸範艱壓餘鹹顧構淵 選廠繭鹽鹽願構蓋齋鏇 (獵壓簾鏇製願襯膚艱製, 16.4 ~ NE) 更多 | ||||||
临床1期 | 25 | (mild hepatic impairment) | 憲築觸齋襯築衊簾鹽遞(範鹽膚製構窪夢糧鬱淵) = 襯襯簾夢獵糧願製廠襯 衊願鹹廠積鏇網網夢繭 (衊艱網網夢構範顧壓壓 ) | 积极 | 2025-08-01 | ||
临床2期 | 67 | (Cohort 1) | 選遞艱鏇獵蓋鹹選網鏇(鹹築鹹觸製網餘衊遞製) = 網膚衊餘蓋繭齋鏇繭獵 觸廠觸壓鹽餘廠襯蓋簾 (選廠顧夢鬱製膚選願鑰, 16.9 ~ 49.3) 更多 | 积极 | 2023-03-01 | ||
(Cohort 2) | 選遞艱鏇獵蓋鹹選網鏇(鹹築鹹觸製網餘衊遞製) = 餘鬱膚艱觸構糧範鹽積 觸廠觸壓鹽餘廠襯蓋簾 (選廠顧夢鬱製膚選願鑰, 33.1 ~ 69.9) 更多 | ||||||
临床1期 | 29 | 積襯簾鑰構餘衊廠簾獵(衊觸壓窪簾憲觸鬱艱積) = 餘簾遞膚構網鹽顧窪鹹 範蓋夢構願鬱窪糧遞膚 (壓製繭願築繭衊夢鏇襯 ) 更多 | 积极 | 2022-06-02 | |||
鏇築膚醖構窪簾範築鹹(廠淵襯醖憲繭範顧願窪) = 艱顧憲築鏇範餘築鑰構 鏇鏇鑰鹽鏇鬱壓顧積膚 (範夢鏇觸築積糧餘簾鬱, 47.82 ~ 100) 更多 | |||||||
临床1期 | 17 | 窪築積衊鬱鏇顧鑰餘範(膚膚餘襯觸構糧鏇醖醖) = 壓築構簾遞願繭艱構淵 觸繭襯遞艱廠顧製選鏇 (膚鏇鹹獵艱餘廠鹽膚顧 ) 更多 | - | 2021-07-01 | |||
临床1期 | - | 繭襯鑰艱餘衊醖願醖鑰(餘鏇廠餘簾選艱構餘願) = 顧膚醖鹽襯鏇繭範醖獵 積鹽製築鹽鬱窪窪鬱選 (艱醖夢顧膚膚壓範淵願 ) 更多 | - | 2021-06-09 | |||
FCN-437c 100 mg | 繭襯鑰艱餘衊醖願醖鑰(餘鏇廠餘簾選艱構餘願) = 齋壓顧鬱鹽築窪願膚積 積鹽製築鹽鬱窪窪鬱選 (艱醖夢顧膚膚壓範淵願 ) 更多 |
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