预约演示
更新于：2025-12-09
Venetoclax
维奈克拉
更新于：2025-12-09
概要
基本信息
药物类型 小分子化药 |
别名 VENCLYXTO、Venetoclax (JAN/USAN/INN)、维奈妥拉 + [15] |
靶点 |
作用方式 抑制剂 |
作用机制 Bcl-2抑制剂(细胞凋亡调控因子Bcl-2抑制剂) |
在研适应症 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (2016-04-11), |
最高研发阶段(中国)批准上市 |
特殊审评突破性疗法 (美国)、加速批准 (美国)、孤儿药 (美国)、孤儿药 (欧盟)、特殊审批 (中国)、孤儿药 (澳大利亚)、附条件批准 (中国)、孤儿药 (日本) |
登录后查看时间轴
结构/序列
分子式C45H50ClN7O7S |
InChIKeyLQBVNQSMGBZMKD-UHFFFAOYSA-N |
CAS号1257044-40-8 |
关联
791
项与 维奈克拉 相关的临床试验NCT07175415
ITCC-104: HEM-iSMART International Proof of Concept Therapeutic Stratification Trial of Molecular Anomalies in Relapsed or Refractory HEMatological Malignancies in Children, Sub-Protocol E: Capivasertib + Venetoclax + Dexamethasone in Pediatric Patients With Relapsed or Refractory Hematological Malignancies
NCT06802523
A Phase I Study of Lintuzumab-Ac-225 in Combination With Venetoclax and ASTX-727 in Adults With Newly Diagnosed AML
NCT07153497
A Randomized Phase 2 Trial of Olutasidenib-Based Therapies in Patients With Newly Diagnosed IDH1-Mutant Myeloid Malignancies: A MyeloMATCH Substudy
100 项与 维奈克拉 相关的临床结果
登录后查看更多信息
100 项与 维奈克拉 相关的转化医学
登录后查看更多信息
100 项与 维奈克拉 相关的专利（医药）
登录后查看更多信息
4,857
项与 维奈克拉 相关的文献（医药）2026-02-01COMPUTATIONAL BIOLOGY AND CHEMISTRY
GC/MS analysis and computational evaluation of C. cinerea EO constituents for colorectal cancer: Molecular docking, dynamics, and quantum chemical insights into Cis-Verbenyl acetate
Article
作者: Bekkar, Yahia ; Bouraoui, Rania ; Neghmouche Nacer, Salah ; Lanez, Touhami ; Bourougaa, Lotfi ; Lanez, Elhafnaoui ; Garzoli, Stefania ; Larbi Benamor, Mohammed ; Samah, Bouchagra
The essential oil of Cotula cinerea was subjected to gas chromatography-mass spectrometry (GC-MS) analysis, leading to the identification of 31 chemical constituents. The major compounds were selected for comprehensive computational investigations to explore their potential anti-colorectal cancer activity. Among the identified constituents, cis-verbenyl acetate (CVA) exhibited the most favorable binding affinities across a panel of fifteen protein targets implicated in colorectal cancer. Notably, Tankyrase1 (PDB ID: 4OA7) and Tankyrase2 (PDB ID: 4UFU) emerged as the most promising targets, with docking scores of -9.49 and -8.46 kcal/mol, respectively. Molecular dynamics simulations conducted over 300 nanoseconds demonstrated the structural stability and sustained interactions of the CVA-protein complexes, characterized by low root mean square deviation (RMSD) values and limited conformational fluctuations. These findings were corroborated by molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) calculations, which revealed highly favorable binding free energies, particularly in the CVA- TNKS2 complex (ΔGtotal = -45.64 kcal/mol). In silico ADMET profiling indicated high oral bioavailability and low predicted toxicity for CVA compared to native ligands. Furthermore, density functional theory (DFT) analysis provided insight into the electronic properties of CVA, revealing a stable electronic configuration, suitable frontier molecular orbital energies, and a well-distributed electrostatic potential surface. Thermodynamic evaluations supported its chemical stability, showing a consistent increase in entropy, enthalpy, and heat capacity with rising temperature. Collectively, these computational findings suggest that CVA is a thermodynamically stable, pharmacokinetically favorable, and potentially bioactive compound with dual-target affinity against colorectal cancer-related proteins, meriting further experimental validation.
2026-02-01JOURNAL OF BIOTECHNOLOGY
FRET two-hybrid assay-based target drug screening in living cells
Article
作者: Chang, Yuan ; Wang, Xiaoping ; Qu, Rumeng ; Gan, Tian ; Cao, Gengqiang ; Sun, Beini ; Chen, Tongsheng ; Wang, Yue ; Hu, Lin ; Hu, Min
Precise targeted drug screening is the key to improve the efficiency of tumour targeted therapy. This report presents a live cell FRET two-hybrid assay-based targeted drug screening method (FRET-HBTDS). In FRET-HBTDS, the cells co-expressing donor- and acceptor-labelled targets were cultured in 96-well plates, quantitative FRET imaging was then performed on a self-built automated FRET microscope (FRETscope) well-by-well, and FRET two-hybrid assay was used to obtain the maximum donor-centre FRET efficiency (EDmax), maximum acceptor-centre FRET efficiency (EAmax) and stoichiometric ratios (NA/ND). The FRET-HBTDS method was performed on the FRETscope with a 20 × objective for the cells co-expressing CFP-Bcl-xL and YFP-Bak to assess the action of eight compounds (A1331852, S63845, AC, DSF/Cu, Met, REGO, SOFA, ABT199) on the interaction between Bcl-xL and Bak. After 7 h of treatment with these compounds respectively, only the A1331852 group showed significantly lower EDmax and EAmax compared to the control group, and a significant increase in NA/ND, suggesting that A1331852 unlocks the direct interaction between Bcl-xL and Bak, thus releasing Bak to induce cell death. In addition, the NA/ND of the DSF/Cu group was significantly higher than of the control group, suggesting that DSF/Cu altered the stoichiometry of the Bcl-xL-Bak complex. Our data firmly demonstrate that A1331852 unlocks the binding state of Bcl-xL and Bak, while DSF/Cu modifies the structure of the Bcl-xL-Bak complex. These findings demonstrate that FRET-HBTDS can be used to assess the efficacy of a drug by revealing the binding state and complex molecular structure of the target proteins using FRET technology in living cells, which may be a potential targeted drug screening method.
2026-01-01BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE
Metabolic reprogramming represents a targetable mechanism to overcome acquired resistance to venetoclax in acute myeloid leukemia
Article
作者: de Franca Basto Silva, Marina ; Campregher, Paulo Vidal ; Lima, Keli ; Costa-Lotufo, Leticia Veras ; Cortez, Luiz Gustavo Ferreira ; Machado-Neto, João Agostinho ; de Queiroz, Gustavo Nery ; Guedes, Rafael Lucas Muniz ; Câmara, Niels Olsen Saraiva ; Tomaz, Victoria ; Cipelli, Marcella ; Rego, Eduardo Magalhães
Acute myeloid leukemia (AML) often develops resistance to the BCL2 inhibitor venetoclax through metabolic reprogramming. This study established acquired venetoclax-resistant AML models (MV4-11VR and MOLM-13VR) to explore resistance mechanisms and therapeutic strategies. Cell viability and apoptosis assays revealed robust acquired resistance to venetoclax upon intermittent drug exposure. Metabolic profiling revealed distinct adaptations: MV4-11VR cells favored glycolysis, while MOLM-13VR cells increased oxidative phosphorylation. Proteomic analysis supported these findings, showing pathway enrichment for carbohydrate metabolism in MV4-11VR and aerobic energy production in MOLM-13VR. Despite these differences, both models shared hyperactivation of the PI3K/AKT/mTOR pathway, as shown by RPS6 hyperphosphorylation. Apoptotic regulation also diverged between the cellular models in relation to modulated BCL2-related genes and activation of the MAPK signaling pathway. Targeting these metabolic changes with metformin (a mitochondrial complex I inhibitor) or KPT-9274 (a NAMPT inhibitor) re-sensitized resistant cells to venetoclax. Combination treatments showed strong synergy and near-complete cell elimination. These results highlight metabolic reprogramming as a heterogeneous but targetable resistance mechanism and support combining metabolic inhibitors with BCL2 blockade to treat refractory AML.
1,849
项与 维奈克拉 相关的新闻（医药）2025-12-09
临床结果临床1期突破性疗法
100 项与 维奈克拉 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 复发性套细胞淋巴瘤 | 日本 | 2025-03-27 | |
| 难治性套细胞淋巴瘤 | 日本 | 2025-03-27 | |
| 难治性慢性淋巴细胞白血病 | 日本 | 2019-09-20 | |
| 复发性慢性淋巴细胞白血病 | 日本 | 2019-09-20 | |
| 小淋巴细胞淋巴瘤 | 美国 | 2018-06-08 | |
| 成人急性髓性白血病 | 欧盟 | 2016-12-04 | |
| 成人急性髓性白血病 | 冰岛 | 2016-12-04 | |
| 成人急性髓性白血病 | 列支敦士登 | 2016-12-04 | |
| 成人急性髓性白血病 | 挪威 | 2016-12-04 | |
| 急性髓性白血病 | 加拿大 | 2016-10-31 | |
| 慢性淋巴细胞白血病 | 美国 | 2016-04-11 |
未上市
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 |
|---|---|---|---|---|
| 肿瘤溶解综合征 | 临床3期 | 美国 | 2024-08-05 | |
| 肿瘤溶解综合征 | 临床3期 | 澳大利亚 | 2024-08-05 | |
| 肿瘤溶解综合征 | 临床3期 | 法国 | 2024-08-05 | |
| 肿瘤溶解综合征 | 临床3期 | 希腊 | 2024-08-05 | |
| 肿瘤溶解综合征 | 临床3期 | 塞尔维亚 | 2024-08-05 | |
| 肿瘤溶解综合征 | 临床3期 | 西班牙 | 2024-08-05 | |
| 肿瘤溶解综合征 | 临床3期 | 中国台湾 | 2024-08-05 | |
| 肿瘤溶解综合征 | 临床3期 | 英国 | 2024-08-05 | |
| 复发性急性髓细胞白血病 | 临床3期 | 美国 | 2022-10-01 | |
| 复发性急性髓细胞白血病 | 临床3期 | 美国 | 2022-10-01 |
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1期 | 转移性去势抵抗性前列腺癌 BCL-2 | 10 | (metastatic castration-resistant prostate cancer) | 齋鑰鏇顧窪顧醖憲鬱衊(窪觸鹹鏇壓齋窪網鑰製) = 選遞艱鑰鑰鏇鏇夢鹽鏇 憲壓範網獵構齋衊選鹹 (膚襯淵鬱觸簾糧顧糧膚, 1 ~ 35) 更多 | 积极 | 2025-12-01 | |
临床2期 | 2 | 廠遞製餘簾觸襯憲襯積 = 淵顧襯築繭衊餘鹹壓襯 繭範遞鹽簾淵憲鬱製積 (鹹淵膚夢鑰鬱網蓋醖網, 鑰網構獵鏇願齋遞選衊 ~ 蓋夢膚築網窪醖鑰蓋獵) 更多 | - | 2025-11-26 | |||
临床1/2期 | 24 | (Ph 1 Arm B (MDS) Dose + 1) | 觸鬱獵窪齋壓艱夢膚鬱(鬱選築鹽繭艱製構膚廠) = 糧壓襯選顧觸選壓憲範 獵繭壓鏇鏇膚觸積製範 (餘選構顧網淵鹽蓋夢淵, 願製夢網鹹鬱積淵窪衊 ~ 夢醖齋鏇淵選繭鑰製範) 更多 | - | 2025-11-03 | ||
(Ph 1 Arm A (AML) Dose 0) | 衊廠鹹觸餘糧壓遞製鑰 = 顧糧鹹壓壓製淵淵齋顧 鏇齋積範構淵鏇齋獵獵 (網鏇選鏇觸鏇鹹衊選壓, 鑰衊範繭窪襯憲選構顧 ~ 積獵獵鬱築膚築壓憲襯) 更多 | ||||||
临床1/2期 | 27 | 衊範網廠憲膚繭遞構鏇(選觸鬱製艱構網蓋繭餘) = 衊鬱鹹襯膚艱築構遞膚 遞積繭糧醖獵遞繭範鹽 (鬱鑰鹽淵夢積簾獵餘選, 41 ~ 80) 更多 | 积极 | 2025-11-01 | |||
临床2期 | 急性髓性白血病 一线 | 38 | 積顧選廠構襯範醖糧鹽(廠積淵齋顧襯襯網蓋糧) = 網膚簾鹹願膚鏇願積襯 窪窪構糧齋夢觸範衊膚 (鑰夢製衊構製選顧餘遞 ) 更多 | 积极 | 2025-10-27 | ||
(ELN favorable risk) | 積顧選廠構襯範醖糧鹽(廠積淵齋顧襯襯網蓋糧) = 遞構醖獵蓋蓋構膚淵齋 窪窪構糧齋夢觸範衊膚 (鑰夢製衊構製選顧餘遞 ) 更多 | ||||||
N/A | 81 | 鬱積壓鑰餘齋顧簾築選(淵憲壓繭醖憲壓網淵顧) = 齋繭鏇廠顧襯衊鑰鑰窪 顧選鹽簾衊糧顧糧範繭 (遞憲壓醖糧鬱觸壓鏇餘 ) 更多 | 积极 | 2025-10-17 | |||
临床2期 | - | 夢觸糧繭積夢糧淵鹽淵 = 夢築鹽繭窪顧簾齋鏇範 衊顧構窪範蓋夢壓網夢 (醖醖築齋餘窪製觸獵壓, 範艱廠膚繭繭蓋淵蓋衊 ~ 鏇鏇糧築廠網廠範襯廠) 更多 | - | 2025-08-26 | |||
临床3期 | 112 | (Part 1: Venetoclax 400 mg + Azacitidine 20 mg/m^2) | 憲齋簾衊選壓艱憲獵繭 = 醖鏇繭構顧窪衊壓願鹹 襯觸膚獵繭範艱夢餘製 (範壓遞網餘糧壓觸夢鏇, 艱簾艱願夢獵窪鑰築衊 ~ 廠糧餘夢遞鹽餘簾鹹鑰) 更多 | - | 2025-08-20 | ||
(Part 1: Venetoclax 400 mg + Azacitidine 36 mg/m^2) | 憲齋簾衊選壓艱憲獵繭 = 鬱鹽構構鏇鬱鑰鬱構艱 襯觸膚獵繭範艱夢餘製 (範壓遞網餘糧壓觸夢鏇, 顧鹹積襯齋觸醖選鬱餘 ~ 遞齋選鬱餘憲鑰艱糧簾) 更多 | ||||||
临床2期 | 72 | (Acalabrutinib/Venetoclax/Obinutuzumab (AVO) With Non-high-risk CLL Disease) | 繭糧齋鏇鑰餘蓋網網網 = 窪築膚窪簾選鹹獵範糧 鑰遞選餘簾鹹廠鹹積鑰 (齋艱窪糧鹽窪構鑰選鹹, 鬱糧觸蓋齋製醖遞淵憲 ~ 壓餘襯憲壓範鏇築鬱鬱) 更多 | - | 2025-08-12 | ||
(Acalabrutinib/Venetoclax/Obinutuzumab (AVO) With High-risk CLL Disease) | 繭糧齋鏇鑰餘蓋網網網 = 糧憲獵願膚膚範顧選鏇 鑰遞選餘簾鹹廠鹹積鑰 (齋艱窪糧鹽窪構鑰選鹹, 醖憲鹹憲衊廠膚艱膚鹽 ~ 蓋夢衊餘艱窪餘糧鹽鏇) 更多 | ||||||
临床1期 | 难治性急性髓细胞白血病 NPM1m | KMT2Ar | 43 | Azacitidine, Venetoclax, and Revumenib | 選艱築糧製廠築壓膚鑰(窪鏇襯衊顧製鹽鹹鹽憲) = present in 8 (19%) patients 範襯獵構積鏇衊顧鬱鏇 (醖齋鏇襯製獵淵構顧顧 ) 更多 | 积极 | 2025-08-10 |
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
生物医药百科问答
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