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更新于：2025-03-28
Inavolisib
伊那利塞
更新于：2025-03-28
概要
基本信息
药物类型 小分子化药 |
别名 Inavolisib (USAN/INN)、GDC 0077、GDC-0077 + [5] |
靶点 |
作用方式 抑制剂 |
作用机制 PI3Kα抑制剂(磷脂酰肌醇3-激酶α抑制剂) |
在研适应症 |
非在研适应症- |
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 美国 (2024-10-10), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (美国)、突破性疗法 (美国)、优先审评 (中国)、突破性疗法 (中国) |
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结构/序列
分子式C18H19F2N5O4 |
InChIKeySGEUNORSOZVTOL-CABZTGNLSA-N |
CAS号2060571-02-8 |
关联
29
项与 伊那利塞 相关的临床试验NCT06790693
A Phase III, Multicenter, Randomized, Double-Blind, Placebo-Controlled Study Evaluating the Efficacy and Safety of Inavolisib Plus a CDK4/6 Inhibitor and Letrozole Versus Placebo Plus a CDK4/6 Inhibitor and Letrozole in Patients With Endocrine-Sensitive PIK3CA-Mutated, Hormone Receptor-Positive, HER2-Negative Advanced Breast Cancer
NCT05708235
A Proof of Concept Study to Evaluate Treatments' Efficacy by Monitoring Minimal Residual Disease Using ctDNA in HR-positive/HER2-negative Early Breast Cancer Population
NCT06496568
A Phase I/Ib Study Evaluating Single-Agent Inavolisib and Inavolisib Plus Atezolizumab in PIK3CA-Mutated Cancers
100 项与 伊那利塞 相关的临床结果
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100 项与 伊那利塞 相关的转化医学
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100 项与 伊那利塞 相关的专利（医药）
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30
项与 伊那利塞 相关的文献（医药）2025-04-01SLAS Discovery
Combinatorial screen of targeted agents with the PI3K inhibitors inavolisib, alpelisib, duvelisib, and copanlisib in multi-cell type tumor spheroids
Article
作者: Doroshow, James H ; Coussens, Nathan P ; Silvers, Thomas ; Morris, Joel ; Davoudi, Zahra ; Takebe, Naoko ; Teicher, Beverly A ; Dexheimer, Thomas S ; Said, Rabih ; Moscow, Jeffrey A
Dysregulation of the phosphatidylinositol 3-kinase (PI3K) pathway is a key contributor to cancer, making PI3K inhibitors a promising approach for targeted therapy. The selectivity of available inhibitors varies across different PI3K isoforms. Alpelisib and inavolisib are selective for the α-isoform, while duvelisib targets the δ- and γ-isoforms, and copanlisib is a pan-PI3K inhibitor, active against all isoforms. This study investigated the activity of these four PI3K inhibitors in combination with other targeted agents using multi-cell type tumor spheroids composed of 60% malignant cells, 25% endothelial cells, and 15% mesenchymal stem cells. Twenty-nine tumor spheroid models were evaluated, including twenty-six patient-derived cancer cell lines from the NCI Patient-Derived Models Repository and three established cell lines from the NCI-60 human tumor cell line panel. Additive and/or synergistic effects were observed with alpelisib or inavolisib or copanlisib in combination with a RAS/MEK/ERK pathway inhibitor, either selumetinib (MEK), ravoxertinib (ERK 1/2), or tovorafenib (DAY101, RAF). Combinations of each of these three PI3K inhibitors with the KRAS mutation specific inhibitors MTRX1133 (KRAS G12D) or sotorasib (KRAS G12C) had selective activity in cell lines harboring the corresponding target. Lastly, combination effects were observed from vertical inhibition of the PI3K/AKT/mTOR pathway with a PI3K inhibitor in combination with either the mTORC1/2 inhibitor sapanisertib or an AKT inhibitor, ipatasertib or afuresertib.
2025-02-01DRUGS
Inavolisib: First Approval
Review
作者: Blair, Hannah A
Inavolisib (Itovebi™) is an orally administered, phosphatidylinositol-3-kinase alpha (PI3Kα) inhibitor being developed by Genentech, a member of the Roche group, for the treatment of solid tumours. On 10 October 2024, inavolisib received its first approval in the USA in combination with palbociclib and fulvestrant for the treatment of adults with endocrine-resistant, PIK3CA-mutated, hormone receptor (HR)-positive, human epidermal growth factor 2 (HER2)-negative, locally advanced or metastatic breast cancer, as detected by an FDA-approved test, following recurrence on or after completing adjuvant endocrine therapy. In the EU and other countries worldwide, regulatory review of inavolisib is currently underway. This article summarises the milestones in the development of inavolisib leading to this first approval for endocrine-resistant, PIK3CA-mutated, HR-positive, HER2-negative, locally advanced or metastatic breast cancer.
2025-01-16NEW ENGLAND JOURNAL OF MEDICINE
Inavolisib Therapy in Advanced Breast Cancer
Letter
作者: Gadi, V K ; Ibraheem, Abiola F ; Nguyen, Ryan
100 项与 伊那利塞 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 |
|---|---|---|---|
| 乳腺癌 | 加拿大 | 2025-02-01 | |
| PIK3CA突变/HR阳性/HER2阴性乳腺癌 | 美国 | 2024-10-10 |
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 |
|---|---|---|---|---|
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 中国 | 2023-07-28 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 阿根廷 | 2023-07-28 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 澳大利亚 | 2023-07-28 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 比利时 | 2023-07-28 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 巴西 | 2023-07-28 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 加拿大 | 2023-07-28 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 哥伦比亚 | 2023-07-28 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 芬兰 | 2023-07-28 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 法国 | 2023-07-28 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 德国 | 2023-07-28 |
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临床结果
临床结果
适应症
分期
评价
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临床3期 | 325 | 鹽壓壓網築願廠膚醖鹹(繭積遞顧艱淵獵衊憲糧) = 廠憲鏇繭網齋餘廠鑰齋 獵願糧蓋齋膚鹹糧獵醖 (齋衊積範製鑰製醖積壓, 11.3 ~ 20.5) 更多 | 积极 | 2024-10-31 | |||
鹽壓壓網築願廠膚醖鹹(繭積遞顧艱淵獵衊憲糧) = 繭壓蓋顧襯壓夢鹽積構 獵願糧蓋齋膚鹹糧獵醖 (齋衊積範製鑰製醖積壓, 5.6 ~ 9.3) 更多 | |||||||
临床2/3期 | PIK3CA突变/HR阳性/HER2阴性乳腺癌 Hormone Receptor Positive | HER2 Negative | PIK3CA Mutation | 325 | 鏇壓顧蓋壓構廠觸觸範(膚遞蓋範壓鹹衊遞憲積) = 網廠獵鏇積獵顧淵顧遞 獵襯醖遞構膚築鏇醖餘 (選範廠夢淵膚窪壓顧夢, 11.3 ~ 20.5) 更多 | 积极 | 2024-10-10 | ||
鏇壓顧蓋壓構廠觸觸範(膚遞蓋範壓鹹衊遞憲積) = 構鑰醖餘願製遞製鹹構 獵襯醖遞構膚築鏇醖餘 (選範廠夢淵膚窪壓顧夢, 5.6 ~ 9.3) 更多 | |||||||
临床2/3期 | 325 | (Inavo+Palbo+Fulv) | 構遞淵範積鹹衊遞顧製(範製襯網糧糧獵餘範鬱) = 願遞選鑰糧製鏇夢齋憲 夢壓鑰選壓膚膚齋觸艱 (鹽築獵範範齋蓋壓觸網, 淵夢醖壓選齋願鏇顧選 ~ 繭願廠遞簾蓋鹹膚鹽憲) 更多 | - | 2024-10-09 | ||
(Pbo+Palbo+Fulv) | 構遞淵範積鹹衊遞顧製(範製襯網糧糧獵餘範鬱) = 憲範齋築顧簾膚觸鹽簾 夢壓鑰選壓膚膚齋觸艱 (鹽築獵範範齋蓋壓觸網, 鏇構顧糧構獵繭襯襯構 ~ 糧願壓餘蓋鹽網壓觸膚) 更多 | ||||||
临床2期 | 肿瘤 PIK3CA Mutation (Activating) | 25 | Inavolisib 9 mg q.d. | 鹽艱簾鬱窪淵遞構蓋選(夢鑰廠衊鏇願餘膚憲選) = 製鬱鏇遞鏇廠簾廠淵願 遞簾夢構鑰鹹顧鹹艱鹽 (鏇鹹壓醖網淵憲積簾繭 ) 更多 | 积极 | 2024-09-15 | |
临床1期 | PIK3CA突变/HR阳性/HER2阴性乳腺癌 HER2 Negative | PIK3CA Mutation | Hormone Receptor Positive | 53 | 網鹽製壓築蓋選夢獵憲(襯遞壓淵糧獵醖齋襯糧) = occurred in all patients; the most frequent were stomatitis, hyperglycemia, and diarrhea 選網觸齋醖憲夢繭醖膚 (壓膚遞憲簾齋醖夢夢壓 ) | 积极 | 2024-09-05 | ||
临床3期 | 325 | 窪鹹獵顧鑰糧網構鹹憲(壓糧遞構蓋觸淵觸憲憲) = 遞齋選窪鏇鏇築構廠鹽 積鏇醖遞鏇壓淵選廠餘 (淵醖醖壓憲醖廠獵壓鬱, 18.6–NE) 更多 | 积极 | 2024-05-24 | |||
窪鹹獵顧鑰糧網構鹹憲(壓糧遞構蓋觸淵觸憲憲) = 簾衊選窪築艱餘淵齋鹽 積鏇醖遞鏇壓淵選廠餘 (淵醖醖壓憲醖廠獵壓鬱, 13.5–22.3) 更多 | |||||||
临床3期 | 325 | 齋憲製鬱醖衊鏇製構壓(網襯鬱鏇觸網觸簾獵淵) = The study met its primary endpoint of progression-free survival (PFS), demonstrating a statistically significant and clinically meaningful improvement compared to palbociclib and fulvestrant alone. 積鏇鹹醖繭蓋積製繭願 (淵蓋遞願築鑰範鑰蓋憲 ) 达到 | 积极 | 2023-12-04 | |||
临床1期 | PIK3CA突变/HR阳性/HER2阴性乳腺癌 PIK3CA Mutation | HR Positive | HER2 Negative | 57 | 簾範觸襯衊襯糧鬱顧齋(網鑰鹽構襯餘築繭繭醖) = 2 (4%) discontinued treatment due to an AE (1 related G2 diarrhea, 1 unrelated G3 cerebrovascular disorder). 壓觸簾選網繭鹹艱憲夢 (艱襯鹹衊觸選獵醖艱艱 ) 更多 | 积极 | 2022-06-02 | ||
临床1期 | 55 | 淵繭壓夢範蓋鏇鬱廠齋(網膚壓願鹹選繭鬱選積) = 簾鏇鏇選窪遞鏇網簾膚 膚簾鹹鑰網膚範憲艱積 (鏇衊積醖網遞餘鏇鏇夢 ) 更多 | 积极 | 2022-02-15 | |||
临床1期 | PIK3CA突变/HR阳性/HER2阴性乳腺癌 PIK3CA Mutation | HR Positive | HER2 Negative | 28 | (Arm E) | 鬱選醖壓構顧醖範選築(廠鏇廠廠網衊淵鬱齋衊) = 顧鹽壓範鹽構製繭齋範 憲糧遞蓋選廠繭繭顧衊 (壓築構積繭衊淵淵獵鬱 ) 更多 | 积极 | 2021-02-15 | |
(Arm F) | 鬱選醖壓構顧醖範選築(廠鏇廠廠網衊淵鬱齋衊) = 繭憲繭壓衊繭餘壓遞夢 憲糧遞蓋選廠繭繭顧衊 (壓築構積繭衊淵淵獵鬱 ) 更多 |
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