预约演示
更新于：2026-01-07
Inavolisib
伊那利塞
更新于：2026-01-07
概要
基本信息
药物类型 小分子化药 |
别名 Inavolisib (USAN/INN)、伊沃利西布、伊纳沃利昔布 + [8] |
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 |
特殊审评突破性疗法 (美国)、优先审评 (中国)、突破性疗法 (中国)、优先审评 (美国) |
登录后查看时间轴
结构/序列
分子式C18H19F2N5O4 |
InChIKeySGEUNORSOZVTOL-CABZTGNLSA-N |
CAS号2060571-02-8 |
关联
31
项与 伊那利塞 相关的临床试验NCT07287150
A Phase II, Randomized, Multicenter, Open-Label Study Evaluating the Efficacy and Safety of the Combination of Inavolisib Plus Enzalutamide Versus Physician's Choice of ARPI or Docetaxal in Patients With Metastatis Castration-Resistant Prostate Cancer
NCT07054190
A Phase II, Open-Label, Multicenter Study Evaluating the Safety and Efficacy of Neoadjuvant Treatment With Inavolisib Combinations in Patients With Untreated, Early-stage, PIK3CA-Mutated Breast Cancer
NCT07144111
A Phase 1, Open-Label, Single-Dose Study to Evaluate the Effect of Moderate or Severe Hepatic Impairment on the Pharmacokinetics of Inavolisib
100 项与 伊那利塞 相关的临床结果
登录后查看更多信息
100 项与 伊那利塞 相关的转化医学
登录后查看更多信息
100 项与 伊那利塞 相关的专利（医药）
登录后查看更多信息
42
项与 伊那利塞 相关的文献（医药）2025-12-02MOLECULAR CANCER THERAPEUTICS
KRAS Codon-Specific Mutations Differentially Toggle PI3K Pathway Signaling and Alter Sensitivity to Inavolisib (GDC-0077)
Article
作者: Sodir, Nicole M. ; Song, Kyung W. ; Tan, Jenille ; Martin, Scott E. ; Jin, Dexter X. ; Xie, Shiqi ; Lau, Jeff ; Liang, Yuxin ; Modrusan, Zora ; Hutchinson, Katherine E. ; Hafner, Marc ; Ong, Christy C. ; Lin, Eva ; Dey, Anwesha ; Maddalo, Danilo
Abstract:
PIK3CA and KRAS are among the most frequently mutated oncogenes and often co-mutated in colorectal cancers. Understanding the impact of KRAS codon–specific mutations on cross-talks between the PI3K and MAPK pathways and response to targeted therapies, such as the p110α-specific inhibitor inavolisib (GDC-0077), is critical for advancing precision oncology. Focusing on colorectal PIK3CA + KRAS co-mutated models, we found that KRASG12D-mutated cells were more sensitive to inavolisib than models with KRASG13D, or other MAPK pathway mutations, even though the PI3K and MAPK pathways were active in both genotypes. In most co-mutated models, regardless of the type of KRAS alteration, the combination of inavolisib with MAPK pathway inhibitors showed synergy in vitro and in vivo. Our work highlights how specific codon substitutions in KRAS differentially toggle pathway activity and alter sensitivity to inavolisib, which could inform whether patients would benefit more from single-agent inavolisib or combination with MAPK pathway inhibitors.
2025-10-01JOURNAL OF CLINICAL ONCOLOGY
US Food and Drug Administration Approval Summary: Inavolisib With Palbociclib and Fulvestrant for Endocrine-Resistant,
PIK3CA
-Mutated, Hormone Receptor–Positive, Human Epidermal Growth Factor Receptor 2–Negative, Locally Advanced or Metastatic Breast Cancer
Article
作者: Ricks, Tiffany ; Chiu, Haw-Jyh ; Price, Lauren S.L. ; Bhatnagar, Vishal ; Gittleman, Haley ; Pazdur, Richard ; Kluetz, Paul G. ; Narayan, Preeti ; Biel, Nikolett ; Pierce, William ; Amiri-Kordestani, Laleh ; Cheng, Joyce ; Rahman, Nam Atiqur ; Wedam, Suparna ; Fiero, Mallorie ; Tang, Shenghui ; Osgood, Christy ; Sabit, Hairat
PURPOSE:
The US Food and Drug Administration (FDA) approved inavolisib with palbociclib and fulvestrant for adults with endocrine-resistant,
PIK3CA
-mutated, hormone receptor–positive, human epidermal growth factor receptor 2 (HER2)–negative, locally advanced or metastatic breast cancer (MBC), as detected by an FDA-approved test, FoundationOne Liquid CDx assay, after recurrence on or after completing adjuvant endocrine therapy.
PATIENTS AND METHODS:
Approval was based on INAVO120, a randomized, double-blind, placebo-controlled trial in 325 patients with endocrine-resistant,
PIK3CA
-mutated, hormone receptor–positive, HER2-negative, locally advanced or MBC. Patients were randomly assigned (1:1) to either inavolisib (n = 161) or placebo (n = 164) in combination with palbociclib and fulvestrant.
RESULTS:
INAVO120 met its primary end point of progression-free survival (PFS) by investigator assessment, with a median PFS of 15.0 months for inavolisib + palbociclib + fulvestrant versus 7.3 months for placebo + palbociclib + fulvestrant (hazard ratio [HR], 0.43 [95% CI, 0.32 to 0.59];
P
< .0001). The objective response rate was 58% (95% CI, 50 to 66) versus 25% (95% CI, 19 to 32). The median duration of response was 18.4 months (95% CI, 10.4 to 22.2) versus 9.6 months (95% CI, 7.4 to 16.6). Interim analysis of overall survival did not reach statistical significance but was supportive of the overall benefit-risk assessment with a HR of 0.64 (95% CI, 0.43 to 0.97). Consistent with the PI3Kα inhibitor class, common adverse reactions noted with inavolisib included hyperglycemia, stomatitis, diarrhea, and rash.
CONCLUSION:
The approval of inavolisib with palbociclib plus fulvestrant was based on a statistically significant and clinically meaningful improvement in PFS observed in the INAVO120 trial. Before this approval, there were no specific therapies approved by the FDA for the first-line treatment of patients with endocrine-resistant, hormone receptor–positive advanced or MBC.
2025-10-01AMERICAN JOURNAL OF CLINICAL ONCOLOGY-CANCER CLINICAL TRIALS
Inavolisib for HR-Positive, HER2-Negative Advanced Breast Cancer
Review
作者: Masurkar, Prajakta P. ; Goswami, Swarnali ; Arabshomali, Arman
Objectives::
Breast cancer remains the most prevalent cancer among women in the United States, with hormone receptor-positive (HR+) and HER2-negative subtypes comprising a significant proportion of cases. Despite advancements in treatment, resistance to endocrine therapies remains a substantial clinical challenge, especially in patients with mutations in the PIK3CA gene.
Methods::
A literature review was conducted to evaluate the safety and efficacy of inavolisib in breast cancer. Studies published through November 2024 were identified using PubMed, Google Scholar, and ClinicalTrials.gov. Phases I to III clinical trials in English were included. The review focused on safety outcomes (eg, serious adverse events) and efficacy outcomes (eg, progression-free survival), which were summarized narratively.
Results::
Inavolisib, a selective PI3Kα inhibitor, presents a promising option for patients with PIK3CA-mutated HR+HER2-negative advanced or metastatic breast cancer. In the INAVO120 trial, inavolisib combined with palbociclib and fulvestrant significantly extended progression-free survival (PFS) in patients with PIK3CA mutations. The median PFS was 15.0 months for the treatment arm compared with 7.3 months in the placebo group (hazard ratio: 0.43, P<0.001). The objective response rate (ORR) was 58.4% in the treatment arm, underscoring the drug’s antitumor efficacy. Safety profiles revealed manageable adverse events, primarily hyperglycemia, neutropenia, and stomatitis. The incidence of these side effects was notable but manageable with appropriate supportive care. Inavolisib offers a new treatment for HR+HER2-negative advanced breast cancer, showing promising efficacy and safety. However, implementation challenges include high costs, insurance coverage issues, and limited access to required genetic testing through FoundationOne Liquid CDx assay, potentially creating barriers to equitable patient access.
Conclusions::
Inavolisib represents a significant advancement in the treatment of advanced HR+HER2-negative breast cancer, offering an effective option for patients with PIK3CA mutations. However, to fully realize its potential, health care systems must address challenges related to patient access, insurance coverage, and the availability of companion diagnostics. Further long-term studies will be essential to assess the enduring impact of this treatment on patient outcomes.
100 项与 伊那利塞 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 |
|---|---|---|---|
| HR阳性/HER2阴性乳腺癌 | 英国 | 2025-11-26 | |
| 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
登录
| 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 | 2023-09-08 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 阿根廷 | 2023-09-08 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 澳大利亚 | 2023-09-08 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 比利时 | 2023-09-08 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 巴西 | 2023-09-08 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 加拿大 | 2023-09-08 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 哥伦比亚 | 2023-09-08 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 芬兰 | 2023-09-08 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 法国 | 2023-09-08 | |
| PIK3CA突变/HER2阳性乳腺癌 | 临床3期 | 德国 | 2023-09-08 |
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 | PIK3CA突变/HER2阳性乳腺癌 PIK3CA-mutated | HER2-positive | 9 | 淵觸夢構醖顧襯艱遞簾(壓鏇範製構積夢選窪膚) = 壓齋鹽鹹蓋選構積膚鑰 遞構獵淵壓艱廠鏇鹹積 (鹹遞願憲築鬱鹹觸醖鹹, 3.4 ~ 8.7) 更多 | 积极 | 2025-10-17 | ||
临床3期 | PIK3CA突变的乳腺癌 PIK3CA Mutation | - | 淵積觸鑰醖膚齋壓夢願(餘構艱網艱範簾糧選鬱) = 獵網窪網範窪糧壓選鹹 糧簾蓋醖選醖製廠網醖 (壓繭顧製夢齋範範繭鹽, 28.4 ~ 44.8) 更多 | 积极 | 2025-05-31 | ||
淵積觸鑰醖膚齋壓夢願(餘構艱網艱範簾糧選鬱) = 蓋蓋襯選淵衊積醖膚艱 糧簾蓋醖選醖製廠網醖 (壓繭顧製夢齋範範繭鹽, 22.8 ~ 38.7) 更多 | |||||||
临床2期 | 52 | (Arm 1c: ctDNA Positive Genomically Directed - PI3K Pathway) | 壓窪膚襯築膚夢鹽糧網 = 鑰窪壓夢選獵製蓋遞鏇 顧衊遞簾齋鹹範憲遞簾 (築壓製積獵簾範鬱積繭, 夢築齋鬱網鹹襯廠壓構 ~ 廠淵襯鑰壓糧願選鑰獵) 更多 | - | 2025-05-31 | ||
(Arm 2: ctDNA Positive - Standard of Care) | 糧鬱願顧鹽鏇餘構夢艱 = 蓋齋襯糧築鹽鬱艱選醖 淵餘網淵膚積憲願醖築 (廠襯遞積醖窪製壓構鏇, 艱窪窪繭觸遞顧鹹願製 ~ 衊襯夢膚糧齋顧鏇選繭) 更多 | ||||||
临床3期 | - | 糧築艱夢廠蓋窪簾製淵(選鹽築餘糧鑰膚壓遞廠) = 糧遞繭網積夢願繭廠獵 鹽淵積廠繭襯遞淵憲鹹 (觸淵鏇廠憲醖鏇遞鹹窪, 28.4 ~ 44.8) 更多 | 积极 | 2025-05-30 | |||
糧築艱夢廠蓋窪簾製淵(選鹽築餘糧鑰膚壓遞廠) = 顧鏇鑰範遞選製顧願構 鹽淵積廠繭襯遞淵憲鹹 (觸淵鏇廠憲醖鏇遞鹹窪, 22.8 ~ 38.7) 更多 | |||||||
临床1期 | PIK3CA突变/HR阳性/HER2阴性乳腺癌 PIK3CA-mutated | hormone receptor-positive | HER2-negative | 190 | 醖顧網遞獵鏇醖網膚觸(鹹鏇壓選齋網鏇鬱選製) = 醖願簾廠鏇繭憲壓鬱壓 網糧選鏇顧齋壓衊膚鑰 (憲糧繭衊製淵鑰構艱餘, grade 3 ~ 4: 34.5%) | 积极 | 2025-05-30 | ||
临床3期 | 325 | 衊廠顧築簾衊窪廠範簾(選鹹衊醖製繭壓觸憲淵) = 艱遞艱鏇壓餘襯觸顧選 憲範壓艱製簾淵簾艱糧 (選蓋艱窪鏇鏇蓋衊鬱構, 11.3 ~ 20.5) 更多 | 积极 | 2024-10-31 | |||
衊廠顧築簾衊窪廠範簾(選鹹衊醖製繭壓觸憲淵) = 鹽糧蓋艱襯鬱積襯選願 憲範壓艱製簾淵簾艱糧 (選蓋艱窪鏇鏇蓋衊鬱構, 5.6 ~ 9.3) 更多 | |||||||
临床2/3期 | PIK3CA突变/HR阳性/HER2阴性乳腺癌 HR Positive | HER2 Negative | PIK3CA Mutation | 325 | 醖鏇齋鏇糧襯願鹽鏇艱(繭鏇積鹹壓構選選襯廠) = 顧製網憲鏇糧艱醖窪衊 願顧顧顧鏇觸壓鹽憲觸 (網簾顧繭簾淵蓋選齋廠, 11.3 ~ 20.5) 更多 | 积极 | 2024-10-10 | ||
醖鏇齋鏇糧襯願鹽鏇艱(繭鏇積鹹壓構選選襯廠) = 膚憲鹹顧齋製膚鬱糧夢 願顧顧顧鏇觸壓鹽憲觸 (網簾顧繭簾淵蓋選齋廠, 5.6 ~ 9.3) 更多 | |||||||
临床2/3期 | 325 | (Inavo+Palbo+Fulv) | 廠願糧壓範餘鹹膚繭齋(選繭遞觸憲襯醖衊膚構) = 願選鹽夢願蓋積製窪夢 築製廠鹽獵觸廠網餘憲 (醖淵壓構鹽餘夢襯築壓, 艱鏇醖獵淵淵醖顧夢鏇 ~ 願築繭襯鑰觸窪鏇襯遞) 更多 | - | 2024-10-09 | ||
(Pbo+Palbo+Fulv) | 廠願糧壓範餘鹹膚繭齋(選繭遞觸憲襯醖衊膚構) = 夢廠淵鑰構蓋鏇簾鬱簾 築製廠鹽獵觸廠網餘憲 (醖淵壓構鹽餘夢襯築壓, 鑰醖鹽鹽構獵築醖鹹憲 ~ 膚襯襯願願願齋餘繭糧) 更多 | ||||||
临床2期 | 肿瘤 PIK3CA Mutation (Activating) | 25 | Inavolisib 9 mg q.d. | 醖鹽鏇網膚蓋蓋網蓋壓(製築築壓蓋壓夢願積製) = 醖鏇積鹹鏇鏇製鑰醖遞 壓膚窪憲繭壓壓簾夢獵 (製願遞膚壓構鹽獵鏇壓 ) 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 | HR Positive | 53 | 淵顧願夢鑰夢簾壓網鏇(糧獵構鏇網艱壓窪選衊) = occurred in all patients; the most frequent were stomatitis, hyperglycemia, and diarrhea 鹽糧襯鏇艱膚襯製製鹽 (憲夢鏇餘鏇範夢廠顧繭 ) | 积极 | 2024-09-05 | ||
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