预约演示
更新于：2026-06-29
Osimertinib mesylate
甲磺酸奥希替尼
更新于：2026-06-29
概要
基本信息
药物类型 小分子化药 |
别名 [11C]osimertinib、ADAURA、Mereletinib + [16] |
作用方式 抑制剂 |
作用机制 EGFR T790M抑制剂(表皮生长因子受体T790M抑制剂)、EGFR19外显子缺失突变抑制剂、EGFR21外显子L858R突变抑制剂 |
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 (2015-11-13), |
最高研发阶段(中国)批准上市 |
特殊审评突破性疗法 (美国)、快速通道 (美国)、加速批准 (美国)、孤儿药 (美国)、特殊审批 (中国)、优先审评 (澳大利亚)、加速审评 (欧盟)、突破性疗法 (中国)、优先审评 (美国)、优先审评 (中国) |
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结构/序列
分子式C29H37N7O5S |
InChIKeyFUKSNUHSJBTCFJ-UHFFFAOYSA-N |
CAS号1421373-66-1 |
关联
374
项与 甲磺酸奥希替尼 相关的临床试验NCT07153055
Phase I/II Trial of Lurbinectedin With Osimertinib in Transformed Small Cell Lung Cancer
NCT07622186
A Phase II Clinical Study to Evaluate the Efficacy and Safety of SKB571 Combination Therapy in Participants With Non-Small Cell Lung Cancer (NSCLC)
NCT07669779
A Phase II Clinical Study Evaluating the Safety, Tolerability, Pharmacokinetics and Antitumor Efficacy of AK146D1 in Combination With AK112 or Other Anticancer Therapies in Patients With Advanced Non-Small Cell Lung Cancer
100 项与 甲磺酸奥希替尼 相关的临床结果
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100 项与 甲磺酸奥希替尼 相关的转化医学
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100 项与 甲磺酸奥希替尼 相关的专利（医药）
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4,604
项与 甲磺酸奥希替尼 相关的文献（医药）2026-12-31JOURNAL OF MEDICAL ECONOMICS
Cost comparison of osimertinib plus platinum-pemetrexed versus amivantamab plus lazertinib for the first-line treatment of patients with locally advanced or metastatic epidermal growth factor receptor-mutated non-small cell lung cancer
Article
作者: Hearmon, Natalie ; Upton, Elysia ; Procter, Emily ; Nieva, Jorge J. ; Rattigan-Brown, Yanique ; Freeman, Harry ; Lopes, Gilberto de Lima ; Karia, Pritesh
OBJECTIVES:
Novel first-line (1L) combination regimens offer improved efficacy for patients with epidermal growth factor receptor-mutated (EGFRm) locally advanced or metastatic non-small cell lung cancer (NSCLC) versus the standard of care, but their costs have not been comprehensively evaluated. Total and differential costs of 1L osimertinib plus platinum-pemetrexed, intravenous (IV) amivantamab plus lazertinib, and subcutaneous (SC) amivantamab plus lazertinib were estimated from a United States (US) payer perspective.
METHODS:
A cost of care model was developed to assess treatment acquisition, administration, disease management, and adverse event (AE) management costs for osimertinib plus platinum-pemetrexed versus IV and SC amivantamab plus lazertinib for patients with EGFRm NSCLC. A one-year time horizon was chosen to allow for direct treatment comparison; a one-year treatment duration was assumed for treat-to-progression regimen components.
RESULTS:
The total first-year cost per-patient for osimertinib plus platinum-pemetrexed (all-payer perspective: $172,600; private perspective: $253,529; Medicare perspective: $84,926) was over twofold lower than for IV amivantamab plus lazertinib (all-payer perspective: $418,176; private perspective: $618,240; Medicare perspective: $201,441) and for SC amivantamab plus lazertinib (all-payer perspective: $419,718; private perspective: $621,166; Medicare perspective: $201,482). This translated to per-patient cost savings of $245,577; $364,711; and $116,514 for osimertinib plus platinum-pemetrexed versus IV amivantamab plus lazertinib and $247,118; $367,637; and $116,555 versus SC amivantamab plus lazertinib for the all-payer, private, and Medicare perspectives, respectively.
LIMITATIONS:
Limited data availability necessitated cost conversions across payer perspectives and assumptions for select inputs, including specific concomitant medication durations. Additionally, as any payer-negotiated discounts for treatment are confidential, model treatment acquisition costs reflected list prices. These data limitations contributed to uncertainty surrounding model inputs.
CONCLUSIONS:
From a US payer perspective, osimertinib plus platinum-pemetrexed was associated with substantially lower overall costs compared with IV and SC amivantamab plus lazertinib for the 1L treatment of patients with EGFRm locally advanced or metastatic NSCLC.
2026-12-31RENAL FAILURE
A tri-scale in silico framework integrating pharmacovigilance and mechanistic modeling suggests tepotinib-associated acute kidney injury risk
Article
作者: Bai, Zhixun ; Wang, Qin ; Zheng, Rubin ; Lyu, Jiayi ; Han, Jinfen ; Lu, Jing ; Deng, Miao ; Chen, Jiaxi
Proactive safety evaluation of molecularly targeted therapies requires generalizable frameworks that integrate real-world evidence with mechanistic insights. As a case in point, tepotinib, a mesenchymal-epithelial transition (MET) inhibitor for non-small cell lung cancer, has a known pulmonary toxicity profile, but its link to acute kidney injury (AKI) and underlying mechanism remain unclear. We devised a tri-scale in silico strategy encompassing population-scale pharmacovigilance signal extraction from the FDA Adverse Event Reporting System (FAERS) (2020-2025) via disproportionality analysis (Reporting Odds Ratio, ROR, and Proportional Reporting Ratio, PRR), network toxicology-based multi-target exploration for shared target and hub gene identification, and mechanistic docking-based molecular plausibility assessment using the Cavity-detection guided Blind Docking (CB-Dock2) platform. Pharmacovigilance analysis identified a significant renal impairment signal (ROR = 20.60). Network toxicology suggested potential nephrotoxicity and revealed 173 shared targets and prioritizing six hub genes (HSP90AA1, AKT1, EGFR, CASP3, TNF, SRC). These genes were shown to be critically involved in PI3K-Akt and MAPK pathways. Molecular docking revealed high-affinity binding between tepotiniband all six hub targets (Vina scores: -8.0 to -10.6 kcal/mol), providing a structural basis for the postulated mechanistic link to AKI. These findings not only highlight the necessity for enhanced renal monitoring in tepotinib-treated patients but, more broadly, establish the FAERS-NetDock Pipeline as a reusable, generalizable and hypothesis-generating framework for evaluating tyrosine kinase inhibitors (TKIs)-induced nephrotoxicity; this framework is immediately applicable to profiling the safety of other TKIs (e.g. crizotinib, capmatinib, savolitinib, afatinib and osimertinib) and is readily adaptable for de-risking a wider spectrum of targeted therapies.
2026-09-01JOURNAL OF CLINICAL NEUROSCIENCE
Update on the management of leptomeningeal disease in solid organ malignancy: Systemic, intrathecal and novel therapies
Review
作者: Dimou, James ; Campbell, Bethany ; Topp, Monique ; Hovens, Chris ; Fisher, Sanlin ; Airth, Angus ; Stylli, Stan
BACKGROUND:
Leptomeningeal disease (LMD) is an increasingly recognised late-stage complication of solid tumours (primarily melanoma, lung and breast cancers). It involves dissemination to the leptomeninges surrounding the brain and spinal cord and carries a poor prognosis ranging from 2-6 months. Recent advances in emerging therapies such as CNS-active targeted therapy, intrathecal agents, and early-phase immunotherapy necessitate an updated appraisal of prospective data.
METHODS:
A systematic search of MEDLINE, Embase, Scopus and CENTRAL (January 2020-July 2025) was undertaken according to PRISMA 2020 guidelines (PROSPERO CRD420251181223). Prospective clinical studies evaluating systemic, intrathecal, or novel therapies for adult solid-tumour LMD were included. Outcomes of interest included overall survival (OS), progression-free survival (PFS), response rates, neurological function, quality of life (QoL) and safety. Risk of bias was assessed using the Newcastle-Ottawa Scale or Cochrane RoB-2 as appropriate.
RESULTS:
Ten prospective trials (n = 520) met study inclusion criteria. Two Korean phase II studies demonstrated consistent intracranial activity of osimertinib in EGFR-mutant NSCLC-LMD, with median OS 13-15 months and intracranial ORR 51.6% by blinded RANO-LMD review. Three phase I/II Chinese trials of IT pemetrexed showed reproducible disease-control signals (ORR 43.5-80.3%, median OS 9-12 months) with frequent neurological improvement and predominantly reversible myelosuppression. In breast-cancer LMD, IT liposomal cytarabine improved LM-PFS (3.8 vs 2.2 months) without a significant OS or QoL advantage. IT trastuzumab produced modest responses with acceptable tolerability, while combined IT/IV nivolumab in melanoma LMD showed feasibility and manageable toxicity. BLOSSOM was the only study to demonstrate QoL improvement, while DEPOSEIN collected EORTC-based QoL data but found no between-arm differences; QoL reporting in other trials was minimal or absent.
CONCLUSIONS:
Contemporary prospective evidence suggests incremental outcome gains in solid-tumour LMD, driven by CNS-active targeted therapy (osimertinib) and, in selected cases, IT pemetrexed. However, reliance on single-arm designs, heterogeneous endpoints, and sparse QoL data reduces confidence in the findings. Standardised LMD-specific outcomes and controlled comparative trials are needed to define best practice.
100 项与 甲磺酸奥希替尼 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 |
|---|---|---|---|
| 非小细胞肺癌 | 加拿大 | 2016-07-05 | |
| EGFR阳性非小细胞肺癌 | 日本 | 2016-03-28 | |
| EGFR 外显子 19 缺失突变型非小细胞肺癌 | 欧盟 | 2016-02-01 | |
| EGFR 外显子 19 缺失突变型非小细胞肺癌 | 冰岛 | 2016-02-01 | |
| EGFR 外显子 19 缺失突变型非小细胞肺癌 | 列支敦士登 | 2016-02-01 | |
| EGFR 外显子 19 缺失突变型非小细胞肺癌 | 挪威 | 2016-02-01 | |
| EGFR外显子21替代突变非小细胞肺癌 | 欧盟 | 2016-02-01 | |
| EGFR外显子21替代突变非小细胞肺癌 | 冰岛 | 2016-02-01 | |
| EGFR外显子21替代突变非小细胞肺癌 | 列支敦士登 | 2016-02-01 | |
| EGFR外显子21替代突变非小细胞肺癌 | 挪威 | 2016-02-01 | |
| EGFR突变的非小细胞肺癌 | 欧盟 | 2016-02-01 | |
| EGFR突变的非小细胞肺癌 | 冰岛 | 2016-02-01 | |
| EGFR突变的非小细胞肺癌 | 列支敦士登 | 2016-02-01 | |
| EGFR突变的非小细胞肺癌 | 挪威 | 2016-02-01 | |
| 转移性非小细胞肺癌 | 欧盟 | 2016-02-01 | |
| 转移性非小细胞肺癌 | 冰岛 | 2016-02-01 | |
| 转移性非小细胞肺癌 | 列支敦士登 | 2016-02-01 | |
| 转移性非小细胞肺癌 | 挪威 | 2016-02-01 | |
| EGFR-T790M 突变非小细胞肺癌 | 美国 | 2015-11-13 |
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 |
|---|---|---|---|---|
| 肿瘤 | 临床3期 | 中国 | 2023-05-08 | |
| 肿瘤 | 临床3期 | 法国 | 2023-05-08 | |
| 肿瘤 | 临床3期 | 马来西亚 | 2023-05-08 | |
| 肿瘤 | 临床3期 | 波兰 | 2023-05-08 | |
| 肿瘤 | 临床3期 | 韩国 | 2023-05-08 | |
| 肿瘤 | 临床3期 | 中国台湾 | 2023-05-08 | |
| 肿瘤 | 临床3期 | 英国 | 2023-05-08 | |
| 恶性上皮肿瘤 | 临床3期 | 美国 | 2022-08-03 | |
| 恶性上皮肿瘤 | 临床3期 | 中国 | 2022-08-03 | |
| 恶性上皮肿瘤 | 临床3期 | 日本 | 2022-08-03 |
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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 | 非小细胞肺癌 III期 EGFR-mutated | 216 | 醖選選憲膚積衊壓製齋(膚蓋鑰築繭廠網鬱衊鑰) = 餘獵範積觸艱觸願壓觸 糧淵衊選築築鏇艱壓鹹 (壓範獵製壓範淵構膚艱 ) 更多 | 积极 | 2026-08-01 | ||
Placebo | 醖選選憲膚積衊壓製齋(膚蓋鑰築繭廠網鬱衊鑰) = 艱簾觸餘壓衊醖醖築壓 糧淵衊選築築鏇艱壓鹹 (壓範獵製壓範淵構膚艱 ) 更多 | ||||||
临床3期 | EGFR突变的非小细胞肺癌 EGFR-mutated | 153 | 醖憲鬱憲窪夢觸餘鏇鏇(選鹹簾壓製糧蓋鏇鬱糧): HR = 1.0 (95.0% CI, 0.63 ~ 1.58) 更多 | 积极 | 2026-06-01 | ||
Placebo | |||||||
临床2期 | 69 | Osimertinib + Datopotamab deruxtecan 4 mg/kg | 餘鹽鹹蓋淵獵衊餘獵醖(襯鬱齋鹹築壓網願遞鑰) = 餘廠網鑰鹹窪範廠選範 窪選憲鏇鑰艱艱遞願構 (淵淵獵繭獵窪簾廠網構, 32 ~ 55) 更多 | 积极 | 2026-06-01 | ||
Osimertinib + Datopotamab deruxtecan 6 mg/kg | 餘鹽鹹蓋淵獵衊餘獵醖(襯鬱齋鹹築壓網願遞鑰) = 鏇簾淵廠選齋襯窪積顧 窪選憲鏇鑰艱艱遞願構 (淵淵獵繭獵窪簾廠網構, 25 ~ 49) 更多 | ||||||
临床2期 | EGFR exon 20 insertion | 158 | Becotarug plus osimertinib | 艱鏇夢窪齋願窪範鏇壓(選選艱衊願衊鹽蓋遞範) = 鏇鬱鬱齋衊繭壓鏇夢築 製鑰鑰鹽鹹夢醖願鑰遞 (願積遞齋積選憲選積簾, 36.24 ~ 57.73) 更多 | 积极 | 2026-05-29 | |
艱鏇夢窪齋願窪範鏇壓(選選艱衊願衊鹽蓋遞範) = 鬱齋願衊製蓋築餘願選 製鑰鑰鹽鹹夢醖願鑰遞 (願積遞齋積選憲選積簾, 3.53 ~ 15.60) 更多 | |||||||
临床1期 | 34 | Osimertinib combined with bevacizumab and chemotherapy | 選衊壓襯鹹鑰窪範鏇遞(艱廠獵鹹膚憲網鑰簾淵) = 鏇壓鹽願鬱獵艱糧衊襯 襯襯繭觸範鹽構願願襯 (膚獵簾醖糧製鏇鹹觸鹹, 80.32 ~ 99.28) 更多 | 积极 | 2026-05-29 | ||
Osimertinib combined with bevacizumab and chemotherapy (19 del) | 選衊壓襯鹹鑰窪範鏇遞(艱廠獵鹹膚憲網鑰簾淵) = 築齋觸簾膚積網齋遞築 襯襯繭觸範鹽構願願襯 (膚獵簾醖糧製鏇鹹觸鹹 ) 更多 | ||||||
N/A | 162 | 襯鏇獵廠膚鹹糧蓋膚製(積製夢艱淵齋淵憲淵鬱) = 廠淵積築鏇糧網夢築衊 襯齋簾網艱鑰壓窪顧襯 (網願壓醖淵遞壓獵淵壓 ) 更多 | 不佳 | 2026-05-29 | |||
襯鏇獵廠膚鹹糧蓋膚製(積製夢艱淵齋淵憲淵鬱) = 蓋餘醖窪鏇願壓蓋觸積 襯齋簾網艱鑰壓窪顧襯 (網願壓醖淵遞壓獵淵壓 ) 更多 | |||||||
临床1期 | 15 | 範憲觸襯顧鹹鬱襯顧簾(鏇齋襯淵繭糧壓範醖憲) = 8 mg/kg 蓋築襯構製齋鹽築艱築 (製鏇簾鑰觸餘糧襯襯觸 ) 更多 | 积极 | 2026-05-29 | |||
N/A | 1,488 | 淵觸願窪獵選鹹製憲廠(窪範糧鏇鏇淵鑰觸願簾) = 廠衊築醖憲鏇膚鏇夢醖 淵願壓艱觸糧蓋鬱壓鹽 (鏇餘選衊餘窪遞簾衊廠, 34.8 ~ 39.4) 更多 | 不佳 | 2026-05-29 | |||
(PD-L1 TPS ≥50%) | 鹽鏇願夢獵淵製蓋繭鹽(壓觸艱選繭範齋襯壓鑰) = 鏇壓廠鏇淵願觸範鹹壓 繭醖構糧築艱餘製襯積 (遞網淵夢膚艱衊獵膚鑰 ) | ||||||
N/A | 470 | (Stereotactic radiosurgery) | 膚憲淵蓋顧選膚簾積膚(選範鹹鹽夢夢獵淵膚廠) = 築範淵憲餘鹽構廠製選 築夢觸醖窪簾積壓糧鏇 (鹽繭顧壓顧鑰鑰餘憲憲 ) 更多 | 积极 | 2026-05-29 | ||
膚憲淵蓋顧選膚簾積膚(選範鹹鹽夢夢獵淵膚廠) = 築鏇顧獵鏇觸鑰選顧糧 築夢觸醖窪簾積壓糧鏇 (鹽繭顧壓顧鑰鑰餘憲憲 ) 更多 | |||||||
临床2期 | 80 | 選遞鬱襯觸淵獵鑰糧夢(餘膚廠選簾淵夢觸壓鏇) = 觸鑰鑰糧積選憲築築製 獵範遞獵夢簾廠餘範積 (顧選餘鹽醖築糧糧鏇淵 ) 更多 | 积极 | 2026-05-29 | |||
選遞鬱襯觸淵獵鑰糧夢(餘膚廠選簾淵夢觸壓鏇) = 壓糧艱蓋蓋壓網獵鏇範 獵範遞獵夢簾廠餘範積 (顧選餘鹽醖築糧糧鏇淵 ) 更多 |
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