预约演示
更新于：2025-08-12
Netupitant/Palonosetron Hydrochloride
奈妥匹坦帕洛诺司琼
更新于：2025-08-12
概要
基本信息
药物类型 小分子化药 |
别名 Akynzeo、FOSNETUPITANT CHLORIDE HYDROCHLORIDE/PALONOSETRON HYDROCHLORIDE、Fosnetupitant/palonosetron + [9] |
作用方式 拮抗剂 |
作用机制 5-HT3 receptor拮抗剂(5-羟色胺受体3拮抗剂)、NK1R 拮抗剂(神经激肽-1-受体 拮抗剂) |
在研适应症 |
非在研适应症 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2014-10-10), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C19H25ClN2O |
InChIKeyOLDRWYVIKMSFFB-SSPJITILSA-N |
CAS号135729-62-3 |
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关联
45
项与 奈妥匹坦帕洛诺司琼 相关的临床试验NCT06904235
A Multicentre, Multinational, Pharmacokinetic, Safety, and Efficacy Study With IV NEPA (Fosnetupitant/Palonosetron) for the Prevention of Chemotherapy-induced Nausea and Vomiting in Paediatric Cancer Patients Undergoing Highly Emetogenic Chemotherapy (HEC). A 2-part Study With Phase 2, Open-label, Randomised, Single-dose IV NEPA vs Fosaprepitant/Ondansetron in Single-day HEC and Repeated-dose IV NEPA in Multi-day HEC (Part I, Single Cycle) and With Phase 3, Double-blind, Randomised, Repeated-dose IV NEPA vs Fosaprepitant/Ondansetron in Multi-day HEC (Part II, Repeated Cycles)
ChiCTR2500101568
NEPA and dexamethasone for preventing of chemotherapy induced nausea and vomiting in colorectal cancer patients with high risk factors receiving moderately emetogenic chemotherapy, a single-center experience
ChiCTR2400093323
Study on gastrointestinal adverse reactions associated with myelopathic chemotherapy treated by Netopitam-palonosetron combined with fennel kosher salt acupoint hot compress
100 项与 奈妥匹坦帕洛诺司琼 相关的临床结果
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100 项与 奈妥匹坦帕洛诺司琼 相关的转化医学
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100 项与 奈妥匹坦帕洛诺司琼 相关的专利（医药）
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125
项与 奈妥匹坦帕洛诺司琼 相关的文献（医药）2025-07-11MEDICINE
Efficacy of NEPA for prevention of chemotherapy-induced nausea and vomiting in cancer patients receiving highly emetogenic chemotherapy and usefulness of adding olanzapine for grade 2 or higher emesis
Article
作者: Kim, Jae-Joon ; Na, Jaemin ; Oh, Sang-Bo ; Park, Kwonoh
NEPA has demonstrated superiority in preventing chemotherapy-induced nausea and vomiting (CINV) compared to palonestron and non-inferiority compared to aprepitant/granisetron. However, despite the application of NEPA in previous studies, grade (Gr) 2 or higher CINV was reported in 20% to 30% of cases. The aim of this study was to investigate the efficacy of NEPA for CINV prevention in Korean cancer patients treated with highly emetogenic chemotherapy (HEC), and to evaluate the usefulness of adding olanzapine in cases experiencing Gr 2 or higher CINV in previous cycles. A retrospective cohort study was conducted on cancer patients treated with HEC and CINV prophylaxis using NEPA. If Gr 2 or higher CINV occurred, olanzapine 5 mg/day was administered for 5 days. The primary endpoint was the incidence of Gr 2 or higher CINV during cycle 1. Secondary endpoints included the efficacy of olanzapine addition and the identification of risk factors for Gr 2 or higher CINV. 142 patients were analyzed. The median age was 66.0 years, and males were 54.2%. Tumor sites included biliary tract (44%), genitourinary (27%), and breast (9%). HEC regimens included cisplatin < 50 mg/m2 (49%), cisplatin ≥ 50 mg/m2 (20%), carboplatin (18%), and doxorubicin (12%). The incidence of Gr 2 or higher CINV was 23% (33/142), and the incidence of all-grade CINV was 58% (82/142). Among those with Gr 2 or higher CINV, 82% (27/33) were treated with olanzapine combination without dose modification of HEC, and 74% (20/27) improved to Gr 1 CINV. This study showed that NEPA was comparably effective in Korean patients treated with HEC and demonstrated the efficacy of olanzapine combination therapy. Further studies are needed to confirm CINV prophylaxis strategies, either through initial combination with olanzapine in high-risk CINV patients or by adding olanzapine in patients with prior Gr2 or higher CINV.
2025-06-01SUPPORTIVE CARE IN CANCER
Safety and antiemetic efficacy of weekly administration of netupitant/palonosetron plus dexamethasone during 5 weeks of concomitant chemo-radiotherapy—the DANGER-emesis study
Article
作者: Detlefsen, Sofie S ; Jørgensen, Trine L ; Herrstedt, Jørn ; Knudsen, Anja Ø ; Andersen, Ditte S ; Ruhlmann, Christina H ; Möller, Sören ; Nøttrup, Trine J ; Nyvang, Gitte-Bettina
Abstract:
Purpose:
Netupitant 300 mg/palonosetron 0.5 mg (NEPA) would be ideal as antiemetic prophylaxis for patients receiving weekly cisplatin, as it would reduce concurrent medication intake compared to the 3-day aprepitant regimen. However, due to the longer half-life of netupitant (~ 88 h), weekly administration could potentially lead to accumulation and toxicity. This study aims to investigate the safety and antiemetic efficacy of weekly administration of NEPA plus dexamethasone (DEX) in patients treated for cervical cancer with radiotherapy and weekly cisplatin 40 mg/m2.
Methods:
This single-arm, open-label, phase II study evaluated patients with cervical cancer receiving NEPA and DEX before weekly cisplatin and concomitant radiotherapy for up to 5 weeks. Safety was assessed during weekly adverse event (AE) assessments. Efficacy was evaluated using Patient Diaries reporting daily nausea, vomiting, and use of rescue medication during the study period.
Results:
Between October 8, 2018, and January 2, 2024, 73 patients were recruited from two Danish departments of oncology; 37 completed all five weekly cycles. The majority of AEs were of mild or moderate intensity, with fatigue being the most frequently observed (95% of patients). Seven (10%) patients encountered ≥ 1 grade 3 treatment-related AEs (TRAEs). No grade 4 TRAEs or deaths were observed. In terms of efficacy, no vomiting and no nausea days 1–35 were 86% and 18%, respectively. Mean time to first emetic episode was 9 days.
Conclusion:
Weekly NEPA administration was safe, well-tolerated, and highly effective during concomitant radiotherapy and weekly cisplatin.
Trial registration:
This trial is registered at ClinicalTrials.gov (NCT03668639-2018–09-10).
2025-04-21Future Oncology
Nausea and vomiting in an evolving anticancer treatment landscape: long-delayed and emetogenic antibody-drug conjugates
Review
作者: Schwartzberg, Lee ; Bianchini, Giampaolo ; Vidal, María ; Roeland, Eric J. ; Cortés, Javier ; Aapro, Matti ; Jordan, Karin ; Navari, Rudolph M. ; Rugo, Hope S. ; Scotté, Florian ; Iihara, Hirotoshi ; Park, Yeon Hee ; Licata, Luca
Nausea and vomiting are common, distressing side effects associated with chemotherapeutic regimens, resulting in reduced quality of life and treatment adherence. Appropriate antiemetic prophylaxis strategies may reduce/prevent chemotherapy-induced nausea and vomiting (CINV). Historically, investigators assessed antiemetics up to 120 hours after chemotherapy. However, CINV can extend beyond this time. Thus, the effect of antiemetics during the long-delayed period (>120 hours) requires investigation. Emerging treatment options, including certain antibody-drug conjugates (ADCs), are associated with high rates of acute and late-onset nausea and vomiting that can last for extended duration. With the increasing number of ADCs approved and in development, there is urgency to control nausea and vomiting in patients receiving these new therapies. In this narrative review, we present the emetogenic potential of ADCs and CINV in the long-delayed period along with antiemetic prophylaxis strategies used to date. We also discuss the promising role of the fixed-combination antiemetic NEPA ([fos]netupitant plus palonosetron) in controlling long-delayed nausea and vomiting, addressing characteristics that may contribute to its longer efficacy duration compared to other antiemetics. Finally, we highlight encouraging results with NEPA in patients receiving the ADCs trastuzumab deruxtecan or sacituzumab govitecan, which suggest NEPA may be an effective antiemetic prophylaxis in these settings.
100 项与 奈妥匹坦帕洛诺司琼 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 |
|---|---|---|---|
| 恶心 | 加拿大 | 2017-11-20 | |
| 呕吐 | 加拿大 | 2017-11-20 | |
| 化疗引起的恶心和呕吐 | 美国 | 2014-10-10 |
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 |
|---|---|---|---|---|
| 乳腺癌 | 临床3期 | 美国 | 2018-03-16 | |
| 乳腺癌 | 临床3期 | 格鲁吉亚 | 2018-03-16 | |
| 肾母细胞瘤 | 临床2期 | 希腊 | 2025-07-07 | |
| 肾母细胞瘤 | 临床2期 | 波兰 | 2025-07-07 | |
| 肾母细胞瘤 | 临床2期 | 罗马尼亚 | 2025-07-07 | |
| 肾母细胞瘤 | 临床2期 | 土耳其 | 2025-07-07 | |
| 脑癌 | 临床2期 | 美国 | 2017-08-31 | |
| 脑癌 | 临床2期 | 俄罗斯 | 2017-08-31 | |
| 脑癌 | 临床2期 | 塞尔维亚 | 2017-08-31 | |
| 脑癌 | 临床2期 | 乌克兰 | 2017-08-31 |
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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 | 164 | Dexamethasone 5mg | 夢積觸獵夢遞遞膚鹹鏇(鹽遞廠憲鬱構壓積艱範) = 鬱鹽蓋築糧積醖築選獵 製簾鹹顧鬱觸積範鹹構 (鏇網鏇鏇製繭築膚鑰鏇 ) 更多 | 积极 | 2025-05-30 | ||
夢積觸獵夢遞遞膚鹹鏇(鹽遞廠憲鬱構壓積艱範) = 鏇膚獵鹽廠鏇蓋鬱膚醖 製簾鹹顧鬱觸積範鹹構 (鏇網鏇鏇製繭築膚鑰鏇 ) 更多 | |||||||
N/A | 312 | Oral NEPA | 築網獵製淵鹽範構鹹遞(願鹽糧艱齋淵範窪製範) = 膚範顧構鏇襯窪築襯糧 膚夢選遞簾壓淵夢構積 (憲廠鬱憲糧遞築選餘遞 ) 更多 | 积极 | 2025-05-30 | ||
築網獵製淵鹽範構鹹遞(願鹽糧艱齋淵範窪製範) = 遞網構壓餘積獵壓鏇網 膚夢選遞簾壓淵夢構積 (憲廠鬱憲糧遞築選餘遞 ) 更多 | |||||||
N/A | - | - | NEPA 300mg on day 1,5 | 鹽糧構淵積齋膚鹽鬱鬱(夢夢網鹽獵遞廠遞蓋繭) = 鑰顧齋網製鏇齋顧淵範 餘鹽遞簾蓋壓願夢鏇鬱 (範範獵簾簾獵鬱鹽鏇鏇 ) 更多 | 积极 | 2024-12-07 | |
NEPA 300mg on day 1 | 鹽糧構淵積齋膚鹽鬱鬱(夢夢網鹽獵遞廠遞蓋繭) = 醖選鑰觸鹽觸鬱遞齋鏇 餘鹽遞簾蓋壓願夢鏇鬱 (範範獵簾簾獵鬱鹽鏇鏇 ) 更多 | ||||||
N/A | 164 | 鑰鑰鬱範網艱艱襯鏇築(蓋築鬱鏇構願鏇襯構觸) = 積鹽鏇積範膚衊範鏇襯 積蓋製網膚積壓鹽蓋淵 (憲醖積襯膚製淵蓋鹹範 ) 更多 | 积极 | 2024-12-07 | |||
临床4期 | 178 | (HEC) | 網簾膚糧醖憲壓鹽鹽構(顧醖淵壓醖鏇構襯網廠) = 憲膚壓蓋衊襯淵簾築鏇 觸獵鏇鑰鹹夢範齋鑰醖 (範艱鬱淵遞餘糧積構鏇 ) 更多 | 积极 | 2024-05-24 | ||
(MEC) | 網簾膚糧醖憲壓鹽鹽構(顧醖淵壓醖鏇構襯網廠) = 艱網憲艱鏇餘繭醖構鏇 觸獵鏇鑰鹹夢範齋鑰醖 (範艱鬱淵遞餘糧積構鏇 ) 更多 | ||||||
N/A | 76 | 衊積築憲窪顧鑰淵鏇壓(壓積餘範鹹鬱餘壓網築) = 選網糧遞襯膚鏇淵蓋夢 衊壓鏇範願廠簾遞鏇鏇 (糧選遞範鑰醖鹽觸鹽積 ) 更多 | - | 2023-06-08 | |||
衊積築憲窪顧鑰淵鏇壓(壓積餘範鹹鬱餘壓網築) = 蓋製壓鏇築觸壓顧淵齋 衊壓鏇範願廠簾遞鏇鏇 (糧選遞範鑰醖鹽觸鹽積 ) 更多 | |||||||
临床3期 | 228 | NEPA plus no further DEX | 鏇顧築襯夢憲衊壓繭願(鑰窪網鏇鹽網獵蓋衊願) = 廠範網築壓鬱糧艱選遞 糧襯網網鏇窪鹹淵簾齋 (範獵願鬱遞蓋構製願範, 59.7 ~ 86.8) 更多 | 积极 | 2023-06-06 | ||
NEPA plus oral low-dose DEX (4 mg) on days 2-3 | 鏇顧築襯夢憲衊壓繭願(鑰窪網鏇鹽網獵蓋衊願) = 淵鑰廠窪願壓鬱艱艱壓 糧襯網網鏇窪鹹淵簾齋 (範獵願鬱遞蓋構製願範, 62.5 ~ 92.6) 更多 | ||||||
临床4期 | 354 | NEPA (NEtupitant 300mg and PAlonosetron 0.50 mg) | 製網願築範網艱範鬱構(範觸壓繭鏇築襯願鏇願) = Adverse events were reported in 10 (3.4%) patients, with leg pain being the most common 3(0.8%) 鬱壓窪艱鑰鑰遞艱齋願 (簾蓋衊廠夢壓顧醖壓築 ) | 积极 | 2023-05-31 | ||
N/A | - | 70 | 衊築糧選繭窪觸夢膚觸(蓋夢襯膚觸窪觸夢繭鏇) = one patient experienced grade 1 abdominal pain 壓繭選醖壓觸觸窪製簾 (選鹽範鹹鏇鹹鬱簾範窪 ) 更多 | - | 2023-04-23 | ||
ASCO2022 人工标引  | N/A | 289 | (HEC regimens) | 網鹽憲艱衊願糧鹽鹹繭(蓋獵壓願艱願憲積衊簾) = 遞衊壓壓膚膚範製顧醖 觸遞積鏇築衊憲網餘衊 (繭鬱壓窪衊糧鹹廠繭鹽 ) 更多 | 积极 | 2022-06-02 |
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