Palonosetron 中文名称: 帕洛诺司琼

别名: RS 25259; RS 25259 197; RS 25233-197; RS25233-197; RS-25233-197; RS25233-198; RS-25233-198; RS 25233-198; RS-25259-197; Palonosetron; US brand name: Aloxi; Akynzeo 帕洛诺司琼; 帕洛诺司琼盐酸盐

目录号: V3895 纯度: ≥98%

COA 产品数据产品说明书 SDS

Palonosetron（原RS-25259、RS-25259 197；商品名：Aloxi andAkynzeo）是一种5-HT3拮抗剂，被批准用于预防和治疗化疗引起的恶心和呕吐。

Palonosetron CAS号: 135729-61-2
产品类别: 5-HT Receptor

产品仅用于科学研究，不针对患者销售

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InvivoChem产品被CNS等顶刊论文引用

Nature 2024 Dec 18.

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nat Neurosci 2024, 27:1468-1474.

Nat Metab 2024, 6: 1108-1127.

Cell Stem Cell 2024, 31:106-126.e13.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

Immunity 2024,57:2651-2668.e12.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

纯度/质量控制文件

批次：

纯度: ≥98%

COA

MSDS

产品说明书

产品描述
生物活性&实验参考方法
化学信息
溶解度数据
计算器
临床试验信息
生物数据图片
相关产品

产品描述

帕洛诺司琼（原 RS-25259、RS-25259 197；商品名：Aloxi 和 Akynzeo）是一种 5-HT3 拮抗剂，被批准用于预防和治疗化疗引起的恶心和呕吐。截至2018年4月，fosnetupitant和帕洛诺司琼的组合已获得FDA批准，用于预防与高致吐性癌症化疗的初始和重复疗程相关的急性和迟发性恶心和呕吐。帕洛诺司琼是一种高效、选择性、第二代 5-HT3 受体拮抗剂，其 5-HT3 受体结合亲和力比其他 5-HT3 受体拮抗剂高约 100 倍（pKi 10.5，而格拉司琼为 8.91，托烷司琼为 8.81），昂丹司琼为 8.39，多拉司琼为 7.6）。

生物活性&实验参考方法

靶点	5-HT₃ Receptor ( Ki = 0.17 nM )
体外研究 (In Vitro)	体外活性：帕洛诺司琼是一种高效、选择性的第二代 5-HT3 受体拮抗剂，其 5-HT3 受体结合亲和力比其他 5-HT3 受体拮抗剂高约 100 倍（pKi 10.5，而格拉司琼为 8.91），托烷司琼为 8.81，昂丹司琼为 8.39，多拉司琼为 7.6）。帕洛诺司琼还具有较长的血浆消除半衰期，约为 40 小时，明显长于同类药物（昂丹司琼，4 小时；托烷司琼，7.3 小时；多拉司琼，7.5 小时；雷尼司琼，8.9 小时）。激酶测定：帕洛诺司琼是一种高效、选择性的第二代 5-HT3 受体拮抗剂，其 5-HT3 受体结合亲和力比其他 5-HT3 受体拮抗剂高约 100 倍（pKi 10.5，而格拉司琼为 8.91，托烷司琼为 8.81，昂丹司琼为 8.39，多拉司琼为 7.6)。细胞测定：帕洛诺司琼是一种 5-HT3 拮抗剂，用于预防和治疗化疗引起的恶心和呕吐 (CINV)。 IC50 值：目标：5-HT3 受体帕洛诺司琼是控制第一个化疗疗程后 24 小时以上出现的迟发性 CINV 恶心和呕吐最有效的 5-HT3 拮抗剂。
体内研究 (In Vivo)	帕洛诺司琼在半衰期和结合亲和力方面都超过了第一代5-HT3受体拮抗剂。当健康人和癌症患者静脉注射帕洛诺司琼时，身体在血浆浓度最初下降后逐渐消除药物。在 0.3 至 90 μg/kg 之间，健康个体和癌症患者的平均最大血浆浓度和浓度-时间曲线下面积通常与剂量成比例。帕洛诺司琼的分布容积为 8.3 ± 2.5 L/kg，62% 与血浆蛋白结合。通过代谢过程和肾脏排泄，它被排出体外。 40 小时大致是平均终末消除半衰期[1]。
酶活实验	帕洛诺司琼是第二代、高选择性、强效的 5-HT3 受体拮抗剂，与该受体的结合亲和力比其他 5-HT3 受体拮抗剂高约 100 倍（pKi 10.5，而格拉司琼为 8.91），托烷司琼为 8.81，昂丹司琼为 8.39，多拉司琼为 7.6）。
细胞实验	帕洛诺司琼是一种 5-HT3 拮抗剂，用于治疗和预防化疗 (CINV) 引起的恶心和呕吐。 IC50 值：在 5-HT3 拮抗剂中，5-HT3 受体帕洛诺司琼在治疗迟发性 CINV 恶心和呕吐方面最成功，这种恶心和呕吐在化疗方案初始剂量后 24 小时内出现。
动物实验	Autoradiographical studies[3] Coronal sections of rat and mouse brains were cut at 20 ,um thickness. Sections were dried and pre-incubated in Tris-HCl buffer (50 mM Tris, 120 mM NaCl, pH 7.4, 22°C) for 30 min. The sections were then covered with the same buffer contain- -4 ing 1.0 nM [3H]-RS 42358-197 or [3H]-RS 25259-197 for 60 min at 22°C. Non-specific binding was defined in the presence of 1.0 tLM (S)-zacopride. The incubations were ter- -n minated by rinsing the slides for two washes of 5 min in ice cold buffer. The sections were dried and apposed, together with 3H polymer standards (Amersham, Inc.) to tritiumsensitive X-ray film for 24 weeks. The autoradiograms were then analysed by digital image analysis with the MCID imaging system (Imaging Research, Inc.). Brain areas were verified on cresyl violet stained sections after autoradiography, using the areas described in the rat brain atlas of Paxinos & Watson (1985).
药代性质 (ADME/PK)	Absorption, Distribution and Excretion Low oral bioavailability. After a single intravenous dose of 10 mcg/kg [14C]-palonosetron, approximately 80% of the dose was recovered within 144 hours in the urine 8.3 ± 2.5 L/kg 160 +/- 35 mL/h/kg Metabolism / Metabolites Hepatic (50%), primarily CYP2D6-mediated, although CYP3A4 and CYP1A2 are also involved. Biological Half-Life Approximately 40 hours
毒性/毒理 (Toxicokinetics/TK)	Effects During Pregnancy and Lactation ◉ Summary of Use during Lactation No information is available on the use of palonosetron during breastfeeding. Until more data become available, palonosetron should be used with caution during breastfeeding. An alternate drug may be preferred. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. Protein Binding 62%
参考文献	[1]. Cancer Manag Res. 2009; 1: 167–176. [2]. ACS Chem Neurosci. 2016 Dec 21;7(12):1641-1646. [3]. Br J Pharmacol. 1995 Feb;114(4):851-9.
其他信息	Pharmacodynamics Palonosetron is an antinauseant and antiemetic agent indicated for the prevention of nausea and vomiting associated with moderately-emetogenic cancer chemotherapy and for the prevention of postoperative nausea and vomiting. Palonosetron is a highly specific and selective serotonin 5-HT₃ receptor antagonist that is pharmacologically related to other 5-HT₃ receptor antagonists, but differs structurally. Palonosetron has a high affinity for 5-HT₃ receptors, but has little to no affinity for other receptors. The serontonin 5-HT₃ receptors are located on the nerve terminals of the vagus in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema. It is suggested that chemotherapeutic agents release serotonin from the enterochromaffin cells of the small intestine by causing degenerative changes in the GI tract. The serotonin then stimulates the vagal and splanchnic nerve receptors that project to the medullary vomiting center, as well as the 5-HT3 receptors in the area postrema, thus initiating the vomiting reflex, causing nausea and vomiting.

*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性

化学信息 & 存储运输条件

分子式	C19H24N2O
分子量	296.41
精确质量	296.188
元素分析	C, 76.99; H, 8.16; N, 9.45; O, 5.40
CAS号	135729-61-2
相关CAS号	Palonosetron hydrochloride; 135729-62-3; (R,R)-Palonosetron Hydrochloride; 135729-75-8
PubChem CID	6337614
外观&性状	Solid powder
密度	1.2±0.1 g/cm3
沸点	470.4±45.0 °C at 760 mmHg
闪点	209.5±21.1 °C
蒸汽压	0.0±1.2 mmHg at 25°C
折射率	1.646
LogP	2.61
tPSA	23.55
氢键供体(HBD)数目	0
氢键受体(HBA)数目	2
可旋转键数目(RBC)	1
重原子数目	22
分子复杂度/Complexity	456
定义原子立体中心数目	2
SMILES	O=C1N(C[C@@]([H])(CCC2)C3=C2C=CC=C13)[C@@H]4CN5CCC4CC5
InChi Key	CPZBLNMUGSZIPR-NVXWUHKLSA-N
InChi Code	InChI=1S/C19H24N2O/c22-19-16-6-2-4-14-3-1-5-15(18(14)16)11-21(19)17-12-20-9-7-13(17)8-10-20/h2,4,6,13,15,17H,1,3,5,7-12H2/t15-,17-/m1/s1
化学名	(3aS)-2-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-3a,4,5,6-tetrahydro-3H-benzo[de]isoquinolin-1-one
别名	RS 25259; RS 25259 197; RS 25233-197; RS25233-197; RS-25233-197; RS25233-198; RS-25233-198; RS 25233-198; RS-25259-197; Palonosetron; US brand name: Aloxi; Akynzeo
HS Tariff Code	2934.99.9001
存储方式	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
运输条件	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

溶解度数据

溶解度 (体外实验)

DMSO: ~59 mg/mL (~199.0 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

溶解度 (体内实验)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

注射用配方
(IP/IV/IM/SC等)

注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

口服配方

口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、以上所有助溶剂都可在 Invivochem.cn网站购买。

制备储备液		1 mg	5 mg	10 mg
	1 mM	3.3737 mL	16.8685 mL	33.7371 mL
	5 mM	0.6747 mL	3.3737 mL	6.7474 mL
	10 mM	0.3374 mL	1.6869 mL	3.3737 mL

1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;

2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;

3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;

4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。

计算器

质量

浓度

体积

分子量*

计算重置

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度，具体如下：

计算制备已知体积和浓度的溶液所需的化合物的质量
计算将已知质量的化合物溶解到所需浓度所需的溶液体积
计算特定体积中已知质量的化合物产生的溶液的浓度

参见示例

使用摩尔浓度计算器计算摩尔浓度的示例如下所示：
假如化合物的分子量为350.26 g/mol，在5mL DMSO中制备10mM储备液所需的化合物的质量是多少？

在分子量（MW）框中输入350.26
在“浓度”框中输入10，然后选择正确的单位（mM）
在“体积”框中输入5，然后选择正确的单位（mL）
单击“计算”按钮
答案17.513 mg出现在“质量”框中。以类似的方式，您可以计算体积和浓度。

浓度 (起始)

体积 (起始)

浓度 (终)

体积 (终)

计算重置

稀释计算器可计算如何稀释已知浓度的储备液。例如，可以输入C1、C2和V2来计算V1，具体如下：

制备25毫升25μM溶液需要多少体积的10 mM储备溶液？
使用方程式C1V1=C2V2，其中C1=10mM，C2=25μM，V2=25 ml，V1未知：

在C1框中输入10，然后选择正确的单位（mM）
在C2框中输入25，然后选择正确的单位（μM）
在V2框中输入25，然后选择正确的单位（mL）
单击“计算”按钮
答案62.5μL（0.1 ml）出现在V1框中

分子式

分子量

g/mol

计算重置

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成，具体如下：

注：化学分子式大小写敏感：C12H18N3O4 c12h18n3o4
计算化合物摩尔质量（分子量）的说明：

要计算化合物的分子量 (摩尔质量)，请输入化学/分子式，然后单击“计算”按钮。

分子质量、分子量、摩尔质量和摩尔量的定义：

分子质量（或分子量）是一种物质的一个分子的质量，用统一的原子质量单位（u）表示。（1u等于碳-12中一个原子质量的1/12）
摩尔质量（摩尔重量）是一摩尔物质的质量，以g/mol表示。

配液体积

质量

配液浓度

计算重置

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

输入试剂的质量、所需的配液浓度以及正确的单位
单击“计算”按钮
答案显示在体积框中

动物体内实验配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg

动物平均体重 g

每只动物给药体积 μL

动物数量

第二步：请输入动物体内配方组成（配方适用于不溶/难溶于水的化合物），不同的产品和批次配方组成不同，如对配方有疑问，可先联系我们提供正确的体内实验配方。此外，请注意这只是一个配方计算器，而不是特定产品的确切配方。

% DMSO

% Tween 80

% ddH₂O

计算重置

计算结果:

工作液浓度： mg/mL；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意： (1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。

临床试验信息

Cisplatin Disposition and Kidney Injury
CTID: NCT03817970
Phase: Phase 3 Status: Active, not recruiting
Date: 2024-11-21

HR20013 for Nausea and Vomiting Associated With Moderate Emetic Risk Anticancer Agents
CTID: NCT06554184
Phase: Phase 3 Status: Recruiting
Date: 2024-09-19

A Comparison Between Palonosetron Versus Granisetron as PONV Prophylaxis in Scoliotic Patients Undergoing Spine Surgery
CTID: NCT06540885
Phase: Phase 4 Status: Not yet recruiting
Date: 2024-08-20

PK/PD Study of Netupitant and Palonosetron in Pediatric Patients for Prevention of Chemotherapy-induced Nausea and Vomiting
CTID: NCT03204279
Phase: Phase 2 Status: Completed
Date: 2024-06-25

Palonosetron vs Ondansetron In PONV Prophylaxis Among Idiopathic Scoliosis Patients
CTID: NCT05956899
Phase: Phase 4 Status: Recruiting
Date: 2024-02-07

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A Phase II Trial of Neoadjuvant Laparoscopic Hyperthermic Intraperitoneal Chemotherapy (HIPEC) With Chemoradiation
CTID: NCT04308837
Phase: Phase 2 Status: Recruiting
Date: 2023-11-14

Netupitant and Palonosetron Hydrochloride in Preventing Chronic Nausea and Vomiting in Patients With Cancer
CTID: NCT03040726
Phase: Phase 2/Phase 3 Status: Completed
Date: 2023-10-17

Efficacy and Safety of Intravenous Versus Oral 5-HT3 Antagonists Combined With NK-1 Receptor Antagonists for the Prevention of CINV in Breast Cancer
CTID: NCT05841849
Phase: Phase 4 Status: Not yet recruiting
Date: 2023-05-03

Palonosetron and Blood Coagulation
CTID: NCT04507711
Phase: N/A Status: Recruiting
Date: 2023-03-15

Aprepitant Triple Therapy for the Prevention of CINV in Nondrinking and Young Women Who Received Moderately Emetogenic Chemotherapy
CTID: NCT03674294
Phase: Phase 3 Status: Completed
Date: 2023-02-08

Effect of Palonosetron, Ondansetron and Dexamethasone in the Prevention of Postoperative Nausea and Vomiting
CTID: NCT05439798
Phase: Phase 3 Status: Unknown status
Date: 2022-06-30

An Efficacy and Safety Study of Oral and Intravenous Palonosetron for the Prevention of Nausea and Vomiting
CTID: NCT01363479
Phase: Phase 3 Status: Completed
Date: 2021-09-22

Evaluate Bioequivalence of Palonosetron (0.25mg/5mL)
CTID: NCT04585412
Phase: Phase 4 Status: Completed
Date: 2021-08-04

Granisetron Transdermal Patch for Prophylaxis of Delayed CINV
CTID: NCT04912271
Phase: Phase 3 Status: Unknown status
Date: 2021-06-03

Effect of Palonosetron on Remifentanil for Preventing Emergence Cough in Female
CTID: NCT04563260
Phase: N/A Status: Completed
Date: 2021-05-11

Palonosetron vs. Ondansetron for Postoperative Nausea and Vomiting in Bariatric Surgery
CTID: NCT04533867
Phase: Status: Completed
Date: 2021-01-22

Pilot Study to Assess Palonosetron Versus Ondansetron as Rescue Medication in Subjects That Develop Postoperative Nausea and Vomiting (PONV) in the Postanesthesia Care Unit (PACU)
CTID: NCT00967499
Phase: Phase 2 Status: Completed
Date: 2021-01-11

Palonosetron Versus Ondansetron for PONV Prevention in Patients Undergoing ERCP
CTID: NCT04576390
Phase: Phase 4 Status: Unknown status
Date: 2020-10-06

MEtoclopramide, DExamethasone or Axoli to Prevent or Delay Chemotherapy-induced Nausea and Vomiting in Moderately Emetogenic Non-AC-based Chemotherapy
CTID: NCT02135510
Phase: Phase 3 Status: Completed
Date: 2020-03-31

Intravenous Palonosetron With Radiotherapy and Concomitant Temozolomide
CTID: NCT00900757
Phase: Phase 2 Status: Completed
Date: 2019-08-28

Post-Operative Nausea and Vomiting in Children Submitted to Strabismus Surgery
CTID: NCT04060771
Phase: Phase 3 Status: Unknown status
Date: 2019-08-19

Rolapitant Plus Olanzapine in Multiday Cisplatin Chemotherapy
CTID: NCT03960151
Phase: Phase 2 Status: Withdrawn
Date: 2019-05-22

Postoperative Nausea and Vomiting After Laparoscopic Cholecystectomy
CTID: NCT03933605
Phase: N/A Status: Completed
Date: 2019-05-01

PALONOSETRON X FOSAPREPITANT IN PONV
CTID: NCT03586817
Phase: Phase 4 Status: Unknown status
Date: 2019-03-12

Real-time Decision Support for Postoperative Nausea and Vomiting (PONV) Prophylaxis
CTID: NCT02625181
Phase: N/A Status: Completed
Date: 2019-03-07

Compare Between Two Doses of Palonosetron on the Prevention of Postoperative Nausea and Vomiting in Obese Patients
CTID: NCT02941913
Phase: Phase 4 Status: Completed
Date: 2018-08-07

Effectiveness and Quality of Life Analysis of Palonosetron Against Ondansetron Combined With Dexamethasone and Fosaprepitant in Prevention of Acute and Delayed Emesis Associated to Chemotherapy Moderate and Highly Emetogenic in Breast Cancer.
CTID: NCT03606369
Phase: Phase 2/Phase 3 Status: Unknown status
Date: 2018-07-30

An Efficacy and Safety Study of Intravenous Palonosetron Administered as an Infusion and as a Bolus for the Prevention of Nausea and Vomiting
CTID: NCT02557035
Phase: Phase 3 Status: Completed
Date: 2018-06-20

Comparison of Palonosetron Versus Combination of Palonosetron and Dexamethasone for Preventing Postoperative Vomiting in Patients Receiving Fentanyl by Patient-controlled Analgesia After Minor Orthopedic Surgery
CTID: NCT02744508
Phase: N/A Status: Completed
Date: 2018-06-20

Comparison of Palonosetron and Ramosetron for Preventing Patient-controlled Analgesia Related Nausea and Vomiting Following Spine Surgery; Association With ABCB1 Polymorphism
CTID: NCT02480088
Phase: Phase 4 Status: Completed
Date: 2017-10-27

Prospective Study of Palonosetron in Radiation Induced Nausea and Vomiting (RINV)
CTID: NCT02388750
Phase: Phase 2 Status: Completed
Date: 2017-10-06

Prophylactic Antiemetic Efficacy of Palonosetron Versus Ondansetron for the Prophylaxis of Postoperative Nausea and Vomiting (PONV) in Women Over 60 Years Undergoing Laparoscopic Cholecystectomy
CTID: NCT02541019
Phase: Phase 4 Status: Completed
Phase II randomized multicenter study of multiple doses of palonosetron plus aprepitant versus multiple doses of palonosetron alone in preventing chemotherapy-induced nausea and vomiting in patients with newly diagnosed acute myeloid leukaemia or high-risk myelodysplastic syndrome receiving multiple days chemotherapy
CTID: null
Phase: Phase 2 Status: Ongoing
Date: 2011-11-08

A multicenter, randomized, double-blind, parallel group study to evaluate the efficacy and safety of two different doses of palonosetron compared to ondansetron in the prevention of CINV in pediatric patients undergoing single and repeated cycles of MEC or HEC.
CTID: null
Phase: Phase 3 Status: Ongoing, Completed
Date: 2011-08-04

A phase III, multicenter, randomized, double-blind, unbalanced (3:1) active control study to assess the safety and describe the efficacy of netupitant and palonosetron for the prevention of chemotherapy-induced nausea and vomiting in repeated chemotherapy cycles
CTID: null
Phase: Phase 3 Status: Completed
Date: 2011-05-27

A Multicenter, Double-blind, Double-dummy, Randomized, Parallel Group, Stratified Study to Evaluate the Efficacy and Safety of a Single IV Dose of Palonosetron Compared to a Single IV Dose of Ondansetron to Prevent Postoperative Nausea and Vomiting in Pediatric Patients
CTID: null
Phase: Phase 3 Status: Completed
Date: 2011-05-23

Single-dose, multicenter, randomized, double-blind, double-dummy, parallel group study to assess the efficacy and safety of oral palonosetron 0.50 mg compared to I.V. palonosetron 0.25 mg administered with dexamethasone for the prevention of chemotherapy-induced nausea and vomiting in cancer patients receiving highly emetogenic cisplatin-based chemotherapy
CTID: null
Phase: Phase 3 Status: Completed
Date: 2011-03-23

A phase III multicenter, randomized, double-blind, double-dummy, active-controlled, parallel group study of the efficacy and safety of oral netupitant administered in combination with palonosetron and dexamethasone compared to oral palonosetron and dexamethasone for the prevention of nausea and vomiting in cancer patients receiving moderately emetogenic chemotherapy
CTID: null
Phase: Phase 3 Status: Completed
Date: 2011-02-24

GAND-emesis: A multinational, randomized, double-blind, placebo-controlled, parallel-group study
CTID: null
Phase: Phase 3 Status: Completed
Date: 2010-01-27

Multicenter, Phase IV, Open-Label, Uncontrolled Study to Assess the Efficacy and Safety of a Single Intravenous Dose of Palonosetron 0.25 mg (Aloxi®, Onicit®, Paloxi®) in the Prevention of Chemotherapy-Induced Nausea and Vomiting in Patients with Non-Hodgkin’s Lymphomas Undergoing Repeated Cycles of Moderately Emetogenic Chemotherapy
CTID: null
Phase: Phase 4 Status: Completed, Prematurely Ended
Date: 2009-11-24

ÉTUDE PILOTE OBSERVATIONNELLE CHEZ DES PATIENTES SOUFFRANT D’UN CANCER DU SEIN ET RECEVANT UNE CHIMIOTHÉRAPIE ÉMÉTISANTE TRAITÉES PAR UNE DOSE UNIQUE DE ALOXI® (PALONOSÉTRON) 0,25 MG ASSOCIÉE À UNE CORTICOTHÉRAPIE
CTID: null
Phase: Phase 4 Status: Ongoing
Date: 2007-01-18

Phase II study with Palonosetron alone in preventing chemotherapy-induced nausea and vomiting in untreated patients with aggressive Non Hodgkins Lymphomas who underwent moderately emetogenic chemotherapy
CTID: null
Phase: Phase 2 Status: Completed
Date: 2006-10-31

Open-Label Pilot Study to Evaluate the Efficacy of Palonosetron Associated with Aprepitant (Emend) and Dexamethasone in Preventing Nausea and Vomiting Induced by Highly Emetogenic Chemotherapy (HEC)
CTID: null
Phase: Phase 4 Status: Completed
Date: 2006-10-17

Multicenter, randomized, controlled study to compare palonosetron plus dexamethasone before chemotherapy administration versus the same regimen with dexamethasone continuing on Days 2 and 3 in preventing nausea and vomiting in patients with solid tumors treated with moderately emetogenic chemotherapy
CTID: null
Phase: Phase 3 Status: Completed
Date: 2006-08-04

multicenter phase II study to evaluate palonosetron +desametasone in the prevention of nausea and vomiting in patientes resected for colon cancer and treated with moderate emetogenus chemotherapy.
CTID: null
Phase: Phase 2 Status: Ongoing
Date: 2006-06-27

Estudio Fase IV, Nacional, Multicéntrico, competitivo, aleatorizado, doble ciego, controlado de grupos paralelos, para determinar la seguridad, tolerabilidad, y eficacia de aprepitant, más palonosetrón frente a granisetrón en la prevención de las náuseas y la emesis inducidas por quimioterapia en pacientes tratados con trasplante de progenitores hematopoyéticos.
CTID: null
Phase: Phase 4 Status: Ongoing
Date: 2006-06-26

Double-blind Study to Compare the Efficacy of Palonosetron with or without the use of Dexamethasone on Days 2 and 3, in the Prevention of Nausea and Vomiting Induced by Moderately Emetogenic Chemotherapy (MEC) Given to Female Patients with Breast Cancer
CTID: null
Phase: Phase 4 Status: Completed
Date: 2005-12-14

Single Dose, Randomized, Double-Blind, Parallel Group, Multicenter Study of Palonosetron 0.25 mg, 0.50 mg and 0.75 mg Administered by the Oral Route versus Palonosetron 0.25 mg IV for the Prevention of Moderately Emetogenic Chemotherapy-Induced Nausea and Vomiting in Patients with Cancer
CTID: null
Phase: Phase 3 Status: Completed
Date: 2005-09-23

A Randomized, Double-blind, Multicenter, Parallel Group, Balanced, Stratified Phase 3 Study to Evaluate the Efficacy and the Safety of Single IV Doses of Palonosetron 0.025 mg, 0.050 mg, and 0.075 mg versus Placebo to Prevent Postoperative Nausea and Vomiting Following Elective Gynecologic or Breast Surgery
CTID: null
Phase: Phase 3 Status: Completed
Date: 2005-07-19

A Pivotal Phase 3 Observer-Blind, Randomized Clinical Trial of the Efficacy and Safety of APF530 Compared to Aloxi® for the Prevention of Acute-Onset and Delayed-Onset Chemotherapy-Induced Nausea and Vomiting Following the Administration of either Moderately or Highly Emetogenic Chemotherapy Regimens
CTID: null
Phase: Phase 3 Status: Completed
Date:
A phase II trial of palonosetron and 1-day dexamethasone and 3-day aprepitant to prevent nausea and vomiting in patients receiving paclitaxel and carboplatin
CTID: UMIN000013082
Phase: Status: Complete: follow-up complete
Date: 2014-02-05

Phase2 study of palonosetoron and dexamethasone therapy for prevention of carboplatin-induced nausea and vomiting in patients with gynecological cancer.
CTID: UMIN000012806
Phase: Phase II Status: Complete: follow-up complete
Date: 2014-01-09

A randomized comparative phase 2 study : Palonosetron single-dose vousus repeated-dose for prevention of nausea and vomiting induced by multiple-day high or moderate emetic risk chemotherapy in patients with haematological malignancies .
CTID: UMIN000012295
Phase: Phase II Status: Recruiting
Date: 2013-11-15

A phase II trial of aprepitant, palonosetron, dexamethasone and olanzapine for the prevention of cisplatin-based chemotherapy-induced nausea and vomiting for gynecological cancer.
CTID: UMIN000011857
Phase: Phase II Status: Complete: follow-up complete
Date: 2013-09-26

Efficacy of palonosetron plus aprepitant in preventing chemoradiotherapy-induced nausea and emesis in patients receiving daily low-dose cisplatin-based concurrent chemoradiotherapy for uterine cervical cancer: a phase II study
CTID: UMIN000011616
Phase: Status: Complete: follow-up complete
Date: 2013-09-02

A clinical study of the efficacy of 5HT3 receptor antagonist (palonocetron) in malignant lymphoma patients treated with (R-)CHOP regimen
CTID: UMIN000011092
Phase: Status: Complete: follow-up complete
Date: 2013-08-01

A phase II trial of combination therapy with palonosetron / dexamethasone or palonosetron / aprepitant / dexamethasone for the prevention of chemotherapy-induced nausea and vomiting in patients with urothelial cancer.
CTID: UMIN000010460
Phase: Phase II Status: Recruiting
Date: 2013-04-10

Comparison of antiemetic effectiveness and safety of palonosetron and dexamethasone with palonosetron, dexamethasone and aprepitant in patients with lung cancer receiving combination therapy with carboplatin: A phase II randomized study
CTID: UMIN000010056
Phase: Status: Complete: follow-up complete
Date: 2013-03-10

Prospective, open-label, comparative study on the efficacy of triple (aprepitant + granisetron 3 mg + dexamethasone) versus double (palonosetron 0.75 mg + dexamethasone) combination therapy for nausea and vomiting during moderately emetogenic chemotherapy containing carboplatin: CAP Study
CTID: UMIN000010186
PhaseNot applicable Status: Complete: follow-up complete
Date: 2013-03-07

Phase III study to clarify the efficacy and safety of aprepitant or palonosetron on chemotherapy with paclitaxel and carboplatin for gynecologic cancer
CTID: UMIN000009585
Phase: Phase III Status: Pending
Date: 2013-03-01

A randomized, multicenter non-inferiority trial of 1-day versus 3-day dexamethasone in combination with palonosetron for prevention of nausea and vomiting induced by moderately emetogenic chemotherapy
CTID: UMIN000009403
Phase: Phase III Status: Complete: follow-up complete
Date: 2012-11-27

Randomized double-blind phase 3 study of granisetron vs palonosetron combined with dexamethasone plus fosaprepitant for patient with breast cancer treated with peri-operative AC/EC/FAC/FEC chemotherapy
CTID: UMIN000008897
Phase: Phase III Status: Complete: follow-up complete
Date: 2012-09-11

A single-blind randomized controlled trial comparing Aprepitant plus (Granisetron)1st 5-HT3 receptor antagonist and Palonosetron for the prevention of chemotherapy-induced nausea and vomiting associated with moderately emetogenic chemotherapies including CBDCA in the gynecology cancer patients.
CTID: UMIN000008552
Phase: Status: Complete: follow-up complete
Date: 2012-08-01

Aprepitant, Palonosetron and Dexamethasone Antiemetic Therapy Evaluation trial in germ cell tumor (APDATE)
CTID: UMIN000008110
Phase: Status: Recruiting
Date: 2012-06-05

Examination concerning dosage of dexamethasone when Fosaprepitant and Palonosetron are used together for nausea and vomiting induced chemotherapy for head and neck cancer.
CTID: UMIN000008080
PhaseNot applicable Status: Complete: follow-up complete
Date: 2012-06-01

Study of Palonosetron / Dexamethasone / Olanzapine for nausea and vomiting induced chemotherapy for breast cancer.
CTID: UMIN000008064
Phase: Phase II Status: Complete: follow-up complete
Date: 2012-06-01

Multicenter double-blind randomized comparative parallel study with concomitant therapy of 3 drugs, aprepitant + dexamethasone+palonosetron or aprepitant + dexamethasone+ granisetron, for prevention of nausea/vomiting in breast cancer patients receiving AC therapy
CTID: UMIN000007882
Phase: Phase III Status: Recruiting
Date: 2012-05-02

A phase II study of palonosetron combined with dexamethasone to prevent nausea and vomiting induced by daily low-dose cisplatin-based concurrent chemoradiotherapy in patients with uterine cervical cancer.
CTID: UMIN000007638
Phase: Status: Complete: follow-up complete
Date: 2012-04-02

Efficacy of palonosetron for prevention of chemotherapy-induced nausea and vomitting in patients with haematological malignancies
CTID: UMIN000005733
Phase: Status: Pending
Date: 2011-06-17

Preventive effect of combination therapy with aprepitant, palonosetron and dexamethasone on chemotherapy-induced nausea and vomiting (CINV) in esophageal cancer patients receiving 5-FU plus cisplatin: a prospective phase II study
CTID: UMIN000005551
Phase: Phase II Status: Complete: follow-up complete
Date: 2011-06-01

Randomized study comparing the efficacy of aprepitant with palonosetron as antiemetic drug during chemotherapy including cisplatin
CTID: UMIN000005623
Phase: Status: Complete: follow-up complete
Date: 2011-05-20

Randomized Phase II trial of Palonosetron/Dexamethasone concurrent therapy with prevention of CINV according to chemotherapy including Oxaliplatin or Irinotecan in patients with advanced colorectal cancer.
CTID: UMIN000005534
Phase: Phase II Status: Pending
Date: 2011-05-09

Efficacy and safety of a triple antiemetic combination with palonosetron, dexamethasone and aprepitant in patients receiving multiple-day cisplatin-containing chemotherapy.
CTID: UMIN000005506
Phase: Phase II Status: Complete: follow-up complete
Date: 2011-04-25

A phase II study of Palonosetron combined with Dexamethasone and Aprepitant to prevent nausea and vomiting in patients receiving highly emetogenic chemotherapy for esophageal cancer
CTID: UMIN000005017
Phase: Phase II Status: Recruiting
Date: 2011-02-03

Study of efficacy and tolerability of combination therapy with palonosetron and dexamethasone for the prevention of chemotherapy-induced nausea and vomiting in patients with cervical cancer.
CTID: UMIN000004962
Phase: Phase II Status: Complete: follow-up complete
Date: 2011-02-01

Randomized crossover trial of Granisetron/Dexamethasone/Aprepitant versus Palonosetron/Dexamethasone/Aprepitant for the prevention of nausea and vomiting in patients receiving receiving Cisplatin containing chemotherapy for head and neck cancer
CTID: UMIN000004826
Phase: Phase II Status: Complete: follow-up complete
Date: 2011-01-06

Study of efficacy and tolerability of combination therapy with palonosetron, aprepitant, and dexamethasone for the prevention of chemotherapy-induced nausea and vomiting in patients with germ cell tumors undergoing multiple-day cisplatin-based chemotherapy regimen.
CTID: UMIN000004202
Phase: Phase II Status: Complete: follow-up complete
Date: 2010-09-05

Study of Aprepitant / Palonosetron / Dexamethasone for nausea and vomiting induced chemotherapy for breast cancer.
CTID: UMIN000004025
Phase: Phase II Status: Complete: follow-up complete
Date: 2010-08-10

Efficacy and tolerability of combination therapy with aprepitant,palonosetron,and dexamethasone for the prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based chemotherapy for gynecological cancer(Phase II Study)
CTID: UMIN000003820
Phase: Phase II Status: Complete: follow-up complete
Date: 2010-06-24

生物数据图片

Br J Pharmacol. 1995 Feb; 114(4): 851–859.
Br J Pharmacol. 1995 Feb; 114(4): 851–859.
Br J Pharmacol. 1995 Feb; 114(4): 851–859.