Palonosetron
(Synonyms: 帕洛诺司琼) 目录号 : GC36844
Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
Cas No.:135729-61-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Palonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with Ki value of 0.17 nM. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
Palonosetron is a 5-HT3 receptor antagonist with a high binding affinity for this receptor and little or no affinity for other receptors[1].
Palonosetron has a longer half-life and a higher binding affinity than the first-generation 5-HT3 receptor antagonists. After intravenous dosing of palonosetron in healthy subjects and cancer patients, an initial decline in plasma concentration is followed by a slow elimination from the body. Mean maximum plasma concentration and area under the concentration-time curves are generally dose-proportional over the dose range of 0.3 to 90 μg/kg in healthy subjects and in cancer patients. Palonosetron has a volume of distribution of approximately 8.3 ± 2.5 L/kg and is 62% bound to plasma proteins. It is eliminated from the body through renal excretion and metabolic pathways. The mean terminal elimination half-life is approximately 40 hours[1].
[1] Rudolph M Navari. Cancer Manag Res. 2009, 1: 167-176. [2] Price KL, et al. ACS Chem Neurosci. 2016, 7(12):1641-1646.
| Cas No. | 135729-61-2 | SDF | |
| 别名 | 帕洛诺司琼 | ||
| Canonical SMILES | O=C1N(C[C@@]([H])(CCC2)C3=C2C=CC=C13)[C@@H]4CN5CCC4CC5 | ||
| 分子式 | C19H24N2O | 分子量 | 296.41 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 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 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Palonosetron
Drugs 2004;64(10):1125-32; discussion 1133-4.PMID:15139789DOI:10.2165/00003495-200464100-00006.
Palonosetron is a potent and highly selective serotonin 5-HT(3) receptor antagonist that has been evaluated for the prevention of chemotherapy-induced nausea and vomiting. black triangle Intravenously administered Palonosetron has a linear pharmacokinetic profile, with a long terminal elimination half-life ( approximate, equals 40 hours) and moderate (62%) plasma protein binding. In two randomised, double-blind trials in 1132 cancer patients receiving moderately emetogenic chemotherapy, intravenous Palonosetron 0.25 mg was more effective than intravenous ondansetron 32 mg in producing a complete response (no emesis, no use of rescue medication) during acute (0-24 hours) or delayed (24-120 hours) phases, and similar to intravenous dolasetron 100 mg in acute, but more effective in delayed phase. Palonosetron 0.75 mg was similar to ondansetron (acute and delayed phase) or dolasetron (acute phase), but more effective than dolasetron in delayed phase. In patients receiving highly emetogenic chemotherapy (n = 667), the complete response rates during acute and delayed phases with intravenous Palonosetron (0.25 or 0.75 mg) were similar to those seen in intravenous ondansetron 32 mg recipients in a randomised, double-blind trial. Intravenous Palonosetron was generally well tolerated in clinical trials, with few adverse events being treatment related. Palonosetron had no significant effect on the corrected QT interval or laboratory parameters.
Netupitant-palonosetron (NEPA) for Preventing Chemotherapy-induced Nausea and Vomiting: From Clinical Trials to Daily Practice
Curr Cancer Drug Targets 2022;22(10):806-824.PMID:35570542DOI:10.2174/1568009622666220513094352.
Chemotherapy-induced nausea and vomiting (CINV) is a common adverse event associated with many anticancer therapies and can negatively impact patients' quality of life and potentially limit the effectiveness of chemotherapy. Currently, CINV can be prevented in most patients with guideline-recommended antiemetic regimens. However, clinicians do not always follow guidelines, and patients often face difficulties adhering to their prescribed treatments. Therefore, approaches to increase guideline adherence need to be implemented. NEPA is the first and only fixed combination antiemetic, composed of netupitant (oral)/fosnetupitant (intravenous) and Palonosetron, which, together with dexamethasone, constitute a triple antiemetic combination recommended for the prevention of CINV for patients receiving highly emetogenic chemotherapy and for certain patients receiving moderately emetogenic chemotherapy. Thus, NEPA offers a convenient and straightforward antiemetic treatment that could improve adherence to guidelines. This review provides an overview of CINV, evaluates the accumulated evidence of NEPA's antiemetic activity and safety from clinical trials and real-world practice, and examines the preliminary evidence of antiemetic control with NEPA in daily clinical settings beyond those described in pivotal trials. Moreover, we review the utility of NEPA in controlling nausea and preserving patients' quality of life during chemotherapy, two major concerns in managing patients with cancer.
Palonosetron: in the prevention of nausea and vomiting
Drugs 2009 Nov 12;69(16):2257-78.PMID:19852528DOI:10.2165/11200980-000000000-00000.
Palonosetron is a second-generation serotonin 5-HT3 receptor antagonist, with a distinct pharmacological profile that differs from first-generation 5-HT3 receptor antagonists. Intravenous Palonosetron is widely indicated for the prevention of chemotherapy-induced nausea and vomiting (CINV) in the acute and delayed phases following moderately emetogenic chemotherapy (MEC) and the prevention of CINV in the acute phase following highly emetogenic chemotherapy (HEC). In the US, oral Palonosetron is approved for the prevention of CINV in the acute phase following MEC (although this formulation is not currently available), and intravenous Palonosetron is indicated for the prevention of postoperative nausea and vomiting (PONV) in the first 24 hours following surgery. All indications are currently limited to adult patients. Intravenous Palonosetron was noninferior to intravenous ondansetron (with statistically greater efficacy than ondansetron) or dolasetron in preventing CINV following MEC, or to intravenous ondansetron or granisetron in preventing CINV following HEC, in the acute phase. Statistically greater efficacy was seen with intravenous Palonosetron than ondansetron or dolasetron in preventing CINV following MEC in the delayed phase. Oral Palonosetron was noninferior to intravenous Palonosetron in preventing CINV in the acute phase in patients receiving MEC. Intravenous Palonosetron was superior to placebo in preventing PONV in the first 24 hours following surgery. Palonosetron was generally well tolerated in clinical trials. Intravenous Palonosetron is a valuable option in the prevention of acute- and delayed-phase CINV in adult patients receiving MEC, and of acute-phase CINV in patients receiving HEC. Oral Palonosetron is likely to be a useful addition to oral formulations of other 5-HT3 receptor antagonists in preventing CINV in patients receiving MEC. Intravenous Palonosetron is a useful alternative to currently recommended agents in PONV prevention.
Palonosetron for the treatment of chemotherapy-induced nausea and vomiting
Expert Opin Pharmacother 2014 Dec;15(17):2599-608.PMID:25323946DOI:10.1517/14656566.2014.972366.
Introduction: Chemotherapy-induced nausea and vomiting (CINV) is associated with a significant deterioration in quality of life. The emetogenicity of the chemotherapeutic agents, repeated chemotherapy cycles, and patient risk factors significantly influence CINV. The introduction of 5-hydroxytryptamine-3 (5-HT3) receptor antagonists has been a major factor in the improvement of the prevention of chemotherapy-induced acute and delayed emesis. Palonosetron , a second-generation 5-HT3 receptor antagonist with a different half-life, a different binding capacity, and a different mechanism of action than the first-generation 5-HT3 receptor antagonists appears to be the most effective agent in this drug class. Areas covered: Palonosetron's chemistry, pharmacodynamics, pharmacokinetics, metabolism, clinical efficacy, including comparison with other antiemetics, role in controlling nausea, potential role in multi-day chemotherapy and bone marrow transplantation, and overall safety are discussed. Expert opinion: The clinical data in the literature have established Palonosetron as the 5-HT3 receptor antagonist of choice in terms of efficacy and safety for the prevention of CINV for patients receiving moderately or highly emetogenic chemotherapy. Three international guidelines have listed Palonosetron as the preferred 5-HT3 receptor antagonist. Due to its higher efficacy, the use of Palonosetron may be more cost effective compared to the generic first-generation 5-HT3 receptor antagonists. Clinical organizations' pharmacy and formulary committees should consider efficacy when making recommendations for agents for the prevention of CINV.
Palonosetron: a second generation 5-hydroxytryptamine 3 receptor antagonist
Expert Opin Drug Metab Toxicol 2009 Dec;5(12):1577-86.PMID:19929251DOI:10.1517/17425250903407289.
Background: Chemotherapy-induced nausea and vomiting (CINV) is associated with a significant deterioration in quality of life. The emetogenicity of the chemotherapeutic agents, repeated chemotherapy cycles and patient characteristics (female gender, younger age, low alcohol consumption, history of motion sickness) are the major risk factors for CINV. Objective: This review provides a detailed description of Palonosetron, a second generation 5-HT3 receptor antagonist. Methods: The chemistry and pharmacology of Palonosetron are described, as well as the initial and recent clinical trials. Results/conclusion: Palonosetron has a longer half-life and a higher binding affinity than the first generation 5-HT3 receptor antagonists. Palonosetron has been approved for the prevention of acute CINV in patients receiving either moderately or highly emetogenic chemotherapy and for the prevention of delayed CINV in patients receiving moderately emetogenic chemotherapy. In recent studies, compared to the first generation 5-HT3 receptor antagonists, Palonosetron in combination with dexamethasone demonstrated better control of delayed CINV in patients receiving highly emetogenic chemotherapy. There were no clinically relevant adverse reactions reported in the Palonosetron clinical trials that were different from the common reactions reported for the 5-HT3 receptor antagonist class. Due to its efficacy in controlling both acute and delayed CINV, Palonosetron may be very effective in the clinical setting of multiple-day chemotherapy and bone marrow transplantation.