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MedKoo Cat#: 100695 | Name: Palonosetron HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Palonosetron (INN, trade name Aloxi) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is used for the control of delayed CINV—nausea and vomiting and there are tentative data to suggest that it may be better than granisetron. Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy, or as a single oral capsule one hour before chemotherapy. The oral formulation was approved on August 22, 2008 for prevention of acute CINV alone, as a large clinical trial did not show oral administration to be as effective as intravenous use against delayed CINV. (Source: http://en.wikipedia.org/wiki/Palonosetron).

Chemical Structure

Palonosetron HCl
Palonosetron HCl
CAS#135729-62-3 (HCl); 135729-61-2 (free base).

Theoretical Analysis

MedKoo Cat#: 100695

Name: Palonosetron HCl

CAS#: 135729-62-3 (HCl); 135729-61-2 (free base).

Chemical Formula: C19H25ClN2O

Exact Mass: 0.0000

Molecular Weight: 332.87

Elemental Analysis: C, 68.56; H, 7.57; Cl, 10.65; N, 8.42; O, 4.81

Price and Availability

Size Price Availability Quantity
100mg USD 450.00 2 Weeks
200mg USD 750.00 2 Weeks
500mg USD 1,650.00 2 Weeks
1g USD 2,950.00 2 Weeks
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Related CAS #
No Data
Synonym
RS 25233-197; RS25233-197; RS-25233-197; RS25233-198; RS-25233-198; RS 25233-198; RS-25259-197; Palonosetron hydrochloride; US brand name: Aloxi.
IUPAC/Chemical Name
(R)-2-((S)-quinuclidin-3-yl)-2,3,3a,4,5,6-hexahydro-1H-benzo[de]isoquinolin-1-one hydrochloride
InChi Key
OLDRWYVIKMSFFB-KPVRICSOSA-N
InChi Code
InChI=1S/C19H24N2O.ClH/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;1H/t15-,17+;/m0./s1
SMILES Code
O=C1N([C@@H]2CN3CCC2CC3)C[C@@]4([H])C5=C1C=CC=C5CCC4.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
P alonosetron hydrochloride is the hydrochloride salt of palonosetron, a carbazole derivative and a selective serotonin receptor antagonist with antiemetic activity. Palonosetron competitively blocks the action of serotonin at 5-hydroxytryptamine type 3 (5-HT3) receptors located on vagal afferents in the chemoreceptor trigger zone (CTZ), resulting in suppression of chemotherapy-induced nausea and vomiting. The CTZ is located in the area postrema on the dorsal surface of the medulla oblongata at the caudal end of the fourth ventricle and outside the blood-brain barrier (BBB). Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)   Palonosetron is administered intravenously, as a single dose, 30 minutes before chemotherapy, or as a single oral capsule one hour before chemotherapy. The oral formulation was approved on August 22, 2008 for prevention of acute CINV alone, as a large clinical trial did not show oral administration to be as effective as intravenous use against delayed CINV.   ALOXI is an antiemetic and antinauseant agent. It is a serotonin subtype 3 (5-HT3) receptor antagonist with a strong binding affinity for this receptor. The empirical formula is C19H24N2O.HCl, with a molecular weight of 332.87. Palonosetron hydrochloride is a white to off-white crystalline powder. It is freely soluble in water, soluble in propylene glycol, and slightly soluble in ethanol and 2-propanol. ALOXI Injection is a sterile, clear, colorless, non-pyrogenic, isotonic, buffered solution for intravenous administration. Each 5 mL vial of ALOXI Injection contains 0.25 mg palonosetron base as hydrochloride, 207.5 mg mannitol, disodium edetate and citrate buffer in water for intravenous administration. The pH of the solution is 4.5 to 5.5.   Mechanism of Action Palonosetron is a 5-HT3 receptor antagonist with a strong binding affinity for this receptor and little or no affinity for other receptors. Cancer chemotherapy may be associated with a high incidence of nausea and vomiting, particularly when certain agents, such as cisplatin, are used. 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 thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine and that the released serotonin then activates 5-HT3 receptors located on vagal afferents to initiate the vomiting reflex.  
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Palonosetron hydrochloride is a 5-HT3 antagonist.
In vitro activity:
The present work shows, through several independent experiments, that palonosetron uniquely triggers 5-HT(3) receptor internalization and induces prolonged inhibition of receptor function. After 24h incubation followed by dissociation conditions, [(3)H]palonosetron remained associated with whole cells but not to cell-free membranes (P<0.001). [(3)H]Palonosetron's binding to cells was resistant to both protease and acid treatments designed to denature cell surface proteins suggesting that the receptor complex was inside the cells rather than at the surface. Cells pretreated with unlabeled palonosetron subsequently exhibited reduced cell surface 5-HT(3) receptor binding. Reference: Eur J Pharmacol. 2010 Jan 25;626(2-3):193-9. https://pubmed.ncbi.nlm.nih.gov/19836386/
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO:PBS (pH 7.2) (1:4) 0.2 0.60
Ethanol 0.5 1.50
Water 66.8 200.57
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 332.87 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
Rojas C, Thomas AG, Alt J, Stathis M, Zhang J, Rubenstein EB, Sebastiani S, Cantoreggi S, Slusher BS. Palonosetron triggers 5-HT(3) receptor internalization and causes prolonged inhibition of receptor function. Eur J Pharmacol. 2010 Jan 25;626(2-3):193-9. doi: 10.1016/j.ejphar.2009.10.002. Epub 2009 Oct 15. PMID: 19836386.
In vitro protocol:
Rojas C, Thomas AG, Alt J, Stathis M, Zhang J, Rubenstein EB, Sebastiani S, Cantoreggi S, Slusher BS. Palonosetron triggers 5-HT(3) receptor internalization and causes prolonged inhibition of receptor function. Eur J Pharmacol. 2010 Jan 25;626(2-3):193-9. doi: 10.1016/j.ejphar.2009.10.002. Epub 2009 Oct 15. PMID: 19836386.
In vivo protocol:
TBD
1: Watanabe D, Iihara H, Kobayashi R, Fujii H, Mori R, Kumada K, Shimizu M, Futamura M, Suzuki A. Dexamethasone-sparing strategies in anthracycline and cyclophosphamide-based chemotherapy with a focus on 5-HT3 receptor antagonists: a network meta-analysis. Front Oncol. 2024 Jul 26;14:1414037. doi: 10.3389/fonc.2024.1414037. PMID: 39132500; PMCID: PMC11310115. 2: Ostwal V, Ramaswamy A, Mandavkar S, Bhargava P, Naughane D, Sunn SF, Srinivas S, Kapoor A, Mishra BK, Gupta A, Sansar B, Pal V, Pandey A, Bonda A, Siripurapu I, Muddu VK, Kannan S, Chaugule D, Patil R, Parulekar M, Dhanawat A, Trikha M, Ghosh J, Noronha V, Menon N, Patil V, Prabhash K, Olver I. Olanzapine as Antiemetic Prophylaxis in Moderately Emetogenic Chemotherapy: A Phase 3 Randomized Clinical Trial. JAMA Netw Open. 2024 Aug 1;7(8):e2426076. doi: 10.1001/jamanetworkopen.2024.26076. PMID: 39106066; PMCID: PMC11304110. 3: Liu Y, Hu P, Jiang Y, Chen X, Li S. Low dose of dexamethasone combined with netupitant and palonosetron in preventing nausea and vomiting in breast cancer patients induced by anthracycline drugs. Clin Transl Oncol. 2024 Jul 13. doi: 10.1007/s12094-024-03581-7. Epub ahead of print. PMID: 39002066. 4: Kim MK, Kim I, Kang H, Wi W, Park YH, Jung YH, Woo YC, Baek CW. Effect of intravenous palonosetron on hypotension induced by spinal anesthesia for cesarean section: A randomized controlled trial. PLoS One. 2024 Jun 25;19(6):e0305913. doi: 10.1371/journal.pone.0305913. PMID: 38917195; PMCID: PMC11198823. 5: Sakamoto T, Kado M, Saito Y, Uchiyama K, Kanno R, Taniguchi O, Takekuma Y, Sakakibara-Konishi J, Shimizu Y, Kinoshita I, Sugawara M. Evaluation of Efficacy of Adding Aprepitant to Palonosetron and Dexamethasone in Carboplatin and Etoposide Therapy. Biol Pharm Bull. 2024;47(6):1189-1195. doi: 10.1248/bpb.b24-00046. PMID: 38897969. 6: Lin C, Li J, Wu Q, Luo T, Zheng Z. Postoperative Nausea and Vomiting in Female Patients Undergoing Laparoscopic Gastrointestinal Surgery with Double Prophylactic Therapy. Surg J (N Y). 2024 Jun 3;10(2):e25-e30. doi: 10.1055/s-0044-1787305. PMID: 38835494; PMCID: PMC11147651. 7: Gutgarts V, Gerardine S, Shingarev RA, Knezevic A, Zabor EC, Latcha S, Joy MS, Aleksunes LM, Jaimes EA. Evaluation of Cisplatin-Induced Acute Kidney Injury in Patients Co-Prescribed Serotonin Receptor Antagonists: A Retrospective Analysis. Kidney360. 2024 May 30. doi: 10.34067/KID.0000000000000464. Epub ahead of print. PMID: 38814726. 8: Shen J, Zhao J, Jin G, Li H, Jiang Y, Wu Y, Gao J, Chen F, Li J, Wang W, Li Q. A prospective randomized controlled clinical trial investigating the efficacy of low-dose olanzapine in preventing nausea and vomiting associated with oxaliplatin-based and irinotecan-based chemotherapy. J Cancer Res Clin Oncol. 2024 May 28;150(5):283. doi: 10.1007/s00432-024-05712-7. PMID: 38806870; PMCID: PMC11133208. 9: Ganguly S, Sasi A, Nagaraju SKK, Bakhshi S. Anti-Emetics in Children Receiving Chemotherapy for Solid Tumors and Leukemia: Pharmacology and Optimization of Therapy for Nausea and Vomiting. Pharmaceuticals (Basel). 2024 May 10;17(5):616. doi: 10.3390/ph17050616. PMID: 38794186; PMCID: PMC11124061. 10: Kwak K, Park Y, Kim BS, Kang KW. Efficacy and safety of netupitant/palonosetron in preventing nausea and vomiting in diffuse large B cell lymphoma patients undergoing R-CHOP chemotherapy. Sci Rep. 2024 May 16;14(1):11229. doi: 10.1038/s41598-024-62057-4. PMID: 38755279; PMCID: PMC11099181. 11: Alves RB, Rebouças CV, Yamada AMTD, Cruz FJSM. Prevalence of anticipatory nausea and vomiting in breast cancer patients undergoing highly emetogenic chemotherapy. Rev Assoc Med Bras (1992). 2024 May 3;70(4):e20230937. doi: 10.1590/1806-9282.20230937. PMID: 38716933; PMCID: PMC11068401. 12: Zhang W, Shen Z, Jiang J, Zhu S, Zhang P, Chen S, Kang M. Comparative efficacy of prophylactic protocols in reducing perioperative nausea and vomiting during video-assisted thoracoscopic radical resection of lung cancer. Sci Rep. 2024 Apr 29;14(1):9818. doi: 10.1038/s41598-024-59687-z. PMID: 38684769; PMCID: PMC11059372. 13: Gupta S, Mv C, Thomas B, Biswas G, Gupta S, Dattatreya PS, Bhagat S, Patil S, Bhushan S, Barkate H. An Open-Label, Single-Arm, Multicenter, Observational Study Evaluating the Safety and Effectiveness of Akynzeo® in the Management of Chemotherapy-Induced Nausea and Vomiting in India. Cureus. 2024 Mar 19;16(3):e56447. doi: 10.7759/cureus.56447. Erratum in: Cureus. 2024 Apr 19;16(4):c169. doi: 10.7759/cureus.c169. PMID: 38638750; PMCID: PMC11024873. 14: Hamada H, Suzuki E, Endo M, Mihara Y, Iketani S, Ishida M, Miyasato A, Miyazaki K. Opioid-induced respiratory depression suspected of drug interaction in a prostate cancer patient: a case report. Ann Palliat Med. 2024 Mar;13(2):428-432. doi: 10.21037/apm-23-581. PMID: 38584476. 15: Notini G, Naldini MM, Sica L, Viale G, Rognone A, Zambelli S, Zucchinelli P, Piras M, Bosi C, Mariani M, Aldrighetti D, Bianchini G, Licata L. Management of Trastuzumab Deruxtecan-related nausea and vomiting in real-world practice. Front Oncol. 2024 Mar 11;14:1374547. doi: 10.3389/fonc.2024.1374547. PMID: 38529378; PMCID: PMC10961432. 16: Estrada Alamo CE, Hwangpo S, Chamberlain L, Chon C, Nair B, O'Reilly-Shah V, Bain SE, Liberman JS. Intraoperative Prophylaxis with Palonosetron for Postoperative Nausea and/or Vomiting in Adults Undergoing Cardiothoracic Surgery Under General Anesthesia: A Single-Center Retrospective Study. J Cardiothorac Vasc Anesth. 2024 May;38(5):1181-1189. doi: 10.1053/j.jvca.2024.01.036. Epub 2024 Feb 8. PMID: 38472029. 17: Brown JM, Mathew S, Sulis ML, Dupuis LL, Thackray J. Vomiting in children and adolescents receiving intravenous pegaspargase: a retrospective study. Pediatr Hematol Oncol. 2024 Aug;41(5):376-381. doi: 10.1080/08880018.2024.2311886. Epub 2024 Mar 7. PMID: 38454568. 18: Celio L, Aapro M. Characteristics of nausea and its impact on health-related quality of life in cisplatin-treated patients receiving dexamethasone-sparing prophylaxis: an analysis of the LUNG-NEPA study. Support Care Cancer. 2024 Mar 4;32(3):204. doi: 10.1007/s00520-024-08406-5. PMID: 38433125. 19: Ames M, Patel P, Dupuis LL, Koo A. Palonosetron in pediatric patients: A single-center, retrospective evaluation of policy and clinical practice guideline discordance. J Oncol Pharm Pract. 2024 Feb 29:10781552241233489. doi: 10.1177/10781552241233489. Epub ahead of print. PMID: 38425048. 20: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Fosnetupitant. 2024 Feb 28. PMID: 38498661.

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KS 619-1

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