135729-62-3 Usage
Description
Palonosetron hydrochloride is a potent and selective serotonin 5-HT3 receptor antagonist, chemically synthesized as a conformationally restricted analog of tropisetron and granisetron. It is characterized by its long half-life (approximately 40 hours), high receptor-binding affinity, and long duration of action. This white solid is used primarily as an antiemetic agent, particularly in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
Uses
1. Used in Oncology:
Palonosetron hydrochloride is used as an antiemetic agent for the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). It is particularly effective in managing delayed nausea and vomiting that typically occurs after 24 hours and up to six days post chemotherapy administration. The recommended dosage is 0.25 mg, administered as a single intravenous dose approximately 30 minutes before the start of chemotherapy.
2. Used in Combination Therapy:
Palonosetron hydrochloride is used in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy. This combination therapy aims to enhance the overall efficacy of CINV management.
3. Used in Comparative Clinical Studies:
In comparative clinical studies, palonosetron hydrochloride has demonstrated its effectiveness as being as effective as dolasetron and more effective than ondansetron in controlling acute nausea and vomiting. It has also shown superiority over both in the control of delayed nausea and vomiting.
4. Used in Various Emeticogenic Chemotherapy Regimens:
The efficacy of palonosetron hydrochloride has been demonstrated in patients receiving initial and repeat courses of both moderately and highly emetogenic chemotherapy, including cisplatin, cyclophosphamide, and dacarbazine.
5. Used in Adrenal Cortex Tumor Therapy:
Although not a primary use, palonosetron hydrochloride is also mentioned to specifically inhibit cells of the adrenal cortex and their production of hormones, which could be relevant in adrenocortical tumor therapy. However,
Nausea and vomiting drug
Palonosetron hydrochloride is a drug to inhibit nausea and vomiting, which is a new type highly selective, high-affinity 5-HT3 receptor antagonist that can block the vomiting reflex center peripheral neurons presynaptic 5-HT. Receptor excitement directly affects the central nervous system in 5-HT. Impulse receptor excitement generated by the role of vagal afferent nerve after area, blocking the vagus nerve endings in the gut, preventing signals to 5-HT. Receptor trigger zone can reduce the incidence of nausea and vomiting. Central clinically for the treatment of acute severe emetogenic chemotherapy induced delayed nausea and vomiting. Because of its high curative effect, little side effect, long half-life (about 40 h), small dosage, and so on, it has attracted much attention.
With 1,2,3,4-tetrahydro-1-naphthoic acid as the starting material, the split, amination, reduction, cyclization, salt of palonosetron hydrochloride granisetron.
Clinical studies showed that palonosetron can be used safely with corticosteroids, analgesics, antiemetics, antispasmodics and anticholinergic drugsas the starting material, the split, amination, reduction, cyclization, salt of palonosetron hydrochloride granisetron.
Murine tumor model studies indicate that palonosetron does not inhibit the five kinds of chemotherapy drugs studied (cisplatin, cyclophosphamide, cytarabine, doxorubicin and mitomycin C) anti-cancer activity.
Adverse effects
The most common adverse effects are headache, which occurs in 4–11% of patients, and constipation in up to 6% of patients. In less than 1% of patients, other gastrointestinal disorders occur, as well as sleeplessness, first-and second-degree atrioventricular block, muscle pain and shortness of breath. Palonosetron is similarly well tolerated as other setrons, and slightly less than placebo.
References
https://en.wikipedia.org/wiki/Palonosetron
Originator
Syntex (Roche Bioscience) (US)
Check Digit Verification of cas no
The CAS Registry Mumber 135729-62-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,3,5,7,2 and 9 respectively; the second part has 2 digits, 6 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 135729-62:
(8*1)+(7*3)+(6*5)+(5*7)+(4*2)+(3*9)+(2*6)+(1*2)=143
143 % 10 = 3
So 135729-62-3 is a valid CAS Registry Number.
InChI:InChI=1/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-;/m1./s1
