Nausea and vomiting drug Adverse effects References
ChemicalBook > CAS DataBase List > Palonosetron Hydrochloride

Palonosetron Hydrochloride

Nausea and vomiting drug Adverse effects References
Product Name
Palonosetron Hydrochloride
CAS No.
135729-62-3
Chemical Name
Palonosetron Hydrochloride
Synonyms
PALONOSETRON HCL;Aloxi;Palonosetron HCI;CS-292;Onicit;RS 25259;RS-25259-197;PalnosetronHcl;a 5-HT3 antagonist;Palonosetron-d3 HCl
CBNumber
CB0210849
Molecular Formula
C19H25ClN2O
Formula Weight
332.87
MOL File
135729-62-3.mol
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Palonosetron Hydrochloride Property

Melting point:
>290°C
alpha 
D25 -94.1° (c = 0.4 in water)
storage temp. 
Inert atmosphere,Store in freezer, under -20°C
solubility 
Methanol (Slightly, Heated), Water (Slightly)
form 
Solid
color 
White to Off-White
Merck 
14,6997
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-;/s3
InChIKey
OLDRWYVIKMSFFB-HYCRUXCXNA-N
SMILES
N1(C[C@@]2([H])CCCC3=CC=CC(=C32)C1=O)[C@H]1[C@]2([H])CCN(CC2)C1.Cl |&1:2,15,16,r|
CAS DataBase Reference
135729-62-3(CAS DataBase Reference)
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Safety

HS Code 
29339900
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H312Harmful in contact with skin

H332Harmful if inhaled

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P322Specific measures (see …on this label).

P330Rinse mouth.

P363Wash contaminated clothing before reuse.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

TCI Chemical
Product number
P2051
Product name
Palonosetron Hydrochloride
Purity
>98.0%(HPLC)(T)
Packaging
200mg
Price
$215
Updated
2024/03/01
TCI Chemical
Product number
P2051
Product name
Palonosetron Hydrochloride
Purity
>98.0%(HPLC)(T)
Packaging
1g
Price
$741
Updated
2024/03/01
Cayman Chemical
Product number
16752
Product name
Palonosetron (hydrochloride)
Purity
≥98%
Packaging
5mg
Price
$73
Updated
2024/03/01
Cayman Chemical
Product number
16752
Product name
Palonosetron (hydrochloride)
Purity
≥98%
Packaging
10mg
Price
$131
Updated
2024/03/01
Cayman Chemical
Product number
16752
Product name
Palonosetron (hydrochloride)
Purity
≥98%
Packaging
50mg
Price
$359
Updated
2024/03/01
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Palonosetron Hydrochloride Chemical Properties,Usage,Production

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

Description

Palonosetron is a novel 5-HT3 receptor antagonist launched as an injectable agent for the prevention of acute and delayed nausea and vomiting associated with cancer chemotherapy. It has a much longer half-life (～ 40 h) than the other currently available 5-HT3 antagonists, which provides efficacy advantages in the prevention of delayed nausea and vomiting that typically occurs after 24 h and up to six days post chemotherapy administration. Palonosetron was developed as a conformationally restricted analog of the previously known 5HT3 antagonists tropisetron and granisetron. It is synthesized in four steps starting with the condensation of 1,8- naphthalic anhydride and (S)-3-aminoquinuclidine to produce the corresponding imide. The subsequent steps include catalytic hydrogenation of one of the aromatic rings of the imide intermediate, selective reduction of one of the carbonyls to a hydroxyl group, dehydration to an olefin and catalytic hydrogenation. The recommended dosage of palonosteron is 0.25 mg, administered as a single intravenous dose approximately 30 min before the start of chemotherapy. Palonosetron exhibits dose-proportional pharmacokinetics and it is moderately bound to plasma proteins (62%). Fifty percent of the dose is metabolized in the liver, and 40% is excreted unchanged in the urine. In comparative clinical studies with two other 5- HT3 receptor antagonists, palonosetron is shown to be as effective as dolasetron and more effective than ondansetron in controlling acute nausea and vomiting and superior to both in the control of delayed nausea and vomiting. Efficacy of palonosetron has been demonstrated in patients receiving initial and repeat courses of both moderately and highly emetogenic chemotherapy, including cisplatin, cyclophosphamide and dacarbazine. At 0.25 and 0.75 mg doses, palonosetron is well tolerated and the most occurring adverse events are headache, diarrhea, fatigue, abdominal pain and insomnia.

Chemical Properties

White Solid

Originator

Syntex (Roche Bioscience) (US)

Uses

(S,S)-Palonosetron Hydrochloride is a serotonin 5-HT3 receptor antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). Antiemetic.

Uses

Palonosetron HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting

Uses

specifically inhibits cells of the adrenal cortex and their production of hormones for adrenocortical tumor therapy, causes CNS damage, but no bone marrow depression.

Uses

Palonosetron is a potent, selective antagonist of the serotonin (5-HT) receptor 5-HT3 (pKi = 10.4 in rat cortex) that minimally effects a wide range of other neuronal receptors. It is orally bioavailable and potently inhibits emesis induced by chemotherapeutic drugs, like cisplatin , but not by apomorphine , which acts by dopamine receptor antagonism. Palonosetron is remarkable for its long duration of action, related to its high receptor-binding affinity and long half-life. It is effective in managing chemotherapy-induced nausea and vomiting.[Cayman Chemical]

Definition

ChEBI: A hydrochloride obtained by combining palonosetron with one molar equivalent of hydrogen chloride; an antiemetic used in combination with netupitant (under the trade name Akynzeo) to treat nausea and vomiting in patients undergoing cancer chemotherapy.

brand name

Aloxi (Helsinn).

storage

Store at -20°C

Palonosetron Hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from Palonosetron Hydrochloride manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Palonosetron Hydrochloride 135729-62-3
Price
US $0.00/KG
Min. Order
10g
Purity
99%min
Supply Ability
10kg
Release date
2021-11-02
Hebei Weibang Biotechnology Co., Ltd
Product
Palonosetron Hydrochloride 135729-62-3
Price
US $1.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
10 mt
Release date
2024-11-20
shandong perfect biotechnology co.ltd
Product
Palonosetron hydrochloride 135729-62-3
Price
US $0.00/g
Min. Order
1g
Purity
98% HPLC
Supply Ability
100kg
Release date
2023-08-14

135729-62-3, Palonosetron HydrochlorideRelated Search:

Pazopanib Hydrochloride Tropisetron Docetaxel Iodixanol Entecavir hydrate Lercanidipine hydrochloride Moxifloxacin hydrochloride Flavoxate hydrochloride 1-Adamantanamine hydrochloride Fluoxetine hydrochloride Pramoxine hydrochloride Granisetron Hydrochloride Palonosetron (S)-N-(1-Azabicyclo[2.2.2]oct-3-yl)-5,6,7,8-tetrahydro-1-naphthalenecarboxamide Palonosetron Hydrochloride Palonosetron PALONOSETRON HCL,(3as)-2-(3s)-1-azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-1h-benz[de]isoquinolin-1-one monohydrochloride 2-(piperidin-4-ylmethyl)-1,2,3,4-tetrahydroisoquinoline

  • (S)-2-((S)-quinuclidin-3-yl)-2,3,3a,4,5
  • Palonosetron hydrochloride, 99.5%, a 5-HT3 antagonist
  • PALONOSETRON HCL
  • PALONOSETRON HYDROCHLORIDE
  • CS-292
  • Palonosetronhydrochloride hydrochloride
  • Palonosetron-d3 HCl
  • (3aS)-2-(3S)-1-Azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one Hydrochloride
  • Aloxi
  • Onicit
  • RS-25259-197
  • (3aS)-2-(3S)-1-Azabicyclo[2.2.2]oct-3-yl-2,3,3a,4,5,6-hexahydro-1H-benz[de]isoquinolin-1-one monohydrochloride
  • (S,S)-Palonosetron Hydrochloride
  • (S,S)-Palonosetron HCl
  • (3aS)-2-[(S)-1-Azabicyclo[2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-1-oxo-1H-benz[de]isoquinoline hydrochloride
  • Palonosetron Hydrochloride API
  • 1H-Benz[de]isoquinolin-1-one, 2-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-2,3,3a,4,5,6-hexahydro-, hydrochloride (1:1), (3aS)-
  • RS 25259
  • (S)-2-((S)-quinuclidin-3-yl)-2,3,3a,4,5,6-hexahydro-1H-benzo[de]isoquinolin-1-one hydrochloride
  • Palonosetron hydrochloride, >=99%
  • Palonosetron HCI
  • PalonosetronHydrochloride&gt
  • (S)-8-((((S)-quinuclidin-3-yl)amino)methyl)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
  • Palonosetron Hydrochloride USP/EP/BP
  • a 5-HT3 antagonist
  • PalnosetronHcl
  • Palonosetron HCl (RS25233-197
  • (5S)-3-[(3S)-1-azabicyclo[2.2.2]octan-3-yl]-3-azatricyclo[7.3.1.?,13]trideca-1(13),9,11-trien-2-one hydrochloride
  • Palonosetron Hydrochloride (1492200)
  • Methylisothiazolinone free base
  • RS 25259 197|||Palonosetron HCl|||RS 25259
  • 135729-62-3
  • C19H24N2OHCl
  • C19H25ClN2O
  • C19H24N2OHC
  • Selective 5-HT3 Receptor Antagonist
  • Chiral Reagents
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • API
  • 135729-62-3