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Granisetron hydrochloride

Outline of Granisetron hydrochloride Domestic Market Analysis Instructions Chemical Properties Uses
Granisetron hydrochloride
Granisetron hydrochloride
CAS No.
107007-99-8
Chemical Name:
Granisetron hydrochloride
Synonyms
Kitryl;KYTRIL;BRL-43694A;Gransetron HCl;GRANISETRON HCL;GranisetronBase;midehydrochloride;GranisetronHclFda;endo-monohydrochlorid;endo-monohydrochloride
CBNumber:
CB9728851
Molecular Formula:
C18H25ClN4O
Formula Weight:
348.87
MOL File:
107007-99-8.mol

Granisetron hydrochloride Properties

Melting point:
290-292°C
storage temp. 
Room temp
solubility 
H2O: >10mg/mL
color 
white to off-white
Merck 
14,4536
CAS DataBase Reference
107007-99-8(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  Xn,Xi
Risk Statements  22-62-37/38-36/37/38-36
Safety Statements  26-36-37-24/25
RTECS  NK7882200
Symbol(GHS):
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning P264, P270, P301+P312, P330, P501
Precautionary statements:

Granisetron hydrochloride price More Price(9)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich G3796 Granisetron hydrochloride ≥98% (HPLC), solid 107007-99-8 10mg $118 2018-11-20 Buy
Sigma-Aldrich 1298106 Granisetron hydrochloride United States Pharmacopeia (USP) Reference Standard 107007-99-8 150mg $784 2018-11-20 Buy
TCI Chemical G0401 Granisetron Hydrochloride >98.0%(HPLC)(T) 107007-99-8 200mg $59 2018-11-22 Buy
TCI Chemical G0401 Granisetron Hydrochloride >98.0%(HPLC)(T) 107007-99-8 1g $207 2018-11-22 Buy
Cayman Chemical 21239 Granisetron (hydrochloride) ≥98% 107007-99-8 1g $338 2018-11-19 Buy

Granisetron hydrochloride Chemical Properties,Uses,Production

Outline of Granisetron hydrochloride

Granisetron hydrochloride was originally developed by the British Beecham company in the mid-1980s. At 1991, the merged Smithkline-Beecham (SB) Company had pushed for the first time of 3 mg of injection Kytri1 to the market in South Africa. To date, including 1 mg of oral tablets, 1mg of injections, granisetron hydrochloride has already entered into market in United States, Britain, France, Japan, Germany, Italy and other more than forty countries and regions around the world. When the Smithkline-Beecham (SB) Company was merged with Glaxo Company, it transferred this product to the Roche Company.
Foreign research data has shown that granisetron hydrochloride has a high selectivity to receptor. Its affinity to 5-HT3 receptor is 4000 to 10000 time as high as its affinity to other receptors, such as 5-HT1, 5-HT2, dopamine D1, D1, histamine H1, benzodiazepine and opioid receptor. For comparison, the difference for ondansetron is only about 1,000 times. For the test of its prevention of cisplatin-induced emesis in ferrets, the antiemetic rates in the three dose groups of granisetron hydrochloride 2 × 0.005,2 × 0.05 and 2 × 0.5mg/kg (iv) were 93%, 96% and 100 %, respectively while for ondansetron in 2 × 2.5mg/kg, this value was 89%, demonstrating that granisetron hydrochloride exhibited a at least five times stronger efficacy of anti-emetic than ondansetron. Toxicity studies suggest that granisetron hydrochloride can achieve very excellent antiemetic effect even in small dose with only minor side effects. However, there may be sth abnormal occurring in cardiovascular system upon large doses. Since the recommended clinical dose of granisetron hydrochloride is small (3mg/d), which is only 1/25 (<1 mg/kg) of the lowest dose used in animal studies, therefore, clinical application of it is very safe. Pharmacokinetic study has shown that granisetron hydrochloride has a half-life (t1/2) of 9 h in the body of patient while this value is 4 h at healthy people, 7.7 h in elderly people and 4.9h in young people. Granisetron hydrochloride is mainly metabolized in the liver and can be excreted through the feces and urine in the form of 7-hydroxy granisetron hydrochloride and other forms of metabolic product. For patients of liver damage or liver metastases, they have reduced plasma clearance rate with the scavenging rate upon renal insufficiency being 1/4 of the normal case. It has been observed of high first pass metabolism upon oral administration with the absolute bioavailability being 60%.

Domestic Market Analysis

1993, China has approved of the import of the Kytri1 injection (3 mg/ 3 mL) of British SB company, Registration No: X930279, and has allowed for in clinical trials. In 1994, the China-US Tianjin Smith Kline Pharmaceutical Co., Ltd. had used imported raw materials processing method for production of the injection of the 3mg granisetron hydrochloride and had obtained the approval of the Ministry of Health: (94) health medicine approved: J-10 number (fourth class) with the trade name being "Kay Reiter. " Currently there are a number of domestic manufacturers having their products enter into market with the number of manufacture which makes formulation being up to dozen, see Annex I for details.
China has a large population with the annual number of newly identified cancer patients being more than 1.6 million. The nausea and vomiting induced by chemotherapy and radiotherapy-induced have been one of the serious side effects that doctors and patients worry of. Therefore, new antiemetics are in urgent demand. Currently, ondansetron class of drugs has occupied most of the market antiemetic including ondansetron (ShufuLing), granisetron hydrochloride (Kytril) and tropisetron (Oubiting), wherein the ondansetron and granisetron has been accumulated of large number of clinical application experience with good response from the doctors and has played positive role on improving the domestic situation of the treatment of chemotherapy vomiting. With the localization of products, the decreasing price and the increasing income level of people, antiemetics market will be certainly greatly improved. In this case, granisetron hydrochloride, as the secondary antiemetic drug entering into market, will certainly have good market prospects.
The above information is edited by the chemicalbook of Dai Xiongfeng.

Instructions

[Character]it is colorless or nearly colorless liquid clarity.
[Toxicology]This product is a highly selective 5-HT3 receptor antagonist and has excellent preventive and therapeutic effect on treating nausea and vomiting induced by radiotherapy, chemotherapy and surgery. Radiotherapy, chemotherapy and surgery and other factors can cause enterochromaffin cells to release 5-HT; 5-HT can activate the 5-HT3 receptors in central nerve or vagus nerve and cause vomiting reflex. The mechanism of this product in controlling nausea and vomiting is through antagonizing the 5-HT3 receptor in the central chemosensory area and peripheral vagus nerve terminal, further suppressing the nausea and vomiting. This product has high selectivity and no side effects such as extrapyramidal reactions, excessive sedation and so on.
[Indications]it is suitable for the treatment of nausea and vomiting induced by radiation therapy and cytotoxic drug.
[Dosage and usage amount]intravenous drip. Recommended dosage for adults is usually 3 mg. Administer it intravenously 30 minutes prior to chemotherapy. Most patients only need to be administered once with the prevention action against nausea and vomiting being more than 24 hours. The number of doses can be increased by 1-2 times if necessary, but the maximum daily dose should not exceed 9 mg and the infusion time should not be less than 5 minutes.
[Pharmacokinetics]healthy volunteers, after intravenous injection of this product for 20 or 40 μg/kg, the average peak plasma concentration was 13.7 and 42.8μg/L, the plasma elimination half-life is approximately 3.1-5.9 hours. This product is widely distributed in the body with serum protein binding rate being about 65%. Most of them are rapidly metabolized with the major metabolic pathway being N-dealkylation and conjugation after aromatic oxidation. This product is excreted through the feces and urine.

Chemical Properties

It is white or yellowish white crystalline powder and is odorless. It is easily soluble in water but hardly soluble in methanol, extremely hardly to be dissolved in ethanol and almost insoluble in ether. It has a melting point of 290-292 ℃. For acute toxicity LD50, female mice, male and female rats (mg/kg): 17, 25, 14, 16, respectively. Intravenous injection.

Uses

It is the selective antagonist of the 5-serotonin 3 (5-HT3) in peripheral and central nervous system.

Chemical Properties

White to Off-White Crystalline Sold

Uses

anticoagulant

Uses

A specific serotonin (5HT3) receptor antagonist. Used as an antiemetic. Granisetron HCl is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemothera py. Its main effect is to reduce the activity of the vagus nerve. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarini c receptor

brand name

Kytril (Roche).

Biological Activity

5-HT 3 receptor antagonist that possesses potent antiemetic activity.

Granisetron hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products


Granisetron hydrochloride Suppliers

Global( 306)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19958 60
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3218 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22063 58
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1529 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20795 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32764 55
PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2549 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 663 60
Jinan Jianfeng Chemical Co., Ltd
15562555968
info@pharmachemm.com CHINA 617 58
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 20001 58

View Lastest Price from Granisetron hydrochloride manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-07-26 Granisetron hydrochloride
107007-99-8
US $100.00 / KG 1KG 99% Customized career henan chemical co

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