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Isophosphamide

History Cyclophosphamide isomer Instructions for ifosfamide (for injection) Contraindications and Precautions Medicine interactions Uses The domestic market situation
Isophosphamide
Isophosphamide
CAS No.
3778-73-2
Chemical Name:
Isophosphamide
Synonyms
IF;Ifex;cyfos;z4942;A-4942;holoxan;IfoMide;mjf9325;NSC-1097;mitoxana
CBNumber:
CB7489350
Molecular Formula:
C7H15Cl2N2O2P
Formula Weight:
261.09
MOL File:
3778-73-2.mol

Isophosphamide Properties

Melting point:
48°C
storage temp. 
2-8°C
form 
neat
CAS DataBase Reference
3778-73-2(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  T
Risk Statements  25-36
Safety Statements  26-45
RIDADR  3249
WGK Germany  3
RTECS  RP6050000
HazardClass  6.1(b)
PackingGroup  III
HS Code  29349990
Hazardous Substances Data 3778-73-2(Hazardous Substances Data)
Toxicity LD50 in rats (mg/kg): 160 i.p. (Arnold, 1973); also reported as 150 i.p. (Brock)
Symbol(GHS):
Signal word: Danger
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H301 Toxic if swalloed Acute toxicity,oral Category 3 Danger P264, P270, P301+P310, P321, P330,P405, P501
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning P264, P280, P305+P351+P338,P337+P313P
H340 May cause genetic defects Germ cell mutagenicity Category 1A, 1B Danger
H350 May cause cancer Carcinogenicity Category 1A, 1B Danger
H360 May damage fertility or the unborn child Reproductive toxicity Category 1A, 1B Danger
Precautionary statements:
P201 Obtain special instructions before use.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P308+P313 IF exposed or concerned: Get medical advice/attention.

Isophosphamide price More Price(8)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich I4909 Ifosfamide ≥98% 3778-73-2 1g $184 2018-11-20 Buy
Sigma-Aldrich 1336205 Ifosfamide United States Pharmacopeia (USP) Reference Standard 3778-73-2 500mg $352.8 2018-11-20 Buy
Cayman Chemical 17562 Ifosfamide ≥98% 3778-73-2 50mg $25 2018-11-13 Buy
Cayman Chemical 17562 Ifosfamide ≥98% 3778-73-2 1g $150 2018-11-13 Buy
Sigma-Aldrich I0060000 Ifosfamide European Pharmacopoeia (EP) Reference Standard 3778-73-2 i0060000 $179 2018-11-23 Buy

Isophosphamide Chemical Properties,Uses,Production

History

H. Arnold at ASTA Inc. developed a new drug ifosfamide in 1967 by modifying cyclophosphamide. This drug, which is a structural isomer of cyclophosphamide, was not only effective for leukemia treatment but also showed a superior effi cacy compared to cyclophosphamide in solid tumor such as testicular cancer and sarcoma. Therefore, it obtained FDA approval as a therapeutic agent for testicular cancer and sarcoma in 1988. In 1981, while searching for approaches to lower the toxicity of ifosfamide, N. Brock et al. discovered that sodium-2-mercaptoethane sulfonate (mesna), which contains a thiol group, can convert acrolein into a non-toxic compound and thereby effectively prevent bladder toxicity (hemorrhagic cystitis). Since then, mesna has been used until today to clinically prevent the side effects of ifosfamide.

Cyclophosphamide isomer

Ifosfamide is a cyclophosphamide isomer, appearing as white crystalline or crystalline powder at room temperature. The difference with cyclophosphamide is the difference of the position of a chloroethyl. Itself is a latent drug and can take effect only after entering into the body to be activated in the liver. It is used for the treatment of bone and soft tissue sarcoma, non-small cell lung cancer, breast cancer, head and neck cancer, cervical cancer, esophageal cancer, the effect is better than cyclophosphamide.
Cyclophosphamide is the most commonly used alkylating agent antitumor drugs. After entering into the body, it is catalyzed by the liver microsomal enzyme to be decomposed for release of strong alkylation chloroethyl phosphate amide (or phosphamide nitrogen mustard) with cytotoxic effect on tumor cells. In addition, this product also has a significant immune function.
It is clinically used for the treatment of malignant lymphoma, multiple myeloma, leukemia, breast cancer, ovarian cancer, cervical cancer, prostate cancer, colon cancer, bronchial cancer and lung cancer with a certain effect. It can also be used for the treatment of rheumatoid arthritis, nephrotic syndrome in children and autoimmune diseases.

Instructions for ifosfamide (for injection)

Properties: This product is white crystalline or crystalline powder.
Drug categories: alkylating agents antitumor drugs
Pharmacology and Toxicology: This product has no anti-cancer activity in vitro, entering into the body to be hydrolyzed by the phosphorylase or phosphatase in the liver or tumor, becoming activating form of phosphoramide nitrogen mustard. Its mechanism of action can have cross-linking with DNA, causing inhibition of DNA synthesis and interfering with the function of RNA, belonging to cell cycle non-specific drugs. This product has broad anti-tumor spectrum with inhibitory effect on a variety of tumors.
Pharmacokinetics: it is subject to an intravenous infusion 3.8~5.0g/m2 according to the surface area with the plasma concentration being biphasic and terminal half-life of 15 hours. It is subject to an intravenous infusion of 1.6~2.4g/m2 based on the surface area with the plasma concentration exhibiting single Phase with a half-life of 7 hours. It can be degraded by the liver with only a few amounts of its active metabolites penetrating through the blood-brain barrier. Drugs discharged by the kidneys accounts for 70% to 80%; upon intravenous injection of 5.0g/m2 once according to the surface area, 61% is discharged in the form of prototype; upon intravenous injection of 1.2~2.4g/m2 once according to the surface area, only 12% to 18% is discharged in the form of prototype .
Indications: for testicular cancer, ovarian cancer, breast cancer, sarcoma, malignant lymphoma and lung cancer.
Dosage: single drug treatment: apply intravenous injection based on a body surface area of 1.2~2.5g/m2 each time with 5 days as a course of treatment. Combination treatment: apply intravenous injection at 1.2~2.0g/m2 each time based on body surface area with continuous 5 days as a course of treatment. Each course has a 3 to 4 weeks gap with 500 to 600 mg/m2.
Adverse reactions: (1) bone marrow suppression: Leukopenia is more common than thrombocytopenia with the lowest value occurring in 1 to 2 weeks after treatment and will usually recover in 2 to 3 weeks after recovery. It has effect on the liver function. Gastrointestinal reactions: including loss of appetite, nausea and vomiting. It will generally disappear after drug withdrawal in 1 to 3 days.
(2) Urinary tract reaction: can cause hemorrhagic cystitis, manifested as dysuria, urinary frequency and dysuria. This may occur within a few hours or weeks after administration, usually disappear within a few days after stopping the drug.
 (3) Central nervous system toxicity: dose-related, usually manifested as anxiety, confusion, hallucinations and lack of strengthen. In rare cases, there will be syncope, epileptic seizures and even coma.
(4) Rarely: transient asymptomatic liver and kidney dysfunction; upon high dose of medication, there may be metabolic acidosis due to renal toxicity. It is rarely seen of heart and lung toxicity.
(5) Other reactions include hair loss, nausea and vomiting. It can occur of phlebitis in the injection site.
(6) Long-term medication can produce immune suppression, pituitary dysfunction, infertility and secondary tumors.

Contraindications and Precautions

Contraindications
Patients of severe bone marrow suppression being allergic to the products and pregnancy or lactating women should be disabled.
Precautions
(1) The metabolic product of this product has urinary tract irritation. During application, it should be encouraged of patients to drink more water with high-dose application should be hydration, diuretic while giving the protective agent of urinary tract, Mesna.
(2) Patients of hypoalbuminemia, liver and kidney dysfunction, bone marrow suppression and women of childbearing age should use with caution.
(3) This product is unstable aqueous solution, shall be freshly prepared before use.
(4) During treatment, it should be regularly monitored of the white blood cells, platelets and carried out of liver and kidney function determination. Administration of pregnant women and lactating women has mutagenic, teratogenic effects, being able to cause fetal death or congenital malformations. Therefore, pregnant women should be disabled. This product can be discharged in the milk and should be stopped of breast-feeding in the beginning of the medication.

Medicine interactions

(1) Patients previously used cisplatin may get aggravated ifosfamide inhibition of bone marrow, neurotoxicity and renal toxicity.
(2) Simultaneous administration of anticoagulant drugs may lead to bleeding risk.
(3) Simultaneous administration of hypoglycemic agents can enhance hypoglycemic effect.
(4) Upon simultaneous administration with other cytotoxic drugs, it should be considered of appropriate reduction.
Storage: shading, closed, stored at below 30 ℃.
Packing: (1) 0.5g (2) 1.0g

Uses

1.  Anti-cancer drugs;
2.  For the treatment of malignant lymphoma, lung cancer, breast cancer, esophageal cancer, bone and soft tissue sarcoma, non-small cell lung cancer, head and neck cancer, cervical cancer

The domestic market situation

Because the ifosfamide products have much higher price than cyclophosphamide products, so only upon no return in the production of cyclophosphamide, the several major domestic companies of production of cyclophosphamide have changed production lines for production of ifosfamide.
Ifosfamide is cyclophosphamide derivatives, having in vitro activity, but administration in vivo can have a significant inhibitory effect on a variety of metastatic tumors, being able to treat bone and soft tissue sarcoma, non-small cell lung cancer, breast cancer, head and neck cancer, cervical cancer and esophageal cancer. In 1993, it is officially available in the country.
It is understood that the current market price of ifosfamide bulk drugs is more than 8000 yuan/kg. The preparation class drugs, after 18 times of price decreases, can decrease from the original 216 yuan down to 180 yuan each one. The corporate profit margin has decreased, but is still considerable compared to cyclophosphamide.
In the last year, in the rankings list of 42 anti-tumor drugs, ifosfamide ranked 13. In the 14 varieties of the world's leading sales of antineoplastic drugs of 2003, ifosfamide ranked 11 in a sale of 08 million US dollars. The market performance is still stable. According to the reflection of domestic enterprises, the annual demand of ifosfamide preparation is not large, so raw material supply and demand situation is relatively stable.
However, one of the largest manufacturers of anti-tumor drug, the Jiangsu Hengrui, after discontinuing the production line of cyclophosphamide, has also significantly expanded the production of ifosfamide. It is understood that at this year, a securities company's research report on the Hengrui has shown that, ifosfamide needle has obtained an increased production of 650,000 with the new output value of 78 million yuan. Ifosfamide and other anti-cancer drugs have been simultaneously listed important nurturing products. Therefore, it can be expected that, in the circumstances of downturn of cyclophosphamide market, companies have converted to ifosfamide with the latter's market potentially getting a larger growth.
The reason why the latter has been able to get the favor of enterprises is mainly due to the price. Although the production of ifosfamide cyclophosphamide than the process is much more complex and costly, but the market price of 180 yuan/branch can still make the enterprise more profitable, while the production of cyclophosphamide is a high cost with zero return.

Chemical Properties

Crystalline Solid

Uses

antibacterial

Uses

A cytostatic agent, related structurally to cyclophosphamide

Definition

ChEBI: The simplest member of the class of ifosfamides that is 1,3,2-oxazaphosphinan-2-amine 2-oxide substituted by 2-chloroethyl groups on both the nitrogen atoms respectively. It is a nitrogen mustard alkylating agent used in the treatment of advanced breast c ncer.

brand name

Ifex (Bristol-Myers Squibb).

Isophosphamide Preparation Products And Raw materials

Raw materials

Preparation Products


Isophosphamide Suppliers

Global( 274)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22049 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20786 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32651 55
PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2548 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 19990 58
J & K SCIENTIFIC LTD. 400-666-7788 +86-10-82848833
+86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96815 76
3B Pharmachem (Wuhan) International Co.,Ltd. 86-21-50328103 * 801、802、803、804 Mobile:18930552037
86-21-50328109 3bsc@sina.com China 15926 69
Arden pharmaceutical &chemical Co., Ltd +86-(0)533-3595900 13793319233
+86-(0)533-3595900 info@chems.com.cn China 670 61
Chembest Research Laboratories Limited +86(0)21-20908456
+86(0)21-58180499 sales@biochembest.com; market@biochembest.com China 6054 61
Pure Chemistry Scientific Inc. 001-857-928-2050 or 1-888-588-9418
001-617-206-9595 sales@chemreagents.com United States 9943 62

View Lastest Price from Isophosphamide manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-08-08 Isophosphamide
3778-73-2
US $1.00 / KG 1KG 98% 1tons career henan chemical co

Isophosphamide Spectrum


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