Lomustine
- CAS No.
- 13010-47-4
- Chemical Name:
- Lomustine
- Synonyms
- cinu;CCNU;ceenu;rb1509;cecenu;sri2200;nsc79037;icig1109;Lomustin;belustine
- CBNumber:
- CB5123021
- Molecular Formula:
- C9H16ClN3O2
- Molecular Weight:
- 233.7
- MOL File:
- 13010-47-4.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/7/2 8:55:09
| Melting point | 88-90 |
|---|---|
| Boiling point | 63.6°C (rough estimate) |
| Density | 1.3840 (rough estimate) |
| refractive index | 1.5790 (estimate) |
| storage temp. | 2-8°C |
| solubility | Practically insoluble in water, freely soluble in acetone and in methylene chloride, soluble in ethanol (96 per cent). |
| pka | 10.88±0.20(Predicted) |
| form | Solid |
| color | Light orange to Yellow to Green |
| Merck | 14,5564 |
| InChIKey | GQYIWUVLTXOXAJ-UHFFFAOYSA-N |
| CAS DataBase Reference | 13010-47-4(CAS DataBase Reference) |
| IARC | 2A (Vol. 26, Sup 7) 1987 |
| EPA Substance Registry System | 1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea (13010-47-4) |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |   GHS06,GHS08 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H301-H350 | |||||||||
| Precautionary statements | P201-P280-P301+P330+P331+P310-P308+P313 | |||||||||
| Hazard Codes | T | |||||||||
| Risk Statements | 45-25 | |||||||||
| Safety Statements | 53-45 | |||||||||
| RIDADR | 3249 | |||||||||
| WGK Germany | 3 | |||||||||
| RTECS | YS4900000 | |||||||||
| HazardClass | 6.1(a) | |||||||||
| PackingGroup | II | |||||||||
| HS Code | 29299090 | |||||||||
| Toxicity | LD50 in male mice (mg/kg): 51 orally; 56 i.p.; 61 s.c. (Thompson, Larson) | |||||||||
| NFPA 704 |
|
Lomustine price More Price(4)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich(India) | PHR3029 | Lomustine pharmaceutical secondary standard, certified reference material | 13010-47-4 | 500MG | ₹19614.9 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | L5918 | Lomustine ≥98% | 13010-47-4 | 100MG | ₹9028.05 | 2022-06-14 | Buy |
| TCI Chemicals (India) | L0251 | Lomustine | 13010-47-4 | 50MG | ₹3700 | 2022-05-26 | Buy |
| TCI Chemicals (India) | L0251 | Lomustine | 13010-47-4 | 200MG | ₹6700 | 2022-05-26 | Buy |
Lomustine Chemical Properties,Uses,Production
Chemical Properties
Lomustine is a pale yellow powder.
Uses
CCNU is an oral anticancer drug that was approved by the U.S. Food and Drug Administration in 1976 for marketing, as lomustine (FDA 2009a). CCNU is used alone or in combination with other antineoplastic agents, including procarbazine and vincristine, etoposide and prednimustine, and other combinations (IARC 1981, HSDB 2009). It is used primarily in the treatment of Hodgkin’s disease and brain tumors, but it has also been used to treat other cancer, includ-ing lung cancer, non-Hodgkin’s lymphoma, malignant melanoma, breast cancer, kidney cancer, and cancer of the gastrointestinal tract (MedlinePlus 2009). It has also been applied to the skin to treat mycosis fungoides and psoriasis.
Definition
ChEBI: An N-nitrosourea that is urea in which one of the nitrogens is substituted by a 2-chloroethyl group and by a nitroso group, while the other nitrogen is substituted by a cyclohexyl group. An alkylating antineoplastic agent, it is used in he treatment of brain tumours, lung cancer, malignant melanoma and other solid tumours.
General Description
Lomustine is available in 10-, 40-, and 100-mg capsules fororal administration in the treatment of primary and metastaticbrain cancers and Hodgkin’s lymphoma. This lipophilicagent is well absorbed, widely distributed, and crosses theblood-brain barrier. Lomustine undergoes extensive hepaticmetabolism, which is mediated by CYP3A4 to give severalhydroxylated metabolites, which arise as a result of oxidationof the cyclohexyl ring. Several of these are more activethan the parent compound. Denitrosation and dechlorinationhave also been demonstrated to occur for lomustine as well.The intact drug was not found in plasma when the agent wasadministered orally. Elimination occurs primarily in theurine with an elimination half-life of 16 to 72 hours.Myelosuppression is dose limiting and presents in a mannersimilar to that seen with carmustine. Other toxicities includenausea, vomiting, anorexia, impotence, sterility, amenorrhea,and infertility. Pulmonary and renal toxicity are rarelyseen during standard-dose therapy but increase during highdosetherapy.
Mechanism of action
Like other nitrosoureas, lomustine acts as a DNA-alkylating agent, and it also inhibits various key enzymatic reactions by carbamoylating proteins.
Safety Profile
Confirmed carcinogen with experimental carcinogenic and tumorigenic data. Poison by ingestion, intraperitoneal, subcutaneous, intravenous, and possibly other routes. Human systemic effects by ingestion: anorexia, nausea or vomiting, leukopenia (decrease in the white blood cell count), and thrombocytopenia (decrease in the number of blood platelets). Experimental teratogenic and reproductive effects. Human mutation data reported. When heated to decomposition it emits very toxic fumes of Cland NOx. See also NNITROSO COMPOUNDS.
Potential Exposure
A potential danger to those involved in the manufacture, administration or consumption of this antineoplastic (anti-cancer) agent
Drug interactions
Potentially hazardous interactions with other drugs
Antipsychotics: avoid concomitant use with
clozapine (increased risk of agranulocytosis).
Carcinogenicity
1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU) is reasonably anticipated to be a human carcinogen based on sufficient evidence of carcinogenicity from studies in experimental animals.
Metabolism
After oral application of radioactive marked lomustine approximately 15–30% of the measured radioactivity in the plasma can be detected in the cerebrospinal fluid. Lomustine is rapidly metabolised through hepatic microsomal enzymes and the metabolites are excreted mainly via the kidneys. About half a dose is excreted as metabolites in the urine within 24 hours and about 75% is excreted within 4 days. In addition, 10% is excreted as CO2 and<5% excreted in the faeces. Lomustine cannot be detected in its active form in the urine at any time.
Shipping
UN2811 Toxic solids, organic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials, Technical Name Required. UN3249 Medicine, solid, toxic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials
Waste Disposal
It is inappropriate and possibly dangerous to the environment to dispose of expired or waste drugs and pharmaceuticals by flushing them down the toilet or discarding them to the trash. Household quantities of expired or waste pharmaceuticals may be mixed with wet cat litter or coffee grounds, double-bagged in plastic, discard in trash. Larger quantities shall carefully take into consideration applicable DEA, EPA, and FDA regulations. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.
Lomustine Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Acura Life Sciences | +917780672646 | Hyderabad, India | 37 | 58 | Inquiry |
| RANI LIFE SCIENCES PVT LTD | +91-8008797507 +91-8008797507 | Hyderabad, India | 37 | 58 | Inquiry |
| Dr. Reddy's Laboratories Ltd | +91-4049002900 +91-4049002900 | Hyderabad, India | 165 | 58 | Inquiry |
| Basil Drugs AND Pharmaceuticals Pvt Ltd | +91-2249700250 +91-9619320820 | Mumbai, India | 108 | 58 | Inquiry |
| Euroasia Trans Continental | +91 22 56349035-36 | New Delhi, India | 519 | 47 | Inquiry |
| Shivam Pharma Chemicals | 91-22-26403900 | Maharashtra, India | 656 | 58 | Inquiry |
| Clearsynth Labs | 91-22-45045900 | Maharashtra, India | 3889 | 58 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| TCI Chemicals (India) Pvt. Ltd. | 1800 425 7889 | New Delhi, India | 6778 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |