4755 Lomustine Lomustine is only found in individuals that have used or taken this drug. It is an alkylating agent of value against both hematologic malignancies and solid tumors. Lomustine is a highly lipophilic nitrosourea compound which undergoes hydrolysis in vivo to form reactive metabolites. These metabolites cause alkylation and cross-linking of DNA (at the O6 position of guanine-containing bases) and RNA, thus inducing cytotoxicity. Other biologic effects include inhibition of DNA synthesis and some cell cycle phase specificity. Nitrosureas generally lack cross-resistance with other alkylating agents. As lomustine is a nitrosurea, it may also inhibit several key processes such as carbamoylation and modification of cellular proteins. 13010-47-4 3950 C9H16ClN3O2 White powder. 88 - 90°C 111 mg/L Well and rapidly absorbed from the gastrointestinal tract. Lomustine is a highly lipophilic nitrosourea compound which undergoes hydrolysis in vivo to form reactive metabolites. These metabolites cause alkylation and cross-linking of DNA (at the O6 position of guanine-containing bases) and RNA, thus inducing cytotoxicity. Other biologic effects include inhibition of DNA synthesis and some cell cycle phase specificity. Nitrosureas generally lack cross-resistance with other alkylating agents. As lomustine is a nitrosurea, it may also inhibit several key processes such as carbamoylation and modification of cellular proteins. Hepatic. Rapid and complete, with active metabolites. Route of Elimination: Following oral administration of radioactive CeeNU at doses ranging from 30 mg/m2 to 100 mg/m2, about half of the radioactivity given was excreted in the urine in the form of degradation products within 24 hours. Half Life: Approximately 94 minutes, however the metabolites have a serum half-life of 16 to 48 hours. Oral, rat: LD₅₀ = 70 mg/kg. Pulmonary toxicity has been reported at cumulative doses usually greater than 1,100 mg/m2. There is one report of pulmonary toxicity at a cumulative dose of only 600 mg. The onset of toxicity has varied from 6 months after initiation of therapy, to as late as 15 years after. 2A, probably carcinogenic to humans. (L135) For the treatment of primary and metastatic brain tumors as a component of combination chemotherapy in addition to appropriate surgical and/or radiotherapeutic procedures. Also used in combination with other agents as secondary therapy for the treatment of refractory or relapsed Hodgkin's disease. 2014-09-11T02:05:33Z 2026-03-26T21:11:04Z http://en.wikipedia.org/wiki/Lomustine C07079 110898 DB01206 true ClCCN(N=O)C(=O)NC1CCCCC1 C9H16ClN3O2 InChI=1S/C9H16ClN3O2/c10-6-7-13(12-15)9(14)11-8-4-2-1-3-5-8/h8H,1-7H2,(H,11,14) GQYIWUVLTXOXAJ-UHFFFAOYSA-N 233.695 233.093104478 Exogenous Solid 2.83 HMDB15337 CHEMBL514 3813 CHEM003658 DTXSID2023222 NS00003479 3-(2-chloroethyl)-1-cyclohexyl-3-nitrosourea