Nitrosourea

Nitrosoureas are a group of chemical compounds derived as a base as derivatives of nitrosourea. Some nitrosoureas used in oncology as cytostatic agents for the treatment of various cancers.

Main Features

Nitrosoureas are among the alkylating agents. That is, they can change the DNA in the nucleus chemically so that the function of DNA is largely disturbed. The affected cells can not divide further and thus die (apoptosis). In addition, the nitrosoureas prevent the repair of damaged DNA.

Many nitrosoureas are able to overcome by their small molecular size and lipophilicity, the blood -brain barrier. This is in the treatment of CNS metastases and brain tumors is of great importance.

The nitrosoureas are myelotoxic, that is, they damage the bone marrow. This damage has a negative effect on blood formation, especially the platelets and leucocytes from. The platelet and white blood cell count decreases with a significant delay of about 4 to 6 weeks after initiation of therapy, from. For this reason, the distance between two cycles of treatment with nitrosoureas have to be longer than that of other cytostatic agents.

In addition, nausea and hair loss are the main side effects after administration of cytotoxic drugs. Some nitrosoureas are also kidney and lung toxicity.

The nitrosoureas are themselves carcinogenic, ie cancer. High-dose therapy may lead to bladder cancer may therefore.

The most important representatives

• Carmustine 1,3-bis ( 2-chloroethyl )-1 -nitrosourea
• Lomustine 1 - (2 -chloroethyl )-3 -cyclohexyl -1 -nitrosourea
• Semustine N-(2 - Chloroethyl )-N'- (4- methylcyclohexyl) -N -nitrosourea
• Nimustine 1 - [ (4- amino-2- methylpyrimidine -5-yl ) methyl] -3 - ( 2-chloroethyl )-3 -nitrosourea
• Streptozocin 2 -deoxy-2 -(3- methyl-3- nitroso- ureido )-D- glucopyranose
• Fotemustine 1 - (2 -chloroethyl ) -3 - (1- diethoxyphosphorylethyl )-1 -nitrosourea
• Chlorozotocin
• Ranimustine
• N -ethyl-N -nitrosourea ( ENU )
• N -methyl-N -nitrosourea