Lomustine

Structural formula
General
Non-proprietary name	Lomustine
other names	CCNU; 1- (2-chloroethyl) -3-cyclohexyl-1-nitrosourea;
Molecular formula	C 9 H 16 ClN 3 O 2
External identifiers / databases
EC number	235-859-2
ECHA InfoCard	100.032.585
PubChem	3950
DrugBank	DB01206
Wikidata	Q415378
Drug information
ATC code	L01 AD02
Drug class	Cytostatic
properties
Molar mass	233.70 g mol −1
Physical state	firmly
Melting point	90 ° C
solubility	soluble in chloroform, ethanol and acetone
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
H and P phrases	H: 301-350
	P: 201-301 + 310-308 + 313
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Lomustine , (synonyms: C hlorethyl- C yclohexyl- N itroso- U rea, abbreviated CCNU ) is a drug , more specifically, a cytostatic agent from the group of alkylating agents (nitrosoureas).

pharmacology

Mechanism of action

Like all alkylating agents, nitrosoureas such as carmustine or lomustine change the genetic material and make it illegible. The affected cells do not divide and die after a certain time. This has a particularly serious effect on rapidly dividing cells and thus on cancer cells. In addition, nitrosoureas have the special feature that they prevent many repair mechanisms for the DNA and thus greatly increase the carcinogenicity .

Lomustine crosses the blood-brain barrier and can therefore often be used successfully against brain tumors . Combinations with surgical removal and radiation are possible.

Side effects

It often comes to bone marrow damage, decreased platelet and leukocyte number, nausea , hair loss . With nitrosoureas, these side effects are delayed. Therefore, constant checks of the blood values and treatment breaks of approx. 6 weeks are necessary.
Kidney toxicity
The risk of cancer, especially leukemia and urinary bladder tumors, is increased especially with high cumulative doses .
Rarely a hardening of is lung connective tissue ( fibrosis ) or a non-bacterial pneumonia (pneumonitis) detectable. This often results in shortness of breath and a lack of oxygen.

Application in veterinary medicine

In cats, the active ingredient can be used in intermediate large cell gastrointestinal lymphoma . The effect is comparable to that of other chemotherapy protocols and the tolerance is good.

Trade names

Monopreparations

Cecenu (D), Ceenu (CH), and a generic (A)

Individual evidence

^ ^A ^b The Merck Index: An Encyclopedia of Chemicals, Drugs, and Biologicals , 14th Edition (Merck & Co., Inc.), Whitehouse Station, NJ, USA, 2006; P. 963, ISBN 978-0-911910-00-1 .

↑ ^a ^b Lomustine data sheet at Sigma-Aldrich , accessed on April 8, 2011 ( PDF ).

^ SE Rau, KE Burgess: A retrospective evaluation of lomustine (CeeNU) in 32 treatment naïve cats with intermediate to large cell gastrointestinal lymphoma (2006-2013). In: Veterinary and comparative oncology. Volume 15, number 3, September 2017, pp. 1019-1028, doi : 10.1111 / vco.12243 , PMID 27277825 .

This text is based in whole or in part on the entry methyl-lomustine in the Flexikon , a wiki of the DocCheck company . The takeover took place on June 29, 2005 under the then valid GNU license for free documentation .

[MERCK_Index-1] A ^b The Merck Index: An Encyclopedia of Chemicals, Drugs, and Biologicals , 14th Edition (Merck & Co., Inc.), Whitehouse Station, NJ, USA, 2006; P. 963, ISBN 978-0-911910-00-1 .