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Description
Curator's Comment: The description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/22385186 | https://clinicaltrials.gov/ct2/show/NCT00335075 | https://www.ncbi.nlm.nih.gov/pubmed/21698685 | https://clinicaltrials.gov/ct2/show/NCT00427570

Semustine is a methylated derivative of carmustine with potent antineoplastic activity. As an alkylating agent, semustine forms covalent linkages with nucleophilic centers in DNA, causing depurination, base-pair miscoding, strand scission, and DNA-DNA cross-linking, which may result in cytotoxicity. Semustine is primarily used to treat brain tumors, colorectal tumors, lymphomas, and stomach cancer.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: CHEMBL2311221
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
A phase 2 evaluation of 1-(2-chloroethyl)-3-(4- methylcyclohexyl)-1-nitrosourea (NSC 95441) in patients with advanced breast cancer.
1974 Jan
Chemotherapeutic effects of some alkylating derivatives of nitrosourea on the development of tumors transplacentally induced in rats by ENU.
1976 Jan 31
Enhancement by electron-affinic agents of the therapeutic effects of cytotoxic agents against the KHT tumor: structure-activity relationships.
1982 Mar-Apr
Comparative nephrotoxicity of 1-(2-chloroethyl)-3-(trans-4-methylcyclohexyl)-1-nitrosourea (MeCCNU) and chlorozotocin: functional-structural correlations in the Fischer 344 rat.
1986 Mar 15
Anticancer drug-induced kidney disorders.
2001 Jan
1-(2-Chloroethyl)-3-(4-methylcyclohexyl)-1-nitrosourea (MeCCNU).
2002
Randomized trial of adjuvant therapy in colon carcinoma: 10-year results of NSABP protocol C-01.
2004 Aug 4
Interstitial chemotherapy with biodegradable BCNU (Gliadel) wafers in the treatment of malignant gliomas.
2007 Oct
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.
2011 Jul 14
Patents

Patents

Sample Use Guides

Semustine orally once every 28 days at a dose of 150 mg/m2/day.
Route of Administration: Intravenous
In Vitro Use Guide
Cell lines BE and HT (HT-29), were used for activity evaluation. BE and HT cell cultures were treated with MMeCCNU (Semustine) 50, 100, or 200 mkM. For cell culture experiments, stock drug solutions were prepared immediately before use at a concentration of 12.38 mg/ml (0.05 M) in 95% ethanol. Appropriate dilutions of the stock solution were made so that 20 mkI of drug solution were added to cultures in all experiments. Addition of 20 mkl 95% ethanol had no effect on cell growth or DNA integrity in control cells. The experiments show that line BE is sensitive to MeCCNU treatment in tissue culture, which corresponds with its response in vivo. There is a differential response to 100 mkM MeCCNU between lines BE and HT. At this dose approximately 50% of the cells in the BE cultures were lost from the plate with remaining cells showing little or no proliferation capacity, while line HT showed only a slight initial inhibition of growth with little or no cell loss
Name Type Language
SEMUSTINE
HSDB   INN   MART.   USAN   WHO-DD  
USAN   INN  
Official Name English
UREA, N-(2-CHLOROETHYL)-N'-(4-METHYLCYCLOHEXYL)-N-NITROSO-
Common Name English
METHYL-CCNU
Code English
ICIG-1110
Code English
SEMUSTINE [MART.]
Common Name English
SEMUSTINE [IARC]
Common Name English
semustine [INN]
Common Name English
SEMUSTINE [HSDB]
Common Name English
Semustine [WHO-DD]
Common Name English
ICIG 1110
Code English
NSC-758471
Code English
1-(2-CHLOROETHYL)-3-(P-METHYLCYCLOHEXYL)-1-NITROSOUREA
Common Name English
SEMUSTINE [USAN]
Common Name English
METHYL LOMUSTINE
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C699
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WHO-VATC QL01AD03
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WHO-ATC L01AD03
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Code System Code Type Description
EVMPD
SUB10482MIG
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CHEBI
6863
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EPA CompTox
DTXSID8031603
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INN
3191
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HSDB
7760
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ChEMBL
CHEMBL12948
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NCI_THESAURUS
C827
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CAS
13909-09-6
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MESH
D012673
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PUBCHEM
5198
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FDA UNII
6YY7T1T567
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WIKIPEDIA
SEMUSTINE
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NSC
758471
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DRUG CENTRAL
4704
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DRUG BANK
DB13647
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All of the following components must be present:
Definition References