Tìm theo
Lomustine
Các tên gọi khác (12 ) :
  • 1-(2-Chloroethyl)-3-cyclohexyl-1-nitrosourea
  • 1-(2-Chloroethyl)-3-cyclohexylnitrosourea
  • Belustine
  • CCNU
  • Cecenu
  • CeeNU
  • Chloroethylcyclohexylnitrosourea
  • CINU
  • Cyclohexyl chloroethyl nitrosourea
  • Lomustina
  • Lomustinum
  • N-(2-Chloroethyl)-n'-cyclohexyl-N-nitrosourea
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
CAS: 13010-47-4
ATC: L01AD02
ĐG : Bristol-Myers Squibb Co. , http://www.bms.com
CTHH: C9H16ClN3O2
PTK: 233.695
An alkylating agent of value against both hematologic malignancies and solid tumors. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C9H16ClN3O2
Phân tử khối
233.695
Monoisotopic mass
233.093104478
InChI
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)
InChI Key
InChIKey=GQYIWUVLTXOXAJ-UHFFFAOYSA-N
IUPAC Name
3-(2-chloroethyl)-1-cyclohexyl-3-nitrosourea
Traditional IUPAC Name
lomustine
SMILES
ClCCN(N=O)C(=O)NC1CCCCC1
Độ tan chảy
88-90 °C
Độ hòa tan
111 mg/L
logP
2.83
logS
-2.5
pKa (strongest acidic)
13.3
pKa (Strongest Basic)
-5.3
PSA
61.77 Å2
Refractivity
58.65 m3·mol-1
Polarizability
23.61 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Lomustine is an alkylating agent of the nitrosourea type. Lomustine and its metabolites interferes with the function of DNA and RNA. It is cell cycle–phase nonspecific. Cancers form when some cells within the body multiply uncontrollably and abnormally. These cells then spread and destroy nearby tissues. Lomustine acts by slowing this process down. It kills cancer cells by damaging the DNA (the genetic material inside the cells) and stops them from dividing.
Cơ Chế Tác Dụng : An alkylating agent of value against both hematologic malignancies and solid tumors. [PubChem] 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.
Dược Động Học :
▧ Absorption :
Well and rapidly absorbed from the gastrointestinal tract.
▧ Protein binding :
50%
▧ Metabolism :
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.
Độc Tính : 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.
Chỉ Định : 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.
Tương Tác Thuốc :
  • Atomoxetine The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine
  • Bendamustine Increases toxicity through pharmacodynamic synergism. Additive myelosuppression.
  • Terbinafine Terbinafine may reduce the metabolism and clearance of Lomustine. Consider alternate therapy or monitor for therapeutic/adverse effects of Lomustine if Terbinafine is initiated, discontinued or dose changed.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Ceenu 10 mg capsule
    Giá bán buôn : USD >10.77
    Đơn vị tính : capsule
  • Biệt dược thương mại : Ceenu dose pack
    Giá bán buôn : USD >30.47
    Đơn vị tính : each
  • Biệt dược thương mại : CeeNU 300 mg capsule
    Giá bán buôn : USD >31.69
    Đơn vị tính : capsule
  • Biệt dược thương mại : Ceenu 40 mg capsule
    Giá bán buôn : USD >31.88
    Đơn vị tính : capsule
  • Biệt dược thương mại : Ceenu 100 mg capsule
    Giá bán buôn : USD >60.61
    Đơn vị tính : capsule
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Belustine
  • Công ty :
    Sản phẩm biệt dược : Cecenu
  • Công ty :
    Sản phẩm biệt dược : CeeNU
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01206
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3950
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506562
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00363
ChemSpider
http://www.chemspider.com/Chemical-Structure.3813.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0015-3030-20
PharmGKB
http://www.pharmgkb.org/drug/PA164749407
Wikipedia
http://en.wikipedia.org/wiki/Lomustine
RxList
http://www.rxlist.com/cgi/generic2/lomustine.htm
Drugs.com
http://www.drugs.com/cdi/lomustine-ccnu.html
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