Tìm theo
Idarubicin
Các tên gọi khác (7 ) :
  • (1S,3S)-3-Acetyl-3,5,12-trihydroxy-6,11-dioxo-1,2,3,4,6,11-hexahydronaphthacen-1-yl 3-amino-2,3,6-trideoxy-alpha-L-lyxo-hexopyranoside
  • 4-Demethoxydaunomycin
  • 4-Demethoxydaunorubicin
  • 5,12-Naphthacenedione, 9-acetyl-7-((3-amino-2,3,6-trideoxy-alpha-L-lyxo-hexopyranosyl)oxy)-7,8,9,10-tetrahydro-6,9,11-trihydroxy-, (7S-cis)-
  • Idarubicina
  • Idarubicine
  • Idarubicinum
antibiotics antineoplastic, antibiotics
Thuốc Gốc
Small Molecule
CAS: 58957-92-9
ATC: L01DB06
ĐG : Bedford Labs , http://www.bedfordlabs.com
CTHH: C26H27NO9
PTK: 497.4939
An orally administered anthracycline antineoplastic. The compound has shown activity against breast cancer, lymphomas and leukemias, together with the potential for reduced cardiac toxicity. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C26H27NO9
Phân tử khối
497.4939
Monoisotopic mass
497.168581467
InChI
InChI=1S/C26H27NO9/c1-10-21(29)15(27)7-17(35-10)36-16-9-26(34,11(2)28)8-14-18(16)25(33)20-19(24(14)32)22(30)12-5-3-4-6-13(12)23(20)31/h3-6,10,15-17,21,29,32-34H,7-9,27H2,1-2H3/t10-,15-,16-,17-,21+,26-/m0/s1
InChI Key
InChIKey=XDXDZDZNSLXDNA-TZNDIEGXSA-N
IUPAC Name
(7S,9S)-9-acetyl-7-{[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy}-6,9,11-trihydroxy-5,7,8,9,10,12-hexahydrotetracene-5,12-dione
Traditional IUPAC Name
idarubicin
SMILES
C[C@@H]1O[C@H](C[C@H](N)[C@@H]1O)O[C@H]1C[C@@](O)(CC2=C1C(O)=C1C(=O)C3=CC=CC=C3C(=O)C1=C2O)C(C)=O
Độ hòa tan
7.72e-01 g/l
logP
0.2
logS
-2.8
pKa (strongest acidic)
9.55
pKa (Strongest Basic)
8.95
PSA
176.61 Å2
Refractivity
126.43 m3·mol-1
Polarizability
50.33 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
10
H Bond Donor Count
5
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Dược Lực Học : Idarubicin is an antineoplastic in the anthracycline class. General properties of drugs in this class include: interaction with DNA in a variety of different ways including intercalation (squeezing between the base pairs), DNA strand breakage and inhibition with the enzyme topoisomerase II. Most of these compounds have been isolated from natural sources and antibiotics. However, they lack the specificity of the antimicrobial antibiotics and thus produce significant toxicity. The anthracyclines are among the most important antitumor drugs available. Doxorubicin is widely used for the treatment of several solid tumors while daunorubicin and idarubicin are used exclusively for the treatment of leukemia. Idarubicin may also inhibit polymerase activity, affect regulation of gene expression, and produce free radical damage to DNA. Idarubicin possesses an antitumor effect against a wide spectrum of tumors, either grafted or spontaneous. The anthracyclines are cell cycle-nonspecific.
Cơ Chế Tác Dụng : An orally administered anthracycline antineoplastic. The compound has shown activity against breast cancer, lymphomas and leukemias, together with the potential for reduced cardiac toxicity. [PubChem] Idarubicin has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Idarubicin forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes.
Dược Động Học :

▧ Protein binding :
97%
▧ Route of Elimination :
The drug is eliminated predominately by biliary and to a lesser extent by renal excretion, mostly in the form of idarubicinol.
▧ Half Life :
22 hours
Chỉ Định : For the treatment of acute myeloid leukemia (AML) in adults. This includes French-American-British (FAB) classifications M1 through M7.
Tương Tác Thuốc :
  • Trastuzumab Trastuzumab may increase the cardiotoxicity of Idarubicin. Signs and symptoms of cardiac dysfunction should be monitored for frequently. Increased risk of heart failure. Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Liều Lượng & Cách Dùng : Powder, for solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Idamycin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01177
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=42890
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506973
ChemSpider
http://www.chemspider.com/Chemical-Structure.39117.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0013-2526-86
PharmGKB
http://www.pharmgkb.org/drug/PA449961
Wikipedia
http://en.wikipedia.org/wiki/Idarubicin
RxList
http://www.rxlist.com/cgi/generic2/idarubicin.htm
Drugs.com
http://www.drugs.com/cdi/idarubicin.html
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