Tìm theo
Gallium nitrate
Thuốc Gốc
Small Molecule
CAS: 13494-90-1
CTHH: GaN3O9
PTK: 255.738
Gallium nitrate is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. This condition may occur when individuals develop various types of cancer. Gallium nitrate is also known by the common brand name Ganite.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
GaN3O9
Phân tử khối
255.738
Monoisotopic mass
254.889034525
InChI
InChI=1S/Ga.3NO3/c;3*2-1(3)4/q+3;3*-1
InChI Key
InChIKey=CHPZKNULDCNCBW-UHFFFAOYSA-N
IUPAC Name
gallium(3+) ion tris(nitrooxidane)
Traditional IUPAC Name
gallium(3+) ion tris(nitrooxidane)
SMILES
[Ga+3].[O-][N+]([O-])=O.[O-][N+]([O-])=O.[O-][N+]([O-])=O
logP
0.028
pKa (strongest acidic)
-1.4
pKa (Strongest Basic)
-6.1
PSA
68.88 Å2
Refractivity
9.85 m3·mol-1
Polarizability
3.24 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
-1
Number of Rings
0
Bioavailability
1
Rule of Five
true
Dược Lực Học : Gallium nitrate exerts hypocalcemic effect by inhibiting calcium resorption from bone, possibly by stabilizing bone matrix, thereby reducing increased bone turnover. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. The mechanism(s) of cytotoxicity is (are) only partly understood but appears to involve a two-step process: (1) targeting of gallium to cells, and (2) acting on multiple, specific intracellular processes. Gallium shares certain chemical properties with iron; therefore, it binds avidly to the iron transport protein transferrin. Transferrin-gallium complexes preferentially target cells that express transferrin receptors on their surface. Expression of transferrin receptors is particularly high on lymphoma cells. Cellular uptake of the gallium-transferrin complex leads to inhibition of cellular proliferation primarily via disruption of iron transport and homeostasis and blockade of ribonucleotide reductase. Recent studies have shown that cellular uptake of gallium leads to activation of caspases and induction of apoptosis. In phase II trials in patients with relapsed or refractory lymphoma, the antitumor activity of gallium nitrate is similar to, or better than, that of other commonly used chemotherapeutic agents.
Cơ Chế Tác Dụng : Gallium nitrate is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. This condition may occur when individuals develop various types of cancer. Gallium nitrate is also known by the common brand name Ganite. Gallium nitrate is believed to exert a hypocalcemic effect by inhibiting calcium resorption from bone. Gallium nitrate localizes preferentially where bone resorption and remodeling is occurring, and inhibits osteoclast activity. Inhibition of resorption may occur via a reduction in increased bone turnover. It seems to enhance hydroxyapatite function, inhibit osteocalcin, and inhibit the vacuolar ATPase on the osteoclast ruffled membrane. All these aid in the reduction of bone resorption.
Dược Động Học :

▧ Route of Elimination :
Gallium nitrate is not metabolized either by the liver or the kidney and appears to be significantly excreted via the kidney.
▧ Half Life :
Alpha: 1 hour. Beta: 24 hours, but lengthens to 72 to 115 hours with prolonged intravenous infusion.
▧ Clearance :
* 0.15 L/hr/kg [cancer patients receiving daily infusion of gallium nitrate at a dose of 200 mg/m2 for 5 or 7 days]
Chỉ Định : For the treatment of hypercalcemia. Also intended for the treatment of non-hodgkin's lymphoma.
Tương Tác Thuốc :
  • Vancomycin Additive nephrotoxic effects may occur. Avoid concomitant therapy.
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Genta inc.
    Sản phẩm biệt dược : Ganite
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB05260
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=61635
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508923
ChemSpider
http://www.chemspider.com/Chemical-Structure.55543.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/66657-301-05
PharmGKB
http://www.pharmgkb.org/drug/PA164781198
Drugs.com
http://www.drugs.com/cdi/gallium.html
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