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Details

Stereochemistry ACHIRAL
Molecular Formula Ga
Molecular Weight 69.7231
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 3

SHOW SMILES / InChI
Structure of GALLIUM CATION

SMILES

[Ga+3]

InChI

InChIKey=CKHJYUSOUQDYEN-UHFFFAOYSA-N
InChI=1S/Ga/q+3

HIDE SMILES / InChI
Gallium nitrate (brand name Ganite) is a drug that is used to treat hyper-calcemia, or too much calcium in the blood. Ganite exerts a hypocalcemic effect by inhibiting calcium resorption from bone, possibly by reducing increased bone turnover. It was shown, that gallium favorably altered the mineral properties to enhance hydroxyapatite crystallization and reduced mineral solubility. The drug also acted on the cellular components of bone to reduce bone resorption by decreasing acid secretion by osteoclasts. Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness. Gallium nitrate inhibits the growth of various lymphoma cell lines in vitro and exhibits antitumor activity in patients with lymphoma. Gallium 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. In phase II of clinical 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.

CNS Activity

Curator's Comment:: gallium nitrate crosses the blood-brain barrier which will allow treatment of the central nervous system lymphoma often seen in patients with AIDS-associated lymphoma

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
Effects of gallium nitrate on calcium transients in UMR-106 rat osteoblastic osteosarcoma cells.
1992
Management of acute hypercalcemia.
1992 Apr 30
Long-term effects of gallium nitrate in patients with Paget's disease of bone.
1992 Oct
Non-iron metalloporphyrins: potent antibacterial compounds that exploit haem/Hb uptake systems of pathogenic bacteria.
1999 Jan
Effects of trace metal compounds on HIV-1 reverse transcriptase: an in vitro study.
1999 May
Role for an essential tyrosine in peptide amidation.
2006 Jul 28
Gallium nitrate is efficacious in murine models of tuberculosis and inhibits key bacterial Fe-dependent enzymes.
2013 Dec
Serum and tissue concentrations of gallium after oral administration of gallium nitrate and gallium maltolate to neonatal calves.
2016 Feb
Patents

Sample Use Guides

The usual recommended dose of Ganite (Gallium nitrate injection) is 200 mg per square meter of body surface area (200 mg/m2) daily for 5 consecutive days. In patients with mild hypercalcemia and few symptoms, a lower dosage of 100 mg/m2/day for 5 days may be considered. If serum calcium levels are lowered into the normal range in less than 5 days, treatment may be discontinued early. The daily dose must be administered as an intravenous infusion over 24 hours. Controlled studies have not been undertaken to evaluate the safety and effectiveness of retreatment with gallium nitrate. When Ganite is added to either 0.9% Sodium Chloride Injection USP or 5% Dextrose Injection USP, it is stable for 48 hours at room temperature (15°C to 30°C) or for 7 days if stored under refrigeration (2°C to 8°C). Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit.
Route of Administration: Intravenous
In Vitro Use Guide
Because bladder cancer has many transferrin (Tf) receptors and gallium has been reported to bind avidly with Tf receptors, gallium cytotoxicity and the possibility of intravesical instillation therapy with gallium nitrate were studied in vitro. The bladder cancer cell lines J82, 639V, VMCuB1, SCaBER, and 5637 were used. The amount of Tf receptor was checked by a rosette assay. As a cytotoxicity assay, two experimental models were tested using two or 72 hours of exposure to gallium solution. For 72 hours of exposure at gallium concentrations above 250 mumol/L, the inhibitory effect was a function of gallium concentration, and 100% cytotoxicity occurred at 2 mmol/L. At lower concentrations of gallium, the effect was related to the amount of Tf and the level of Tf receptor expression of the cells. With two hours of exposure, which was assumed to be a model of intravesical therapy, the inhibitory effect increased in proportion to gallium concentration and the frequency of treatment. Twenty mmol/L gallium effectively inhibited the growth in two hours of exposure.
Name Type Language
GALLIUM CATION
Common Name English
GALLIUM (GA3+)
Common Name English
GALLIUM(III) CATION
Common Name English
GALLIUM(3+) CATION
Common Name English
GALLIUM, ION (GA3+)
Common Name English
GA3+
Common Name English
GALLIUM ION(3+)
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C597
Created by admin on Sat Jun 26 14:58:47 UTC 2021 , Edited by admin on Sat Jun 26 14:58:47 UTC 2021
Code System Code Type Description
EPA CompTox
22537-33-3
Created by admin on Sat Jun 26 14:58:47 UTC 2021 , Edited by admin on Sat Jun 26 14:58:47 UTC 2021
PRIMARY
RXCUI
1546282
Created by admin on Sat Jun 26 14:58:47 UTC 2021 , Edited by admin on Sat Jun 26 14:58:47 UTC 2021
PRIMARY RxNorm
NCI_THESAURUS
C76713
Created by admin on Sat Jun 26 14:58:47 UTC 2021 , Edited by admin on Sat Jun 26 14:58:47 UTC 2021
PRIMARY
FDA UNII
F7K5MP217W
Created by admin on Sat Jun 26 14:58:47 UTC 2021 , Edited by admin on Sat Jun 26 14:58:47 UTC 2021
PRIMARY
CAS
22537-33-3
Created by admin on Sat Jun 26 14:58:47 UTC 2021 , Edited by admin on Sat Jun 26 14:58:47 UTC 2021
PRIMARY
DRUG BANK
DB14524
Created by admin on Sat Jun 26 14:58:47 UTC 2021 , Edited by admin on Sat Jun 26 14:58:47 UTC 2021
PRIMARY
PUBCHEM
105145
Created by admin on Sat Jun 26 14:58:47 UTC 2021 , Edited by admin on Sat Jun 26 14:58:47 UTC 2021
PRIMARY