Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | 2C6H6O7.Ga.H |
| Molecular Weight | 450.946 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H+].[Ga+3].OC(=O)C(O)(CC([O-])=O)CC([O-])=O.OC(=O)C(O)(CC([O-])=O)CC([O-])=O
InChI
InChIKey=YILZORZCGMPVTF-UHFFFAOYSA-K
InChI=1S/2C6H8O7.Ga/c2*7-3(8)1-6(13,5(11)12)2-4(9)10;/h2*13H,1-2H2,(H,7,8)(H,9,10)(H,11,12);/q;;+3/p-3
| Molecular Formula | C6H6O7 |
| Molecular Weight | 190.1076 |
| Charge | -2 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | Ga |
| Molecular Weight | 69.723 |
| Charge | 3 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | H |
| Molecular Weight | 1.0079 |
| Charge | 1 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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 Nevertheless, ganite was withdrawn from sale, although the reasons was not the safety or effectiveness.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.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL4865 |
|||
Target ID: P01584 Gene ID: 3553.0 Gene Symbol: IL1B Target Organism: Homo sapiens (Human) |
|||
Target ID: CHEMBL2095215 |
|||
Target ID: CHEMBL2363055 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | GANITE Approved UseGanite is indicated for the treatment of clearly symptomatic cancer-related hypercalcemia that has not responded to adequate hydration. In general, patients with a serum calcium (corrected for albumin) < 12 mg/dL would not be expected to be symptomatic. Mild or asymptomatic hypercalcemia may be treated with conservative measures (i.e., saline hydration, with or without diuretics). In the treatment of cancer-related hypercalcemia, it is important first to establish adequate hydration, preferably with intravenous saline, in order to increase the renal excretion of calcium and correct dehydration caused by hypercalcemia. Launch Date1991 |
|||
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| 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 |
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
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.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 19:01:40 GMT 2023
by
admin
on
Sat Dec 16 19:01:40 GMT 2023
|
| Record UNII |
6ZNH95J8XB
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Systematic Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
6ZNH95J8XB
Created by
admin on Sat Dec 16 19:01:40 GMT 2023 , Edited by admin on Sat Dec 16 19:01:40 GMT 2023
|
PRIMARY | |||
|
146156601
Created by
admin on Sat Dec 16 19:01:40 GMT 2023 , Edited by admin on Sat Dec 16 19:01:40 GMT 2023
|
PRIMARY | |||
|
1192555-89-7
Created by
admin on Sat Dec 16 19:01:40 GMT 2023 , Edited by admin on Sat Dec 16 19:01:40 GMT 2023
|
PRIMARY | |||
|
100000182753
Created by
admin on Sat Dec 16 19:01:40 GMT 2023 , Edited by admin on Sat Dec 16 19:01:40 GMT 2023
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
PARENT -> SALT/SOLVATE |
|
||
|
PARENT -> SALT/SOLVATE |
|
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
ACTIVE MOIETY |
|