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Chemistry

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Also known as: Gallium nitrate, 13494-90-1, Gallium nitrate anhydrous, Gallium nitrate (anhydrous), Y2v2r4w9tq, Nitric acid, gallium salt (3:1)
Molecular Formula
GaN3O9
Molecular Weight
255.74  g/mol
InChI Key
CHPZKNULDCNCBW-UHFFFAOYSA-N
FDA UNII
Y2V2R4W9TQ

GALLIUM NITRATE
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 anhydrous is a Calcium Resorption Inhibitor. The physiologic effect of gallium nitrate anhydrous is by means of Bone Resorption Inhibition.
1 2D Structure

GALLIUM NITRATE

2 Identification
2.1 Computed Descriptors
2.1.1 IUPAC Name
gallium;trinitrate
2.1.2 InChI
InChI=1S/Ga.3NO3/c;3*2-1(3)4/q+3;3*-1
2.1.3 InChI Key
CHPZKNULDCNCBW-UHFFFAOYSA-N
2.1.4 Canonical SMILES
[N+](=O)([O-])[O-].[N+](=O)([O-])[O-].[N+](=O)([O-])[O-].[Ga+3]
2.2 Other Identifiers
2.2.1 UNII
Y2V2R4W9TQ
2.3 Synonyms
2.3.1 MeSH Synonyms

1. Gallium Nitrate

2. Gallium Nitrate Heptahydrate

3. Gallium Nitrate, 67ga-labeled

4. Ganite

5. Nsc 15200

2.3.2 Depositor-Supplied Synonyms

1. Gallium Nitrate

2. 13494-90-1

3. Gallium Nitrate Anhydrous

4. Gallium Nitrate (anhydrous)

5. Y2v2r4w9tq

6. Nitric Acid, Gallium Salt (3:1)

7. Gallium(iii) Nitrate Solution, Ga 9-10% W/w

8. Ccris 4493

9. Nitric Acid, Gallium(3+) Salt

10. Einecs 236-815-5

11. Unii-y2v2r4w9tq

12. Mfcd00011016

13. Galliumnitrate

14. Gallium Nitrate [mi]

15. Dtxsid0043923

16. Gallium Nitrate [who-dd]

17. Gallium Nitrate (ga(no3)3)

18. Nitric Acid, Gallium Salt, Anhydrate

19. Akos015902357

20. Db05260

21. Sr-01000944456

22. Sr-01000944456-1

23. Gallium (iii) Nitrate, Solution Ga 9-10% W/w, Aldrichcpr

2.4 Create Date
2005-06-24
3 Chemical and Physical Properties
Molecular Weight 255.74 g/mol
Molecular Formula GaN3O9
Hydrogen Bond Donor Count0
Hydrogen Bond Acceptor Count9
Rotatable Bond Count0
Exact Mass254.88903 g/mol
Monoisotopic Mass254.88903 g/mol
Topological Polar Surface Area189 Ų
Heavy Atom Count13
Formal Charge0
Complexity18.8
Isotope Atom Count0
Defined Atom Stereocenter Count0
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently Bonded Unit Count4
4 Drug and Medication Information
4.1 Drug Indication

For the treatment of hypercalcemia. Also intended for the treatment of non-hodgkin's lymphoma.


5 Pharmacology and Biochemistry
5.1 Pharmacology

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.


5.2 MeSH Pharmacological Classification

Calcium-Regulating Hormones and Agents

Hormones and molecules with calcium-regulating hormone-like actions that modulate OSTEOLYSIS and other extra-skeletal activities to maintain calcium homeostasis. (See all compounds classified as Calcium-Regulating Hormones and Agents.)


Antineoplastic Agents

Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)


5.3 FDA Pharmacological Classification
5.3.1 Active Moiety
GALLIUM NITRATE ANHYDROUS
5.3.2 FDA UNII
Y2V2R4W9TQ
5.3.3 Pharmacological Classes
Established Pharmacologic Class [EPC] - Calcium Resorption Inhibitor
5.4 Absorption, Distribution and Excretion

Route of Elimination

Gallium nitrate is not metabolized either by the liver or the kidney and appears to be significantly excreted via the kidney.


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]


5.5 Biological Half-Life

Alpha: 1 hour. Beta: 24 hours, but lengthens to 72 to 115 hours with prolonged intravenous infusion.


5.6 Mechanism of Action

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.


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