Repositioning Candidate Details

Candidate ID: R1099
Source ID: DB06784
Source Type: approved
Compound Type: small molecule
Compound Name: Gallium citrate Ga-67
Synonyms: Gallium (67 Ga) citrate; Gallium citrate Ga 67; Gallium citrate Ga-67; Gallium-67 Citrate
Molecular Formula: C6H5GaO7
SMILES: [67Ga+3].OC(CC([O-])=O)(CC([O-])=O)C([O-])=O
Structure:
DrugBank Description: Gallium citrate Ga 67 is the citrate salt of the radioisotope gallium Ga 67. Although the mechanism is unknown, gallium Ga 67 concentrates in lysosomes and is bound to a soluble intracellular protein in certain viable primary and metastatic tumors and focal sites of inflammation, allowing scintigraphic localization. Ga-67 scintigraphy (GS) cannot differentiate between tumor and acute inflammation.
CAS Number: 41183-64-6
Molecular Weight: 256.0279
DrugBank Indication: Gallium Citrate Ga 67 Injection may be useful to demonstrate the presence and extent of Hodgkin's disease, lymphoma, and bronchogenic carcinoma. Positive gallium Ga-67 uptake in the absence of prior symptoms warrants follow-up as an indication of a potential disease state. Gallium Citrate Ga 67 Injection may be useful as an aid in detecting some acute inflammatory lesions.
DrugBank Pharmacology: It has been reported in the scientific literature that following intravenous injection, the highest tissue concentration of gallium Ga-67 - other than tumors and sites of infection - is the renal cortex. After the first day, the maximum concentration shifts to bone and lymph nodes and after the first week, to liver and spleen. Gallium Ga-67 is excreted relatively slowly from the body. The average whole body retention is 65 percent after seven days, with 26 percent having been excreted in the urine and 9 percent in the stools.
DrugBank MoA: Gallium Citrate Ga 67, with no carrier added, has been found to concentrate in certain viable primary and metastatic tumors as well as focal sites of infection. The body generally handles Ga3+ as though it were ferric iron (Fe-III), and thus the free isotope ion is bound (and concentrates) in areas of inflammation, such as an infection site, and also areas of rapid cell division. Ga-67 binds to transferrin, leukocyte lactoferrin, bacterial siderophores, inflammatory proteins, and cell-membranes in neutrophils, both living and dead. Lactoferrin is contained within leukocytes. Ga-67 may bind to lactoferrin and be transported to sites of inflammation, or binds to lactoferrin released during bacterial phagocytosis at infection sites (and remains due to binding with macrophage receptors). Ga-67 also attaches to the siderophore molecules of bacteria themselves, and for this reason can be used in leukopenic patients with bacterial infection (here it attaches directly to bacterial proteins, and leukocytes are not needed). Uptake is thought to be associated with a range of tumour properties including transferring receptors, anaerobic tumor metabolism and tumor perfusion and vascular permeability.
Targets: --
Inclusion Criteria: Therapeutic strategy associated