GalliuM Maltolate Chemical Properties

form 

Solid

color 

Off-white to light yellow

InChI

InChI=1S/3C6H4O5.Ga/c3*7-3-1-2-11-5(4(3)8)6(9)10;/h3*1-2,8H,(H,9,10);/q;;;+3/p-3

InChIKey

LRPKBZSTANNRLK-UHFFFAOYSA-K

SMILES

[Ga+3].O1C(C([O-])=O)=C(O)C(=O)C=C1.O1C(C([O-])=O)=C(O)C(=O)C=C1.O1C(C([O-])=O)=C(O)C(=O)C=C1

GalliuM Maltolate Usage And Synthesis

Description

Gallium maltolate (GaM) is a new orally administered compound that has the potential to fundamentally improve the lives of many of these patients by providing effective treatment without serious side effects. GaM is being developed as an orally active formulation of gallium, a drug already approved by the FDA in intravenous form (gallium nitrate for injection). Clinical and preclinical studies have repeatedly shown gallium to have efficacy against cancer, inflammatory disorders, infectious disease, and bone loss.

Biological Activity

Gallium maltolate is a ribonucleoside-diphosphate reductase inhibitor potentially for the treatment of prostate cancer.

Clinical Use

Gallium maltolate has been administered to healthy volunteers and to some late-stage cancer patients in Phase I clinical trials. It has been given at doses as high as 3,500 mg/day for multiple 28-day cycles, with no dose-limiting toxicity or serious drug-related adverse effects. The compound has shown high oral bioavailability with an elimination half-life of approximately 17 to 21 hours. Anecdotal efficacy has been observed in patients with lymphoma, end-stage liver cancer (hepatocellular carcinoma), metastatic prostate cancer, metastatic colon cancer, metastatic lung cancer, and metastatic breast cancer.

Structure and conformation

Gallium maltolate, tris(3-hydroxy-2-methyl-4-pyronato)gallium, is a coordination complex consisting of a gallium atom surrounded by three maltolate ligands. Gallium maltolate is electrically neutral and moderately soluble in both water and lipids. It is stable over a pH range of approximately 5 through 8, a relatively large interval for a metal-organic complex.