Jan 24, 2009

Vanadium treatment of type 2 diabetes: a view to the future

Journal of Inorganic Biochemistry
Katherine H ThompsonChris Orvig

Abstract

3-Hydroxy-2-methyl-4-pyrone and 2-ethyl-3-hydroxy-4-pyrone (maltol and ethyl maltol, respectively) have proven especially suitable as ligands for vanadyl ions, in potential insulin enhancing agents for diabetes mellitus. Both bis(maltolato)oxovanadium(IV) (BMOV), and the ethylmaltol analog, bis(ethylmaltolato)oxovanadium(IV) (BEOV), have the desired intermediate stability for pro-drug use, and have undergone extensive pre-clinical testing for safety and efficacy. Pharmacokinetic evaluation indicates a pattern of biodistribution consistent with fairly rapid dissociation and uptake, binding to serum transferrin for systemic circulation and transport to tissues, with preferential uptake in bone. These bis-ligand oxovanadium(IV) (VOL(2)) compounds have a clear advantage over inorganic vanadyl sulfate in terms of bioavailability and pharmaceutical efficacy. BEOV has now completed Phase I and has advanced to Phase II clinical trials. In the Phase I trial, a range of doses from 10 mg to 90 mg BEOV, given orally to non-diabetic volunteers, resulted in no adverse effects; all biochemical parameters remained within normal limits. In the Phase IIa trial, BEOV (AKP-020), 20 mg, daily for 28 days, per os, in seven type 2 diabetic subjects, ...Continue Reading

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Citations

Mentioned in this Paper

Glycated Hemoglobin TEST
Diabetes Mellitus, Non-Insulin-Dependent
Oral Glucose Tolerance Test
Maltol
Hemoglobin, Glycosylated
Fasting Blood Glucose Measurement
Serum Transferrin Measurement
Pyrones
Complex (molecular entity)
Organometallic Compounds

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