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Table 1—

Therapeutic agents targeting AGEs: human and animal data

Category of therapy: human studiesMost advanced stage of trials as relates to AGEsTrial resultsSafety concerns
Prevent AGE formation    
Therapeutic entity    
Aminoguanidine Human, phase III ↓nephropathy, ↓retinopathy ↑glomerulonephritis, ↓vitamin B6, ↓iNOS 
Benfotiamine Human, phase II ↓neuropathy None reported 
AR inhibitors (epalrestat, zopolrestat) Human, phase II ↓AGE levels, ↓neuropathy, ↑esophageal motility None reported 
AGE cross-link disrupter    
Therapeutic entity    
ALT-711 (alagebrium chloride) Human, phase III ↓arterial stiffness, ↓pulse pressure, breaks cross-links formed by AGEs, ↑diastolic heart function None reported 
Antihypertensive    
Therapeutic entity    
ARB Human, phase III ↓macrophages in carotid artery plaque ↓GFR, rare angioedema 
ACE inhibitor Human, phase II ↓RAGE levels ↓GFR, rare angioedema 
Dietary factors    
Therapeutic entity    
Low-AGE diet Human data, stage N/A ↓AGE levels, ↓C-reactive protein None reported 
Prevent AGE formation    
Therapeutic entity    
ALT-946 Animal (diabetic rats) ↓nephropathy better than aminoguanidine None reported 
LR-90 Animal (diabetic rats) ↓nephropathy, ↓oxidative stress ↑weight gain 
OPB 9195 Animal (diabetic rats) ↓stenosis after vessel injury, ↓nephropathy ↓ vitamin B6 
PARP inhibitors Animal (diabetic rats) ↓endothelial dysfunction, ↓diastolic dysfunction, ↓neuropathy None reported 
Pyridoxamine Animal (diabetic rats) ↓nephropathy, ↓cholesterol, ↓weight None reported 
AGE cross-link disrupter    
Therapeutic entity    
PTB Animal (diabetic rats) ↓AGEs None reported 
AGE binder    
Therapeutic entity    
Soluble RAGE Animal (diabetic mice) ↓stenosis after vessel injury, ↓neuropathy None reported 
Lysozyme Animal (diabetic and apolipoprotein E–null mice) ↓AGEs, ↓nephropathy, ↓atherosclerosis None reported 
Antioxidants    
Therapeutic entity    
Green tea Animal (diabetic rats) ↑AGEs, ↑AGE cross-links None reported 
Vitamins E and C Animal (diabetic rats) ↑AGEs, ↑AGE cross-links ↑CV morbidity from vitamin E >400 IU 
Oral hypoglycemic agents    
Therapeutic entity    
Metformin Animal (diabetic rats) ↓AGEs, ↓AGE cross-links Lactic acidosis 
Pioglitazone In vitro ↓AGEs, ↓AGE cross-links ↑hepatitis, ↑CHF if susceptible 
Category of therapy: human studiesMost advanced stage of trials as relates to AGEsTrial resultsSafety concerns
Prevent AGE formation    
Therapeutic entity    
Aminoguanidine Human, phase III ↓nephropathy, ↓retinopathy ↑glomerulonephritis, ↓vitamin B6, ↓iNOS 
Benfotiamine Human, phase II ↓neuropathy None reported 
AR inhibitors (epalrestat, zopolrestat) Human, phase II ↓AGE levels, ↓neuropathy, ↑esophageal motility None reported 
AGE cross-link disrupter    
Therapeutic entity    
ALT-711 (alagebrium chloride) Human, phase III ↓arterial stiffness, ↓pulse pressure, breaks cross-links formed by AGEs, ↑diastolic heart function None reported 
Antihypertensive    
Therapeutic entity    
ARB Human, phase III ↓macrophages in carotid artery plaque ↓GFR, rare angioedema 
ACE inhibitor Human, phase II ↓RAGE levels ↓GFR, rare angioedema 
Dietary factors    
Therapeutic entity    
Low-AGE diet Human data, stage N/A ↓AGE levels, ↓C-reactive protein None reported 
Prevent AGE formation    
Therapeutic entity    
ALT-946 Animal (diabetic rats) ↓nephropathy better than aminoguanidine None reported 
LR-90 Animal (diabetic rats) ↓nephropathy, ↓oxidative stress ↑weight gain 
OPB 9195 Animal (diabetic rats) ↓stenosis after vessel injury, ↓nephropathy ↓ vitamin B6 
PARP inhibitors Animal (diabetic rats) ↓endothelial dysfunction, ↓diastolic dysfunction, ↓neuropathy None reported 
Pyridoxamine Animal (diabetic rats) ↓nephropathy, ↓cholesterol, ↓weight None reported 
AGE cross-link disrupter    
Therapeutic entity    
PTB Animal (diabetic rats) ↓AGEs None reported 
AGE binder    
Therapeutic entity    
Soluble RAGE Animal (diabetic mice) ↓stenosis after vessel injury, ↓neuropathy None reported 
Lysozyme Animal (diabetic and apolipoprotein E–null mice) ↓AGEs, ↓nephropathy, ↓atherosclerosis None reported 
Antioxidants    
Therapeutic entity    
Green tea Animal (diabetic rats) ↑AGEs, ↑AGE cross-links None reported 
Vitamins E and C Animal (diabetic rats) ↑AGEs, ↑AGE cross-links ↑CV morbidity from vitamin E >400 IU 
Oral hypoglycemic agents    
Therapeutic entity    
Metformin Animal (diabetic rats) ↓AGEs, ↓AGE cross-links Lactic acidosis 
Pioglitazone In vitro ↓AGEs, ↓AGE cross-links ↑hepatitis, ↑CHF if susceptible 

AR, aldose reductase; CHF, congestive heart failure; CV, cardiovascular; GFR, glomerular filtration rate; iNOS, inducible nitric oxide synthase; PTB, N-phenacylthiazolium bromide; TZD, thiazolidinedione.

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