Table 1. Pharmacological tools to manipulate FAO.

Compound	Effect on FAO	Target	Approved for human use
Trimetazidine	Inhibition	3-KAT inhibitor	Europe and Asia
Ranolazine	Inhibition	3-KAT inhibitor	Europe and United States
Etomoxir	Inhibition	CPT1 inhibitor	Tested in clinical trials; retired owing to hepatotoxicity
Perhexiline	Inhibition	CPT1 inhibitor	Australia and Asia
Oxfenicine	Inhibition	CPT1 inhibitor	No
4-bromocrotonic acid	Inhibition	Mitochondrial thiolase inhibitor	No
Fenofibrate	Activation	PPARα agonist	Yes
GW5011516	Activation	PPARδ agonist	In clinical trials
TOFA	Activation	ACC inhibitor	No
Metformin	Activation	ETC complex | inhibitor	Yes
Phenformin	Activation	ETC complex | inhibitor	Withdrawn owing to high incidence of lactic acidosis
AICAR	Activation	AMP mimetic	No
Palmitate and carnitine	Activation	PPAR activator and substrate for FAO	No

3-KAT, trimetazidine hydrochloride; ACC, acetyl CoA carboxylase; AICAR, 5-amino-1-β-D-ribofuranosyl-imidazole-4-carboxamide; CPT1, carnitine palmitoyltransferase 1; ETC, electron transport chain; FAO, fatty acid oxidation; PPAR, peroxisome proliferator-activated receptor; TOFA, 5-tetradecyloxy-2-furonic acid.