TABLE 4.

Potential pharmacological targets and inhibitors targeting FAO.

Drug target	Notable inhibitors	Inhibitor description	IC50	Development status	Related diseases	Chemical structure	References
ACSLl	Triacsin C	An natural inhibitor, from Streptomyces aureofaciens	6.3 uM	Preclinical stage	Lung cancer; Colon cancer; Stomach cancer; Brain cancer; Breast cancer		Mashima et al. (2005)
CPT1	Etomoxir	Irreversible; Malonyl-CoA mimetic	5–20 nM (rat liver)	Phase II clinical trial stopped due to hepatoxicity	Leukemia; Glioblastoma		Bristow, (2000); Divakaruni et al. (2018); Lopaschuk et al. (1988); O'Connor et al. (2018)
CPT1, CPT2	Perhexiline (Pexsig)	Inhibit CPT1; to a lesser extent, CPT2	77 μM (rat heart CPT1); 148 μM (CPT1A)	Used primarily in Australia and New Zealand Adverse effects: nausea, hypoglycemia, neuropathy, and hepatitis	Severe angina pectoris		Ashrafian et al. (2007); Ren et al. (2020)
CPT1	ST1326 (Teglicar)	Amino-Carnitine derivative; highly selective for CPT1A; Reversible	0.68 μM (CPT1A)	Discontinued - Phase-II for Type-2 diabetes	Diabetes; Neurodegenerative diseases including Huntington’s disease		Bertapelle et al. (2022); Conti et al. (2011)
CPT1	2-tetradecylglycidate (TDGA)	Glycidic acid analog; An oxirane carboxylate inhibitor	—	Preclinical Stage, (induce myocardial hypertrophy)	Diabetes		Obici et al. (2003); Schlaepfer and Joshi, (2020); Wolkowicz et al. (1999)
CACT	EN936 (SLC25A20-IN-21)	—	—	Preclinical Stage	—		Parker et al. (2017a); Parker et al. (2017b)
VLCAD	Avocadyne	—	—	Phase 1	Acute Myeloid Leukemia; Hyperglycemia		Tcheng et al. (2021a); Tcheng et al. (2022); Tcheng et al. (2021b)
TFPβ	Ranolazine	—	—	FDA approved (NDA #021526)	Chronic Angina		Samudio et al. (2010); Sekine et al. (2022)
TFP	Trimetazidine	—	75 nM	Phase 2 (NCT03273387)	Precapillary pulmonary hypertension; Muscle wasting (cachexia)		Gatta et al. (2017)