TABLE 2.

Potential pharmacological targets and related inhibitors targeting fatty acid synthesis.

Drug target	Notable inhibitors	Inhibitor description	IC50	Development status	Related diseases	Chemical st8ructure	References
SLC25A1 (CIC)	CTPI-2	—	3.5 μM	Preclinical Stage	Steatosis, Obesity		Tan et al. (2020)
SLC25A1 (CIC)	BTA	First-generation inhibitor	—	Preclinical Stage	Solid cancer		Catalina-Rodriguez et al. (2012)
ACLY	Bempedoic acid	An prodrug; Converted to an active drug in liver	29 uM	FDA approved	Hypercholesterolemia, Mixed dyslipidemia, Statin intolerance		Feng et al. (2020); Masana Marin and Plana Gil, (2021); Ray et al. (2019)
ACLY	Hydroxycitric acid	Natural product from Garcinia	—	Phase 4	Obesity, Diabetes		Jena et al. (2002)
ACLY	SB-204990	—	—	Preclinical Stage	Hypolipidaemic		Feng et al. (2020); Pearce et al. (1998)
ACLY	NDI-091143	High-affinity	2.1 nM	Preclinical Stage	Thyroid cancer		Huang et al. (2022); Wei et al. (2019)
ACC	ND-630 (Firsocostat)	Reversible, highly specific	—	Phase 1	Hepatic Steatosis; Obesity		Alkhouri et al. (2020)
ACC	TOFA	Allosteric inhibitor	—	Preclinical stage	Ovarian cancer; Prostate cancer		Guseva et al. (2011); Li et al. (2013); Wang et al. (2009)
ACC	PF-05221304	Liver-specific	—	Phase 2	NASH		Ross et al. (2020)
ACC1	soraphen-A	—	—	Preclinical stage	Prostate cancer; High-Fat Diet-induced Insulin Resistance, Hepatic Steatosis		Beckers et al. (2007)
FASN	Cerulenin	Natural inhibitor from Cephalosporium caeruleus	—	Preclinical Stage	Hepatic Steatosis; Solid cancer		Currie et al. (2013); Menendez and Lupu, (2007)
FASN	C75	Synthetic analog of cerulenin	35 μM	Preclinical Stage	Prostate cancer		Shimokawa et al. (2002); Thupari et al. (2002)
FASN	EGCG	An phenolic antioxidant from plants such as green tea	—	Phase 2	A wild range of cancers		Humbert et al. (2021); Khan et al. (2006)
FASN	Orlistat	The saturated derivative of lipstatin	—	Phase 3	Obesity		Pemble et al. (2007)
FASN	TVB-2640 Denifanstat	Reversible	0.052 μM	Phase 3	NAFLD; Solid Malignant Tumors		Loomba et al. (2021)
FASN	IPI-9119	Selective and Irreversible	0.3 nM	Preclinical Stage	Castration-resistant prostate cancer		Zadra et al. (2019)
FASN	TVB3664	Reversible	18 nM	Preclinical Stage	Colorectal cancer		Wang et al. (2022a)
SCD1	A939572	Synthetic Inhibitor	37 nM	Preclinical Stage	Renal cell carcinoma		Leung and Kim, (2013); von Roemeling et al. (2013)
SCD1	MK-8245	Liver-selective inhibitor	1 nM	Phase1 clinical trials (NCT00790556) for T2D	Diabetes and Dyslipidemia		Oballa et al. (2011)
SCD1	CAY10566	—	26 nM	Preclinical Stage	Breast cancer, Lung cancer, Colorectal cancer		Liu et al. (2007)
DGAT1	AZD-7687	Selective	80 nM	Phase1	Type 2 Diabetes, Obesity		Morentin Gutierrez et al. (2019)
DGAT1	AZD3988	—	6 nM	Preclinical stage	Type 2 Diabetes, Obesity		McCoull et al. (2012)
DGAT1	PF-04620110	selective	19 nM	Phase1	Type 2 Diabetes, Obesity		Dow et al. (2011), Lee et al. (2013)
DGAT1	A922500	selective	9 nM	Preclinical stage	hyperlipidemia		Cheng et al. (2020), King et al. (2010)
DGAT2	PF-06424439	selective	14 nM	Preclinical stage	hyperlipidemia		Futatsugi et al. (2015)
DGAT2	PF-06865571 (Ervogastat)	well-tolerated	—	Phase1	NASH, NAFLD		Calle et al. (2021)
DGAT2	JNJ DGAT2-A	selective	—	Preclinical stage	Type 2 Diabetes, Solid cancer		Irshad et al. (2017)