Table 4.
FAS inhibitors
| Compound (developer) | Potency in biochemical assays | Indication and/or preclinical effects | Clinical trial ID or refs |
|---|---|---|---|
| Clinical stage inhibitors | |||
| Orlistat | IC50: 100 nM | Obesity | Approved |
| TVB-2640 (Sagimet Biosciences, USA) | IC50 < 0.05 μM | NASH | NCT04906421 (in progress, phase II) |
| Lung carcinoma, breast cancer, astrocytoma, colon cancer | NCT03808558, NCT03179904, NCT03032484, NCT02980029 (in progress, phase I/II) | ||
| FT-4101 (Forma Therapeutics, USA) | IC50: 40 nM | NASH | NCT04004325 (terminated, phase I/II) |
| Preclinical stage inhibitors | |||
| BI-99179 (Boehringer Ingelheim Pharma GmbH & Co, Germany) | IC50: 79 nM | Inhibited cancer cell growth | 249 |
| Cerulenin | IC50: 4.5 μM | Reduced weight gain and inhibited cancer cell growth | 253,261 |
| C75 (Johns Hopkins Medical Institutions, USA) | IC50: 15.5 μM | Reduced body weight, hepatic steatosis and blood glucose, and inhibited cancer growth | 255,257 |
| Fasnall (Duke University School of Medicine, USA) | IC50: 3.71 μM | Inhibited cancer cell growth | 245 |
| GSK2194069 (GlaxoSmithKline, USA) | IC50: 7.7 nM | Inhibited cancer cell growth | 246 |
| IPI-9119 (Dana-Farber Cancer Institute, USA) | IC50: 0.3 nM | Inhibited cancer cell growth | 247 |
| MP-ML-24-N1 (University Hospital Tübingen, Germany) | IC50: 1.6 µM | Inhibited cancer cell growth | 246 |
| TVB-3166 (Sagimet Biosciences, USA) | IC50: 42 nM | Inhibited cancer cell growth | 250 |
FAS, fatty acid synthase; IC50, half-maximal inhibitory concentration; NASH, nonalcoholic steatohepatitis.