Resmetirom (MGL-3196) is a liver-targeted selective agonist for the thyroid hormone receptor-β (THR-β) designed to increase cholesterol uptake into the liver and increase its metabolism. Resmetirom (MGL-3196) was well-tolerated at all doses with no dose-related adverse events or liver enzyme, ECG or vital-sign changes. Resmetirom (MGL-3196) showed a beneficial effect on lipid parameters.
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Source | Atherosclerosis (2013). Figure 1. MGL-3196 |
| Method | i.v. | |
| Cell Lines | mice | |
| Concentrations | 0.25, 1, 2.5, 5, 10, 20, 50, 100 and 200 mg | |
| Incubation Time | 24-h | |
| Results | MGL-3196 appeared safe and was well-tolerated at all doses and no maximal tolerated dose was reached. Adverse events were mild, not dose-related or considered related to study drug. There were no effects on 24-h Holter heart rate, ECG intervals including QTcF (Fridericia’s correction), or blood pressure. |
| Molecular Weight | 435.22 |
| Formula | C17H12Cl2N6O4 |
| CAS Number | 920509-32-6 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Bo Shen, et al. Efficacy and safety of drugs for nonalcoholic steatohepatitis
[4] Suzanna L Attia, et al. Evolving Role for Pharmacotherapy in NAFLD/NASH
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