We have a pipeline of novel, fast-follow PCCs (preclinical-candidate-compounds) for the treatment of pain, insomnia, influenza, cerebral apoplexy and others.

Highlights of Project DSC192

Registration Classification：First in Class

Mechanisms/Targets：Selective Thyroid Hormone Receptor β (THR-β) agonists

Dosage Form: Oral solid preparation Dosage

Highlights：

1、The target has been validated, the mechanism of THR β target is clear, and the drug efficacy has been clinically validated.

2、MGL-3196 (Resmetrirom) is the first oral small molecule innovative drug approved by the US Food and Drug Administration (FDA) in 40 years for the treatment of non-alcoholic steatohepatitis (NASH) with liver fibrosis.

3、Based on the results of structure-activity relationship analysis, a series of compounds with novel structures were designed with the support of AI (Artificial Intelligence) technology, and compound DSC192 was obtained through chemical synthesis.

4、Stability: Under normal temperature conditions, DSC192 exhibits strong stability in both proton and non-proton solvents.

5、Activity in vitro: DSC192 is a potent THR β agonist with better selectivity for THR α/β activation than MGL-3196.

6、Pharmacokinetics: Compared to MGL-3196, the peak concentration (C_max) and exposure of DSC192 after oral administration were significantly increased (approximately 2.5 times that of MGL-3196); There is a clear presence of hepatic intestinal circulation in the body, which further increases the exposure of drugs to the liver.

7、Bioavailability: MGL-3196 has a bioavailability of 29% in rats, while DSC192 has a bioavailability of up to 52% in rats.

8、Safety Evaluation: The hERG test data indicates that compound DSC192 has lower cardiac toxicity.

9、Pharmacodynamics: Compared to MGL-3196, DSC192 could significantly reduce the levels of ALT、AST、 TC、TG in the serum, and TC、TG level in the liver of high-fat diet (HFD) induced NASH model mice under the same dosage conditions; At the same time, DSC192 significantly improved mouse liver cell steatosis, inflammatory cell infiltration, and hepatocyte ballooning.

10、Intellectual Property: DSC192 molecule and its related compounds have been patented (Application number: 202310958594.6).

11、IND application: Apply for clinical research in China in February 2025.