October 15, 2019
Terns Pharmaceuticals, Inc., a global biopharmaceutical company focused on discovering and developing innovative therapies to treat non-alcoholic steatohepatitis (NASH) and cancer, today announced it will present preclinical study results on the farnesoid X receptor (FXR) agonist TERN-101 at The Liver Meeting® 2019, being held by the American Association for the Study of Liver Diseases (AASLD) in Boston, MA., November 8-12. The data demonstrate that in preclinical models, TERN-101 was preferentially delivered to the liver, which enables a robust, localized effect on FXR, while potentially mitigating non-liver mediated adverse effects.
The abstract (#2158), titled “Pharmacokinetics, tissue distribution and pharmacodynamics of TERN-101, a novel farnesoid X receptor (FXR) agonist, in preclinical species” will be presented as a poster on Monday, November 11, 2019.
“TERN-101 has the potential to be the backbone of future combination treatments for NASH due to its broad pleiotropic effects of FXR agonism on multiple pathogenetic mechanisms of NASH,” said Erin Quirk, M.D., Chief Medical Officer of Terns. “Our preclinical data show that TERN-101 is efficiently enriched in the liver, the target organ for FXR activity against NASH, which could potentially mitigate non-liver mediated tolerability issues associated with systemic FXR activation.”
TERN-101 has been advanced into clinical studies. A Phase 1 trial demonstrated clinical pharmacokinetic properties consistent with once-daily dosing. At The International Liver Congress™ 2019 in Vienna, Terns presented preclinical data demonstrating that TERN-101 reduced liver steatosis, inflammation, ballooning, and fibrosis in a preclinical model of non-alcoholic steatohepatitis (NASH).
TERN-101 and TERN-201, a semicarbazide-sensitive amine oxidase (SSAO) inhibitor, are both in development for the treatment of NASH and were initially discovered and developed by Eli Lilly and Company. Terns signed a global, exclusive agreement with Eli Lilly in 2018 to develop, manufacture, and commercialize TERN-101, TERN-201, and another preclinical candidate that inhibits an undisclosed NASH target.
About TERN-101 and Farnesoid X Receptor (FXR) Agonism
TERN-101 is a potent non-bile acid FXR agonist being developed as a therapeutic for NASH. FXR is a nuclear receptor that is highly expressed in the liver and small intestine. Bile acids (BA) are natural ligands of FXR, and their binding with and activation of FXR is critical to the regulation of cellular pathways that modulate BA synthesis, lipid metabolism, inflammation, and fibrosis. FXR agonism and activation has demonstrated improvement over placebo in regression of histological liver fibrosis without progression to NASH in a late-stage study, demonstrating the potential for FXR agonists to be a new treatment modality for NAFLD and NASH.
Non-alcoholic steatohepatitis (NASH) is a severe form of non-alcoholic fatty liver disease (NAFLD), which is caused by the accumulation of excess fat in the liver. NASH is associated with chronic liver inflammation and liver cell injury, and it can lead to fibrosis, cirrhosis, and eventually liver cancer or liver failure. Global rates of NAFLD and NASH are increasing rapidly, in tandem with rising rates of obesity. There is currently no approved medication for the treatment of NASH.
About Terns Pharmaceuticals
Terns Pharmaceuticals, Inc. is a clinical-stage pharmaceutical company that is focused on the discovery and development of medicines for chronic liver disease and cancer. Based in China and the United States, the company is advancing a pipeline of drug candidates for the treatment of non-alcoholic steatohepatitis (NASH) and cancer, across multiple modalities. Terns leverages world class expertise in disease biology, medicinal chemistry, and clinical development in order to bring promising new therapies to patients in China and other global markets.