Yuhan Wins U.S. Patent for Preclinical LOX-Inhibitor Candidate Targeting Multi-Organ Fibrosis
核心洞察
Yuhan registered a U.S. patent on July 21 covering bicyclic fused ring derivatives that inhibit the LOX enzyme family, a preclinical small-molecule anti-fibrosis candidate.
The patent lists idiopathic pulmonary fibrosis (搜索), MASH, chronic kidney disease (搜索) and liver cirrhosis (搜索) as target indications, positioning the asset across multiple organ fibrosis markets.
The LOX inhibitor differs mechanistically from Yuhan's disclosed MASH candidate YH25724, which acts on FGF21 (搜索) and GLP-1 (搜索) and entered domestic Phase 1 planning in May.
Yuhan has secured a U.S. patent for an anti-fibrosis drug candidate that does not appear in its publicly disclosed research and development pipeline, positioning the preclinical asset against a cluster of fibrotic diseases spanning the lung, liver and kidney.
According to the pharmaceutical industry, Yuhan registered a patent in the United States on July 21 for "bicyclic fused ring derivatives or salts thereof and pharmaceutical compositions containing the same." The compound described is a small-molecule synthetic drug candidate that inhibits the activity of the LOX (lysyl oxidase (搜索)) family.
LOX comprises a group of enzymes involved in cross-linking collagen and elastin to maintain tissue structure. When LOX-family enzymes become excessively active, collagen accumulates, hardening tissue and potentially reducing organ function. The patent lists idiopathic pulmonary fibrosis (搜索) (IPF), metabolic dysfunction-associated steatohepatitis (搜索) (MASH), chronic kidney disease (搜索) (CKD) and liver cirrhosis (搜索) as target diseases.
A Yuhan official said, "It is still a preclinical-stage candidate, so it is difficult to provide detailed explanations."
A Distinct Mechanism From YH25724
The new candidate is drawing attention because it differs mechanistically from YH25724, the MASH treatment Yuhan is currently developing. YH25724 acts simultaneously on FGF21 (搜索), a hormone that regulates energy metabolism, and GLP-1 (搜索), a hormone that regulates blood sugar and appetite, and received approval for a domestic Phase 1 clinical trial plan in May this year.
The LOX-directed candidate, by contrast, is a small-molecule compound that directly targets the LOX family, and the patent proposes a broad range of indications extending to IPF, CKD and liver cirrhosis (搜索). If development succeeds, the candidate could expand into fibrotic diseases of the lung, liver and kidney based on a single mechanism.
Market Sizing and Deal Activity
The industry expects the global IPF treatment market to grow from about $3.7 billion in 2024 to $5.5 billion in 2030, while the CKD treatment market is projected to expand from $14.5 billion to $17.2 billion over the same period. Adding MASH and liver cirrhosis (搜索) widens the candidate's potential market reach further.
Global drugmakers have moved aggressively to secure fibrosis and MASH treatments. Last year, GSK acquired efimosfermin alfa, under development for fatty liver diseases including MASH, for $2 billion. In the same year, Novo Nordisk acquired Akero Therapeutics for $5.2 billion, gaining the MASH candidate efruxifermin. In South Korea, OliX (搜索) licensed out its MASH and obesity candidate OLX702A to Eli Lilly in a deal worth up to $630 million, or about 911.7 billion won at the time.
Fibrosis is a common pathological process that drives disease progression and organ failure across different organs such as the lung, liver and kidney, so the potential to expand into multiple indications could affect the value of the drug.
An industry official said, "Because fibrosis is a pathological process that appears commonly across multiple organs including the lung, liver and kidney, a mechanism that targets it directly has the potential to expand beyond a single indication." The official added, "It is still preclinical, so it is too early to judge the chances of success, but if efficacy and safety are demonstrated, there is room for it to develop into an asset that global pharmaceutical companies could well take interest in."
Parallel Progress in the Fibrosis Space
Separately, D&D Pharmatech (搜索) said on the 11th that Japan had approved registration of a new substance patent for TLY012, its drug candidate for fibrotic diseases, covering therapeutic uses for fibrosis, autoimmune diseases and cancer. The patent covers a next-generation candidate with improvements including reduced immunogenicity compared with the earlier substance. With Japan, D&D Pharmatech now holds rights to TLY012 in the United States, Australia and China as well.
TLY012 is a recombinant protein drug in the TRAIL (tumor necrosis factor-related apoptosis-inducing ligand) class. It targets the DR5 receptor (搜索) on the surface of myofibroblasts, which drive the fibrotic process, killing only the myofibroblasts at lesion sites to restore fibrotic tissue to a normal state.
D&D Pharmatech (搜索) is amending its investigational new drug application to change the indication for TLY012 to liver fibrosis. Having confirmed a reduction in fibrotic liver tissue in preclinical animal models of cirrhosis, the company plans to complete the change of indication and enter global trials as early as the beginning of next year.
"We will quickly wrap up the IND amendment for liver fibrosis and enter clinical trials early next year," said CEO Lee Seul-ki. "With effective treatment options for fibrosis still lacking worldwide, we will do our utmost to contribute to a fundamental improvement in patients' lives through the development of TLY012."