LNK01003 is an oral small molecule JAK inhibitor with intestine-restricted properties developed by the company for the treatment of ulcerative colitis and related diseases. Restricting drug exposure to the gastrointestinal tract, coupled with high systemic clearance, should greatly reduce side effects by avoiding systemic immunosuppression. However, as the concentration of the drug is enriched in the gastrointestinal tissues, it maximizes the inhibition of multiple inflammatory cytokines that play roles in IBD. Thus, LNK01003 has the potential to improve its therapeutic efficacy. As a representative third-generation JAK inhibitor, LNK01003 has the potential to be a first-in-class treatment. The phase I clinical study was to evaluate the safety, tolerability, pharmacokinetics, and food effects of LNK01003 in healthy subjects in a randomized, double-blind, placebo-controlled, single, and multiple dose escalations. A total of 105 healthy subjects were enrolled in this study. The results showed that LNK01003 was safe and well tolerated in all dose groups, with no SAEs (serious adverse events), and no TEAEs (adverse events occurring after dosing) leading to discontinuation or early withdrawal.

Dr. Michael Vazquez, Co-founder, Executive Vice President, and Head of Chemistry of Lynk Pharmaceuticals, said, "We are very pleased to see the positive results from LNK01003 in the Phase I study of healthy subjects. LNK01003 was designed to be GI-restrictive, preclinical studies showed that this compound has good cell permeability and is rapidly cleared from the systemic circulation, which limits the drug to the intestine and reduces systemic exposure. We anticipate that the avoidance of systemic exposure will reduce side effects and improve the safety of the drug. We will continue to advance the clinical development of LNK01003 and look forward to its performance in patient trials."

Dr. Henry Wu, Chief Development Officer of Lynk Pharmaceuticals, said, "LNK01003 is a third-generation JAK inhibitor with intestine-restricted properties that showed desirable pharmacokinetic profiles and tolerability in single and multiple dose escalation studies in healthy subjects. This is an important milestone in our research on intestine-restricted JAK inhibitors. At present, phase II clinical trial of LNK01003 for ulcerative colitis is in progress. The study is led by Prof. Minhu Chen, a renowned gastroenterologist at the First Affiliated Hospital of Sun Yat-sen University, with supports from multiple excellent clinical centers across the country. We will strengthen our development efforts of this promising compound in the hope to provide more treatment options for patients worldwide."