Highlands Pharmaceuticals today announced positive topline results from its Phase III clinical trial ("TARA Study") evaluating Ginositinib, an oral small-molecule JAK1/TYK2 inhibitor， for the treatment of active rheumatoid arthritis (RA). The study met its primary and all secondary efficacy endpoints, demonstrating statistically superior outcomes compared to the positive control drug Tofacitinib (Xeljanz), along with a favorable safety and tolerability profile. This marks the first registrational study globally to use another JAK inhibitor as a positive control and achieve superior efficacy results.

The TARA Study is a multicenter, randomized, double-blind Phase III trial evaluating the efficacy and safety of Ginositinib in RA patients with inadequate response or intolerance to biologic agents. A total of 459 subjects were enrolled and randomized to receive either Ginositinib or the control drug Tofacitinib for 52 consecutive weeks. The primary efficacy endpoint was the ACR50 response rate at 24 weeks, as defined by the American College of Rheumatology. This is also the first global Phase III registrational study in this disease to adopt ACR50 as the primary endpoint.

The study results showed that the primary endpoint was successfully achieved, demonstrating superior efficacy and significant improvement in patients' quality of life. Key secondary endpoints in the Ginositinib group also showed statistically significant superiority over the Tofacitinib group (p<0.0001), including ACR20/70 response rates, the proportion of subjects achieving DAS28 ≤3.2 and DAS28 <2.6, and the proportion of subjects achieving low disease activity (LDA) defined by CDAKI ≤10. Furthermore, patients in the Tofacitinib group who did not achieve ACR50 showed marked improvement after switching to Ginositinib, suggesting that Ginositinib may remain effective in refractory patients — those who respond poorly to both biologics and JAK inhibitors. Currently, no drug is approved for treating refractory patients, representing an unmet clinical need.

Professor Zeng Xiaofeng, the lead principal investigator of the TARA Study from Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, commented: "Rheumatoid arthritis is a significant cause of disability in China, imposing a heavy economic burden on families and society. This study, completed across more than 60 centers in China, represents the world's first head-to-head Phase III registrational study in RA using an active comparator with the same mechanism. The interim analysis results met both the primary and all secondary endpoints. Although multiple drugs with different mechanisms of action are already available on the market, many patients still fail to achieve the treatment goals of clinical remission or low disease activity. Ginositinib demonstrated significantly higher ACR50/70 rates, as well as higher proportions of patients achieving clinical remission or low disease activity, compared to the Tofacitinib group. Ginositinib holds the potential to help more RA patients achieve remission, which is truly promising."

The overall safety profile of Ginositinib during the study period was favorable. The incidence of adverse events was generally comparable between the two groups. The rates of serious adverse events and severe adverse events were low and showed no meaningful difference between groups. The adverse event profile was consistent with other JAK inhibitors, and no new safety signals were identified. Follow-up of the study is ongoing, and complete data will be presented at future academic conferences or published in peer-reviewed journals.

Ginositinib (TLL-018) is a highly selective oral small-molecule JAK1/TYK2 inhibitor designed to modulate key immune-inflammatory signaling pathways for the treatment of various autoimmune and inflammatory diseases. To date, the drug has been evaluated in over 1,000 subjects cumulatively in China and the United States. Currently, Ginositinib is undergoing Phase III clinical trials in China for chronic spontaneous urticaria (CSU) and rheumatoid arthritis (RA).

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