Innovent Biologics Initiates Phase 3 Trial for Novel Gout Drug Tigulixostat in China
核心洞察
Innovent Biologics (搜索) has dosed the first patient in a Phase 3 clinical trial for tigulixostat (IBI128), a novel xanthine oxidase (搜索) inhibitor for gout (搜索) treatment in China.
The randomized, double-blind study will enroll 600 Chinese gout (搜索) patients to compare tigulixostat 100 mg against febuxostat 40 mg over 24 weeks.
Previous Phase 2 data showed tigulixostat achieved 81% serum uric acid compliance rate at 16 weeks, significantly outperforming febuxostat with good safety profile.
Innovent Biologics (搜索) has initiated a pivotal Phase 3 clinical trial for tigulixostat (IBI128), a novel xanthine oxidase (搜索) inhibitor licensed from LG Chem (搜索), marking a significant milestone in addressing China's growing gout (搜索) epidemic. The company announced that the first patient has been dosed in the randomized, double-blind, multi-center study designed to evaluate the drug's efficacy against the current standard of care.
Phase 3 Trial Design and Objectives
The Phase 3 study will enroll 600 Chinese patients meeting the 2015 ACR/EULAR gout (搜索) diagnostic criteria, randomizing them in a 1:1 ratio to receive either tigulixostat 100 mg or febuxostat 40 mg for 24 weeks. The primary endpoint focuses on the proportion of patients achieving serum uric acid levels below 360 μmol/L at week 24, with the overall treatment period extending to one year to assess long-term safety and efficacy.
Professor Zou Hejian from Huashan Hospital, Fudan University, who serves as the study's principal investigator, emphasized the clinical significance of this development. "Current gout (搜索) treatment has dual challenges of drug safety concerns and insufficient efficacy," he stated. "The Phase 2 data of IBI128 have shown significant advantages in lowering uric acid. This Phase 3 study, through head-to-head design and long-term observation, is expected to provide high-level evidence-based evidence for clinical practice."
Promising Phase 2 Results Drive Development
The Phase 3 initiation follows encouraging Phase 2 results that demonstrated tigulixostat's superior efficacy compared to febuxostat. In the Phase 2 study (CIBI128A201), the 100 mg dose group achieved a serum uric acid compliance rate of 81% at 16 weeks, significantly outperforming the febuxostat 40 mg group. The Phase 2 clinical data were published at the Asia-Pacific League of Associations for Rheumatology (APLAR) conference in 2025.
Tigulixostat showed good safety characteristics in previous clinical studies, with favorable renal and cardiovascular safety profiles. As a new-generation highly selective xanthine oxidase (搜索) inhibitor, the drug represents a novel non-purine approach to treating hyperuricemia (搜索) associated with gout (搜索).
Addressing China's Gout Crisis
The development of tigulixostat comes at a critical time for China's healthcare system, as gout (搜索) has emerged as one of the country's largest chronic diseases. According to the latest research cited in the announcement, the overall prevalence of hyperuricemia (搜索) in China reaches 17.7%, with gout prevalence at 3.2%. The patient base is substantial, with approximately 177 million people affected by hyperuricemia, including more than tens of millions with gout.
The disease profile has shifted dramatically, with nearly 60% of patients now between ages 18 and 35 years, and the average age of onset decreasing to 48.28 years. This trend correlates with lifestyle factors including high-purine diets, sugar-containing beverage consumption, and sedentary behavior patterns.
Dr. Lei Qian, Chief R&D Officer of General Biomedicine at Innovent Biologics (搜索), highlighted the urgent medical need. "Gout (搜索) is one of the largest chronic diseases in China, which has long brought a sustained health burden to millions of patients. However, compared with chronic diseases such as diabetes and hypertension, the current therapeutic options are still relatively limited."
Comprehensive Pipeline Strategy
Beyond tigulixostat, Innovent has established a systematic pipeline strategy in the gout (搜索) and hyperuricemia (搜索) therapeutic area. The company is advancing multiple innovative programs, including IBI3011 (搜索), an IL-1RAP (搜索) monoclonal antibody designed to control acute gout flares, and mazdutide, a globally innovative GCG/GLP-1 (搜索) dual receptor agonist that may provide therapeutic benefits for patients with obesity complicated by hyperuricemia.
Strategic Partnership and Commercialization
In December 2022, Innovent Biologics (搜索) entered into a strategic collaboration with LG Chem (搜索), securing exclusive development and commercialization rights for tigulixostat in China. This partnership reflects the growing recognition of China's gout (搜索) market potential and the need for innovative therapeutic solutions.
The Phase 3 trial represents the final stage toward potential commercialization of tigulixostat in China, where current treatment options face significant limitations including cardiovascular risks, hypersensitivity reactions, acute kidney injury risks from excessive uric acid excretion, insufficient drug compliance rates, and medication restrictions for patients with renal impairment.
Long-term uncontrolled gout (搜索) can lead to irreversible organ damage and serious complications, including joint and motor function damage, kidney and metabolic system risks, and substantial socioeconomic burden, potentially resulting in decreased quality of life and labor productivity losses.