San Francisco, USA / Suzhou, China | March 22, 2026
Innovent Biologics has announced that the first participant has been dosed in a Phase 3 clinical study of IBI128 (tigulixostat), a novel xanthine oxidase inhibitor (XOI) being developed for the treatment of gout and hyperuricemia. This milestone marks a significant step forward in the company’s efforts to deliver innovative, targeted therapies for metabolic diseases, addressing a rapidly growing patient population with limited effective and safe treatment options. The initiation of this late-stage trial underscores the potential of tigulixostat to become a next-generation therapy with improved efficacy and safety compared to existing treatments.
Phase 3 Study Designed for Robust Clinical Evidence
The Phase 3 trial is a randomized, double-blind, multi-center study designed to directly compare tigulixostat with febuxostat, a commonly used standard-of-care therapy. The study plans to enroll approximately 600 patients in China who meet established diagnostic criteria for gout, with participants randomized in a 1:1 ratio to receive tigulixostat 100 mg or febuxostat 40 mg over a 24-week evaluation period within a one-year treatment framework.
The primary endpoint focuses on the proportion of patients achieving target serum uric acid (sUA) levels below 360 μmol/L at week 24, a clinically relevant marker for effective disease management. This head-to-head design is expected to generate high-quality comparative data, providing strong evidence to support regulatory submissions and clinical adoption if successful.
Promising Phase 2 Data Supports Advancement
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The advancement of tigulixostat into Phase 3 development is supported by encouraging Phase 2 clinical results, which demonstrated a significantly greater urate-lowering effect compared to febuxostat, along with a favorable safety profile. In earlier studies, the 100 mg dose achieved an 81% compliance rate in reaching target uric acid levels, outperforming the comparator group and highlighting its potential superiority in clinical efficacy.
Importantly, tigulixostat has shown good renal and cardiovascular safety characteristics, addressing key limitations associated with existing gout therapies, such as hypersensitivity reactions, cardiovascular risks, and reduced suitability in patients with renal impairment. These findings position tigulixostat as a potentially best-in-class therapy capable of improving both treatment outcomes and patient safety.
Addressing a Growing Global Health Burden
Gout is one of the fastest-growing metabolic diseases globally, with a significant increase in prevalence, particularly among younger populations. In China alone, millions of patients are affected, with hyperuricemia prevalence reaching nearly 18% and gout affecting over 3% of the population. The disease is associated with chronic pain, joint damage, kidney complications, and increased cardiovascular risk, significantly impacting patient quality of life and healthcare systems.
Despite its prevalence, current treatment options remain limited, with challenges related to efficacy, safety, and long-term adherence. Tigulixostat aims to address these unmet needs by providing a more potent and selective mechanism of action, targeting xanthine oxidase to effectively reduce uric acid production while maintaining a favorable safety profile.
The dosing of the first patient in the Phase 3 study of tigulixostat represents a key milestone in late-stage clinical development, bringing the therapy closer to potential regulatory approval and commercialization. With its strong clinical rationale, promising early data, and targeted mechanism, tigulixostat has the potential to transform the treatment landscape for gout and hyperuricemia, offering a more effective and safer alternative to current standard therapies. This development highlights Innovent’s commitment to advancing innovative therapies that address significant unmet medical needs in metabolic diseases.
Source: Innovent Biologics press release
