Kailile Approved for Marketing in China

On December 23, 2025, Zai Lab officially announced that the National Medical Products Administration (NMPA) has approved the New Drug Application for xanomeline-trospium chloride capsules (KarXT, brand name: Kaijiele). This drug will be used for the treatment of adult schizophrenia. This approval marks a major breakthrough in the field of schizophrenia treatment in China in over 70 years, with the first therapy featuring a novel mechanism of action officially arriving, offering a new treatment option for a vast number of patients.

Functional Characteristics

As a first-in-class innovative therapy, Kaijiele ® employs a unique fixed-dose combination design, consisting of the M1/M4 muscarinic acetylcholine receptor agonist xanomeline and the muscarinic receptor antagonist trospium chloride. Unlike traditional antipsychotic drugs that primarily target dopamine or serotonin receptors, this drug exerts its therapeutic effect by precisely activating the M1 and M4 muscarinic receptors in the central nervous system, while utilizing trospium chloride to reduce peripheral side effects. It has demonstrated significant efficacy advantages and good tolerability in clinical studies. Data from the China Phase 3 bridging study showed that at week five of treatment, the total score on the Positive and Negative Syndrome Scale (PANSS) for patients in the Kaijiele ® group was significantly reduced by 9.2 points compared to the placebo group. Furthermore, all key secondary efficacy endpoints achieved statistically significant improvement, with no unexpected safety signals observed.

Market Impact

The journey of Kaijiele ® to the Chinese market began in November 2021, when Zai Lab acquired the exclusive development and commercialization rights for the drug in Greater China (including Mainland China, Hong Kong, Macau, and Taiwan) from Karuna Therapeutics for $187 million. Subsequently, the global development of the drug continued to accelerate. In December 2023, Bristol Myers Squibb (BMS) acquired Karuna Therapeutics for $14 billion, incorporating Kaijiele ® into its core pipeline.

China has over 8 million schizophrenia patients, but the treatment rate is less than 50%. Existing drugs are mostly dopamine D2 receptor antagonists, which have significant side effects (such as weight gain, extrapyramidal symptoms), leading to poor patient adherence. As the first muscarinic receptor agonist, Kaijiele® demonstrates efficacy covering the three major symptom domains (positive, negative, cognitive) and excellent safety (no black box warning). It is expected to become a first-line treatment option, potentially disrupting the existing market landscape. It is anticipated to achieve rapid uptake, driving the expansion of the overall market size (the global antipsychotic drug market already exceeds tens of billions of dollars, with significant growth potential for China's share).