Paliperidone

Schizophrenia is a severe mental disorder characterized by high recurrence rate and high disability rate. Poor patient compliance in clinical treatment is one of the core inducing factors for disease recurrence. Paliperidone is a second-generation atypical antipsychotic drug and the main active metabolite of risperidone. It exerts its effect by blocking central dopamine D2 receptors and 5-hydroxytryptamine 2A receptors. It can not only effectively control the positive symptoms of schizophrenia, but also has clear advantages in improving negative symptoms, cognitive impairment and affective symptoms. Compared with traditional antipsychotic drugs, it has a lower incidence of extrapyramidal adverse reactions, and is suitable for acute phase treatment and maintenance phase recurrence prevention in adult and adolescent (12-17 years old) patients with schizophrenia. The launch of its long-acting injectable dosage form has greatly improved the compliance of patients requiring long-term medication.

The global market size of paliperidone-related preparations has maintained steady growth in recent years. The overall market size exceeded 4.5 billion US dollars in 2023, among which long-acting injectables accounted for more than 70%, making it the core variety in the field of long-acting treatment for schizophrenia. In terms of the domestic market, with the implementation of the volume-based procurement policy and the successive approval of generic drugs, the price of oral paliperidone preparations has dropped by more than 80%. The domestic market size exceeded 1.2 billion yuan in 2023, with an annual growth rate of around 18%. At present, more than 10 enterprises in China have been approved to produce paliperidone API. Local enterprises have gradually realized the substitution of original research products by virtue of cost advantages. Meanwhile, APIs from multiple enterprises have obtained US FDA DMF certification, and are capable of exporting and supplying to the global market.

The original research enterprise of paliperidone is Johnson & Johnson. The original oral preparation is sold under the trade name "Invega", and the long-acting injectable preparations are sold under the trade names "Invega Sustenna" and "Invega Trinza". Its core compound patent expired in 2017, and formulation patents for different dosage forms will expire successively from 2024 to 2029. The original oral dosage form, which is available in conventional specifications of 3mg, 6mg and 9mg extended-release tablets, has been included in the *Catalogue of Chemical Reference Preparations* issued by NMPA, and is also a reference preparation recognized by FDA. Up to now, the CDE API registration platform has more than 20 paliperidone API registration entries, among which more than 15 are in "A" status and can be used for associated review. Multiple dosage forms including oral extended-release tablets and long-acting injectables have been approved for marketing in China, and the number of generic drug enterprises that have passed the consistency evaluation exceeds 8. (Data as of October 2024, please refer to the official website of CDE for the latest information)

CATO provides a full set of paliperidone impurity reference standards, covering all categories such as synthesis process impurities, degradation impurities, enantiomers, etc. Most products are available in stock. For in-stock products, orders placed before 16:00 will be shipped on the same day. All reference standards comply with the regulatory requirements of the Chinese Pharmacopoeia, FDA and other regulations, and can meet the research needs of the whole process including API R&D, quality research, registration and declaration, etc.