Three key phase I clinical trials of risperidone sustained-release microsphere intramuscular injection preparation ly 03004 in the United States

On May 14, green leaf Pharmaceutical Group Co., Ltd announced that its self-developed muscle injection preparation of risperidone sustained release microspheres (ly 03004) for the treatment of schizophrenia has completed three critical phase I clinical trials in 172 patients in the United States The results show that ly03004 only needs to be injected once every two weeks, which is convenient to use and has similar bioavailability and safety It is expected that ly03004 will simplify the treatment plan, improve drug compliance and develop a new improved product for the treatment of schizophrenia and / or schizoaffective disorder Schizophrenia is a kind of serious mental disorder, which has the characteristics of thinking interruption, affecting language, concept and self cognition According to the World Health Organization (who), more than 21 million people are suffering from schizophrenia According to the National Institutes of Health (NIH), an estimated 2.4 million Americans suffer from schizophrenia At present, the release of risperidone microspheres is limited in the first three weeks after the first injection, which needs to be made up by oral preparation In a single dose, multiple trials, 108 schizophrenics and / or schizophrenic affective disorder patients received 25.0 mg ly 03004 or another microsphere drug (control drug) once every two weeks for five consecutive times The results showed that the steady-state plasma concentration of ly 03004 was reached two weeks after the first administration, while that of the control drug was reached four weeks after the first administration In addition, according to the standard method of food and Drug Administration (FDA) to verify bioequivalence, this key study confirmed that the main pharmacokinetic indexes of ly 03004 after the 5th application were bioequivalent compared with the control drugs In addition, the safety of ly 03004 was similar to that of the control drug for 5 consecutive times In a single, multiple dose trial, 32 patients with schizophrenia and / or schizoaffective disorder in the United States received 25.0 mg or 50.0 mg ly 03004 or a marketed drug (control) The results showed that ly 03004 began to release the drug on the first day after injection, and it could reach the peak concentration level of blood drug on the 14th day; while the control drug only released a small amount of drug after a single injection, and the drug release was very limited in the next 21 days, and it could reach the peak concentration level of blood drug on the 32nd day The results showed that the patients did not need to take oral preparation 3 weeks after the first injection of ly 03004 However, the safety of ly 03004 is similar to that of the control drug after 25.0mg or 50.0mg single application In a single dose incremental trial, 32 American schizophrenics and / or schizophrenic affective disorder patients received one of four incremental doses of ly 03004 (12.5 mg, 25.0 mg, 37.5 mg and 50.0 mg) The results also confirmed that ly 03004 had good safety and dose balance It is reported that on the basis of the completion of these three tests, green leaf pharmaceutical plans to discuss with the FDA the matter of submitting a new drug listing application (NDA) In addition, the company plans to get ly 03004 approved by European and Japanese regulators LVYE pharmaceutical is a leading innovative pharmaceutical enterprise in China, which has been committed to the development of microspheres, liposomes and other new preparations In 2014, the first "National Key Laboratory for long-term and targeted preparations" in China passed the acceptance of the Ministry of science and technology Now, a number of innovative preparations and other products with independent intellectual property rights have been registered for clinical research in China and the United States simultaneously.