On September 1, 2021, Janssen Pharmaceuticals, a subsidiary of Johnson & Johnson, announced that the FDA has approved its long-acting atypical antipsychotic drug INVEGA HAFYERA™ (paliperidone palmitate administered once every 6 months). This product is the first and It is the only drug used to treat adult schizophrenia that is only injected twice a year .

Paliperidone palmitate was developed by Johnson & Johnson and was approved by the US FDA in December 2006. It is a long-acting injection of the second-generation antipsychotic paliperidone and the first approved for the treatment of mental illness in 2003. The new drug for schizophrenia is the main metabolite of risperidone.

The mechanism of action of paliperidone is mediated by the combined action of central dopamine 2 (D2) receptors and serotonin (5HT2A) receptor antagonism. In addition, paliperidone is also α1 and α2 adrenergic receptors and Antagonist of H1 histamine receptor. Paliperidone palmitate can effectively overcome the time lag barrier of other long-acting antipsychotics, and can be used for both the acute and maintenance phases of schizophrenia.

In addition, paliperidone does not cause extensive metabolism in the liver, and is secreted in large quantities through the kidneys without change. It has the characteristics of side effects such as involuntary movements or tremors that are unique to atypical schizophrenia drugs. It is superior to the traditional drug olanzapine in terms of drug resistance and drug resistance. At the same time, there are fewer metabolic disorders, so it has good application prospects.

Paliperidone palmitate is a palmitic acid prodrug of Paliperidone (Paliperidone), the main active metabolite of the early antipsychotic drug Risperidone (Risperidone). The mechanism of action is DRD2 antagonist, 5-HT2A antagonist. At present, the FDA has approved four paliperidones to be marketed for the treatment of schizophrenia.

Relevant data show that since the listing of paliperidone palmitate, the sales volume has been increasing year by year. In 2017, the global sales of paliperidone palmitate reached 3.2 billion U.S. dollars, of which China’s sales were 46.4 million yuan. In 2020, global sales have reached 3.653 billion U.S. dollars. It can be said that both the international and domestic market prospects are very broad. TOSUN PHARM can provide imported raw materials and support joint declaration.