FDA Approves Paliperidone Palmitate for Schizophrenia, Schizoaffective Disorder

Luye Pharma Group announced on July 29, 2024, that the US Food and Drug Administration (FDA) approved paliperidone palmitate (ERZOFRI), an extended-release injectable suspension for the treatment of schizophrenia and schizoaffective disorder in adults as a monotherapy and as an adjunct to mood stabilizers or antidepressants.¹

Long-acting injectables can be effective in managing symptoms of schizophrenia. Injectables improve patient adherence by reducing the dosing frequency and preventing the risk of patients not adhering to their dosing regimen. Paliperidone palmitate is administered once a month.

“As one of the issues with patients with schizophrenia is due potentially to those negative symptoms, the cognitive issues, patients don't always take the oral pills regularly,” Sam Clark, MD, PhD, the founder and CEO of Terran Biosciences, told HCPLive.² “…having long-acting injectable medications helps because even if you're going to take your pills, it's [all] you get with one injection, and it lasts a long time, between 1 to 6 months. And in that sense…the treatment paradigm makes a big difference, and so it's very important.”

Paliperidone palmitate, patented and developed in China, was granted a US patent in 2023, which will expire in 2039.¹ Now, ERZOFRI is approved as a new drug under the 505(b) (2) pathway in the US.

The FDA approval is based on the results of an open-label, randomized (1:1), multiple-dose, parallel-group study of 281 patients aged 18 – 65 years with schizophrenia or schizoaffective disorder. The trial was designed to evaluate the pharmacokinetics profile of paliperidone palmitate as well as to compare its bioavailability with the listed drug, INVEGA SUSTENNA.

Participants randomized to the paliperidone palmitate group received a first dose of 351 mg by injection on day 1 in the deltoid muscle, followed by 5 monthly dosing of 156 mg in the gluteal muscle with the last dose on day 141.³ Participants in the SUSTENA group received the first dose of 234 mg on day 1 in the deltoid muscle and a second dose of 150 mg on day 8 also in the deltoid muscle, followed by 5 monthly doses of 156 in the gluteal muscle with the last dose on day 148.

Investigators optimized the initial dosing for paliperidone palmitate by omitting the injection on Day 8 after the first injection.¹ By doing this paliperidone palmitate had a comparable total drug exposure to INVEGA SUSTENNA.

The safety profile of paliperidone palmitate was comparable with that of INVEGA SUSTENNA. Adverse events had an incidence of ≥ 5% and occurred twice as often as those on placebo. The most common adverse events included injection site reactions, somnolence/sedation, dizziness, akathisia, and extrapyramidal disorder.

Ultimately, the study garnered positive results, demonstrating paliperidone palmitate was bioequivalent to INVEGA SUSTENNA at a steady state after several injections.

References

1. ^{Luye Pharma Announces U.S. FDA Approval of ERZOFRI® (paliperidone palmitate) Extended-Release Injectable Suspension for Treating Schizophrenia and Schizoaffective Disorder. BioSpace. July 29, 2024. https://www.biospace.com/luye-pharma-announces-u-s-fda-approval-of-erzofri-paliperidone-palmitate-extended-release-injectable-suspension-for-treating-schizophrenia-and-schizoaffective-disorder. Accessed July 31, 2024.}
2. ^{Derman, C. Improving Schizophrenia Management: A Patient's Call to Care Providers. HCPLive. July 24, 2024. https://www.hcplive.com/view/improving-schizophrenia-management-a-patient-s-call-to-care-providers. Accessed July 31, 2024.}
3. ^{A Study to Evaluate the PK Profiles of LY03010 and Relative Bioavailability at Steady-state of LY03010 Versus INVEGA SUSTENNA in Schizophrenia Patients. Clinical Key. April 22, 2023. https://www.clinicalkey.com/#!/content/clinical_trial/24-s2.0-NCT04922593. Accessed July 31, 2024.}