Drug name
Last update: Aug 2026Paliperidone Palmitate Three Monthly (PP3M)
Developer(s)
Drug information
Not provided
Paliperidone Palmitate Three-Monthly (PP3M)
INVEGA TRINZA®, TREVICTA® (previously Paliperidone Janssen)
Small molecule
Not provided
Paliperidone palmitate administered as a once every three-month long-acting injectable (PP3M) is indicated for the maintenance treatment of schizophrenia in patients who have achieved a satisfactory therapeutic response following at least four months of continuous treatment with one-monthly paliperidone palmitate (PP1M) injection. INVEGA TRINZA® and TREVICTA® manufactured by Janssen Pharmaceuticals are available in dosage formulations of 273 mg, 410 mg, 546 mg and 819 mg. Due to its extremely low water solubility, PP3M dissolves gradually following intramuscular injection, prior to being hydrolysed to paliperidone and subsequent absorption. Release of the active paliperidone substance lasts up to 18 months, with maximum plasma concentrations achieved after approx. 30-33 days (median Tmax).
PP3M is approved under the trade name of INVEGA TRINZA® by the United States Food and Drug Administration (US FDA) for the treatment of schizophrenia in patients after they have been adequately treated with INVEGA SUSTENNA® (PP1M) for at least 4 months. PP3M is also approved by the European Medicines Agency (EMA) under the trade name of TREVICTA® (previously Paliperidone Janssen) for the maintenance treatment of schizophrenia in adult patients who are clinically stable on PP1M. Generic formulations of PP3M have not yet been approved in the European Union. PP3M is not currently approved for use in children and adolescents.
Countries where PP3M formulations (INVEGA TRINZA® / TREVICTA®) are approved: Asia Pacific: Australia, Brunei Darussalam, China, Hong Kong, Indonesia, Japan, Macao, Malaysia, New Zealand, Philippines, Singapore, South Korea, Taiwan, Thailand. EMEA: Albania, Bahrain, Bosnia and Herzegovina, Egypt, European Union, Ghana, Israel, Jordan, Kazakhstan, Kenya, Kuwait, Latvia, Lebanon, Montenegro, Morocco, Norway, Oman, Qatar, Russian Federation, Rwanda, Saudi Arabia, Serbia, South Africa, Sudan, Switzerland, Turkey, United Arab Emirates, United Kingdom. Latin America: Argentina, Aruba, Brazil, Chile, Colombia , Costa Rica, Curaçao, Dominican Republic, Ecuador, El Salvador, Guatemala, Honduras, Jamaica, Mexico, Nicaragua, Panama, Peru, Trinidad and Tobago. North America: Canada, USA.
Therapeutic area(s)
- Mental Health Disorders (incl. schizophrenia, bipolar disorders, Schiz. Aff. Dis.)
- Treatment
Administration route
Intramuscular
Associated long-acting platforms
Nanocrystal technology, Aqueous drug particle suspension
Use of drug
- Administered by a nurse
- Administered by a specialty health worker
Not provided
Dosage
Not provided
Not provided
Not provided
Not provided
Not provided
Associated compounds, formulations and regimens
Not provided
Associated technologies
Not provided
Additional information
Developer(s)
Johnson & Johnson
Janssen Pharmaceuticals is a subsidiary company of Johnson & Johnson headquartered in Beerse, Belgium. They focus on manufacturing and developing pharmaceutical products for use in areas such as, Immunology, Infectious Diseases & Vaccines, Pulmonary Hypertension, Cardiovascular & Metabolism, Oncology, and Neuroscience.
Drug structure
Scale-up and manufacturing prospects
PP3M is commercially manufactured by Janssen Pharmaceuticals with formulation development provided by Alkermes. The PP3M injectable contains a racemic mixture of (+)- and (-)- of paliperidone, which is joined with palmitic acid through an ester linkage. PP3M, like paliperidone palmitate once-monthly injectable (PP1M), is manufactured using Nanocrystal Technology to improve the dissolution properties of paliperidone palmitate, which is highly insoluble in water. PP3M has an extended dosing interval arising from a higher concentration (312 mg/mL) and an increased nanocrystal particle size.
NanoCrystal® Colloidal Dispersion Nanomill™ apparatus.
NanoCrystal technology enables intrinsically high loading of insoluble drugs as dosage forms consist mostly of pure API packed as a solid crystal, which is the most efficient form possible in relation to weight-to-volume. Paliperidone palmitate particles are dispersed in an aqueous suspension and transformed into smaller nanocrystals through particle-size reduction. These nanocrystals have a greater surface area than the larger original particles, resulting in increased water solubility. This medicinal product does not require any special storage conditions and has a shelf life of two years.
Digital microscope and scanning electron microscopy (SEM) to determine shape of the particles. Differential scanning calorimetric (DSC) and Fourier transforms infrared spectroscopy (FTIR) for quality control.
Excipients & delivery device(s)
No proprietary excipient used
No novel excipient or existing excipient used
No residual solvent used
No delivery device
Safety, Efficacy and Evidence Summary
Not provided
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Paliperidone palmitate LAI dosing regimen for missed doses in PP1M and switch to 3-months formulation (PP3M: 175 or 525 mg eq., 273 or 819 mg PP)
The present application provides a method for treating patients in need of psychiatric treatment, wherein said patient is being treated with the 3-month formulation of paliperidone palmitate and fails to take the next scheduled dose of the 3-month formulation of paliperidone palmitate.
WO2016164218
Dosing regimen
Janssen
Not provided
March 30, 2026
Granted: AU, CA, EA (AM, AZ, BY, KG, KZ, RU, TJ, TM), EP (AT, BE, BG, CH, CZ, DE, EE, ES, FI, FR, GB, GR, HR, HU, IE, IT, LT, LU, LV, MC, MK, MT, NO, NL, PL, PT, RO, RS, SE, SI, SK, SM, TR, BA, ME, MA, MD), IL, JP, KR, MA, UA, US Pending: KR Not in force: BR, NZ
Paliperidone aqueous suspensions
The present invention is concerned with a pharmaceutical composition suitable as a depot formulation for administration via intramuscular or subcutaneous injection, comprising: (1) as an active ingredient a therapeutically effective amount of a 9-hydroxyrisperidone fatty acid ester or a salt, or a stereoisomer or a stereoisomeric mixture thereof and (2) a pharmaceutically acceptable carrier; wherein the pharmaceutically acceptable carrier is water and the active ingredient is suspended therein; and with a process of preparing such a composition. The invention further concerns such a pharmaceutical composition for use as a medicament in the treatment of schizophrenia, non-schizophrenic psychoses, behavioural disturbances associated with neurodegenerative disorders
WO9744039
Composition
Janssen Pharmaceutica, N. V
Not provided
May 12, 2017
Expired