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Sourced From DrugBank

Paliperidone

Developer(s)

Janssen Pharmaceuticals

https://www.janssen.com/

Belgium

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

Paliperidone Chemical Structure

Paliperidone Chemical Structure

Sourced From DrugBank

Drug information

Associated long-acting platforms

Not provided

Administration route

Oral, Intramuscular

Therapeutic area(s)

Mental health

Use case(s)

Treatment

Use of drug

Ease of administration

Administered by a nurse
Administered by a specialty health worker
Self-administered

Frequency of administration

Not provided

User acceptance

Not provided

Dosage

Available dose and strength

Not provided

Maximum dose

Not provided

Recommended dosing regimen

Not provided

Additional comments

Not provided

Dosage link(s)

Not provided

Drug information

Drug's link(s)

Not provided

Generic name

Paliperidone Palmitate

Brand name

Not provided

Compound type

Small molecule

Summary

Paliperidone is an atypical antipsychotic drug indicated for the treatment of both schizophrenia & schizoaffective disorder. Paliperidone is the primary active metabolite of risperidone and functions by strongly binding to dopaminergic D2- and serotonergic 5-HT2-receptors and selectively blocking monoamine effects. Although paliperidone is a potent D2-antagonist, it has less of impact on motor function and catalepsy than traditional neuroleptics. Paliperidone palmitate is the palmitate ester prodrug of paliperidone and displays modest solubility in polar solvents. Several long-acting injectable aqueous nanocrystal formulations of paliperidone palmitate are available as once-monthly (PP1M), three-monthly (PP3M) and six-monthly (PP6M) extended-release suspensions for intramuscular injection.

Approval status

Unknown

Regulatory authorities

Unknown

Delivery device(s)

Not provided

Scale-up and manufacturing prospects

Scale-up prospects

Not provided

Tentative equipment list for manufacturing

Not provided

Manufacturing

Not provided

Specific analytical instrument required for characterization of formulation

Not provided

Clinical trials

Not provided

Excipients

Proprietary excipients used

Not provided

Novel excipients or existing excipients at a concentration above Inactive Ingredients Database (IID) for the specified route of administration

Not provided

Residual solvents used

Not provided

Patent info

Compound patent families

Patent informations
Patent description Representative patent Categories Patent holder Licence with MPP Patent source
Paliperidone dosing regimen
Expiry date: 2028-12-17
The present invention provides a method of treating patients in need of treatment with long acting injectable paliperidone palmitate formulations. 		WO2009080651 Dose/Regimen Janssen Pharmaceutica Nv No
Patent status
Patent status/countries Low, Low- middle and upper-middle High income
Granted Belarus, Azerbaijan, Moldova, Republic of, Armenia, Kazakhstan, Albania, Serbia, Bosnia and Herzegovina, Türkiye, North Macedonia, Ukraine, Malaysia, Philippines, Mexico, Sri Lanka, South Africa Australia, Canada, Russian Federation, Liechtenstein, Italy, Norway, Malta, Denmark, Belgium, United Kingdom, Greece, Netherlands, Hungary, Croatia, Switzerland, Spain, Slovenia, Austria, Romania, Iceland, Cyprus, Finland, France, Bulgaria, Slovakia, Poland, Latvia, Ireland, Estonia, Germany, Luxembourg, Portugal, Czechia, Lithuania, Monaco, Sweden, Hong Kong, Japan, Korea, Republic of, New Zealand, United States of America, Singapore
Filed Ecuador, Guatemala, Nicaragua, Indonesia Finland, Hong Kong, Israel, Korea, Republic of
Not in force World Intellectual Property Organization (WIPO), Brazil, China, Colombia, Tajikistan, Turkmenistan, Kyrgyzstan, Albania, Serbia, Bosnia and Herzegovina, Türkiye, North Macedonia, India World Intellectual Property Organization (WIPO), Liechtenstein, Italy, Norway, Malta, Denmark, Belgium, United Kingdom, Greece, Netherlands, Hungary, Croatia, Switzerland, Spain, Slovenia, Austria, Romania, Iceland, Cyprus, Finland, France, Bulgaria, Slovakia, Poland, Latvia, Ireland, Estonia, Germany, Luxembourg, Portugal, Czechia, Lithuania, Monaco, Sweden, Israel, United States of America
Patent informations
Patent description Representative patent Categories Patent holder Licence with MPP Patent source
Paliperidone depot formulation for injection
Expiry date: 2018-11-10
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-hydroxy-risperidone fatty acid ester or a salt, or a stereoisomer or a stereoisomeric mixture thereof in submicron form and (2) a pharmaceuticall 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 psychosis, schizophrenia, schizoaffective disorders, non-schizophrenic psychoses, behavioural disturbances associated with neurodegenerative disorders, e.g. in dementia, behavioural disturbances in mental retardation and autism, Tourette's syndrome, bipolar mania, depression, anxiety. 		WO9925354 Composition Janssen Pharmaceutica N.V No
Patent status
Patent status/countries Low, Low- middle and upper-middle High income
Granted
Filed
Not in force World Intellectual Property Organization (WIPO), Eswatini, Uganda, Zambia, Zimbabwe, Malawi, Ghana, Sudan, Botswana, Lesotho, Kenya, Gambia (the), Argentina, Brazil, China, Tajikistan, Belarus, Azerbaijan, Moldova, Republic of, Turkmenistan, Armenia, Kyrgyzstan, Kazakhstan, Albania, North Macedonia, Indonesia, Malaysia, Congo, Mauritania, Guinea-Bissau, Niger, Senegal, Cameroon, Mali, Togo, Burkina Faso, Benin, Côte d'Ivoire, Central African Republic, Guinea, Gabon, Chad, Türkiye, Ukraine, South Africa, Viet Nam, Mexico World Intellectual Property Organization (WIPO), Australia, Bulgaria, Canada, Czechia, Russian Federation, Estonia, Liechtenstein, Italy, Denmark, Belgium, United Kingdom, Greece, Netherlands, Switzerland, Spain, Slovenia, Austria, Romania, Cyprus, Finland, France, Latvia, Ireland, Germany, Luxembourg, Portugal, Lithuania, Monaco, Sweden, Hong Kong, Croatia, Hungary, Israel, Japan, Korea, Republic of, Norway, New Zealand, Poland, Slovakia, United States of America, Singapore, Brunei Darussalam
Patent informations
Patent description Representative patent Categories Patent holder Licence with MPP Patent source
Paliperidone aqueous suspensions
Expiry date: 2017-05-12
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, e.g. in dementia, behavioural disturbances in mental retardation and autism, bipolar mania, depression, anxiety. 		WO9744039 Composition JANSSEN PHARMACEUTICA NV [BE] No
Patent status
Patent status/countries Low, Low- middle and upper-middle High income
Granted
Filed
Not in force World Intellectual Property Organization (WIPO), Argentina, Brazil, China, Tajikistan, Belarus, Azerbaijan, Moldova, Republic of, Turkmenistan, Armenia, Kyrgyzstan, Kazakhstan, Albania, Indonesia, Mexico, Malaysia, Türkiye, Ukraine, South Africa World Intellectual Property Organization (WIPO), Australia, Bulgaria, Canada, Cyprus, Czechia, Germany, Russian Federation, Estonia, Liechtenstein, Italy, Denmark, Belgium, United Kingdom, Greece, Netherlands, Switzerland, Spain, Slovenia, Austria, Romania, Finland, France, Latvia, Ireland, Luxembourg, Portugal, Lithuania, Monaco, Sweden, Hong Kong, Croatia, Hungary, Israel, Japan, Korea, Republic of, Norway, New Zealand, Poland, Slovakia, Taiwan, Province of China, United States of America
Patent informations
Patent description Representative patent Categories Patent holder Licence with MPP Patent source
Paliperidone compound and analogues and their use as antipsychotics
Expiry date: 2009-10-16
There is disclosed a process for preparing an enantiomeric form of the compound having the formula:or a pharmaceutically acceptable acid addition salt thereof,wherein said process comprises the steps of:(a) reacting a racemic mixture of said compound with a chiral acid or acid chloride selected from the group consisting of tartaric acid, malic acid, mandelic acid, camphor sulfonic acid, 4,5-dihydro-1H-2-benzopyran-2-carboxylic acid, and the acid chlorides thereof, to form a mixture of diastereomeric salts or esters;(b) physically separating said mixture of diastereomeric salts or esters by selective crystallization or chromatography; and(c) converting said separated diastereomeric salts or esters into the corresponding enantiomeric forms of said compound by hydrolysis in an acidic or basic aqueous medium. 		CA2000786 Compound Janssen Pharmaceutica, N. V No
Patent status
Patent status/countries Low, Low- middle and upper-middle High income
Granted
Filed
Not in force South Africa Canada, Australia, Chile, Cyprus, Germany, Denmark, Liechtenstein, Italy, Belgium, United Kingdom, Greece, Netherlands, Switzerland, Spain, Austria, France, Luxembourg, Sweden, Finland, Hong Kong, Ireland, Israel, Japan, Korea, Republic of, Norway, New Zealand, Portugal, United States of America

Supporting material

Publications

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Useful links

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Access principles

Collaborate for development

Consider on a case by case basis, collaborating on developing long acting products with potential significant public health impact, especially for low- and middle-income countries (LMICs), utilising the referred to long-acting technology

Not provided

Share technical information for match-making assessment

Provide necessary technical information to a potential partner, under confidentiality agreement, to enable preliminary assessment of whether specific medicines of public health importance in LMICs might be compatible with the referred to long-acting technology to achieve a public health benefit

Not provided

Work with MPP to expand access in LMICs

In the event that a product using the referred to long-acting technology is successfully developed, the technology IP holder(s) will work with the Medicines Patent Pool towards putting in place the most appropriate strategy for timely and affordable access in low and middle-income countries, including through licensing

Not provided

Comment & Information

Not provided