Paliperidone Palmitate

Summary

Paliperidone Palmitate (CHEMBL2107360) is an approved small molecule; indicated across 2 conditions including schizoaffective disorder.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Indications: 2 conditions
• Clinical trials: 45
• Chemistry: 664.9 Da · C39H57FN4O4

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2107360
Name	Paliperidone Palmitate
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	9852746
ChEBI	CHEBI:83808
Molecular formula	C39H57FN4O4
Molecular weight	664.9
InChIKey	VOMKSBFLAZZBOW-UHFFFAOYSA-N

SMILES: CCCCCCCCCCCCCCCC(=O)OC1CCCN2C1=NC(=C(C2=O)CCN3CCC(CC3)C4=NOC5=C4C=CC(=C5)F)C

IUPAC name: [3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-9-yl] hexadecanoate

ChEBI definition: A fatty acid ester obtained by the formal condensation of the carboxy group of hexadecanoic acid with the hydroxy group of 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one.

Also known as: Erzofri, Invega sustenna, Invega trinza, JNS-010, JNS010, Niapelf, Paliperidone janssen, Paliperidone palmitate, Palperidone palmitate, R-092670, R092670, RO-92670

Parent form; salt/anhydrous children: CHEMBL4745890

Patent coverage: 166 distinct patent families (467 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 347 (74%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

No target linkage available.

Bioactivity

No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

2 indications (2 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
schizoaffective disorder	4	MONDO:0005487	EFO:0005411

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 45.

Phase distribution

Phase	Trials
PHASE3	17
PHASE4	13
Not specified	7
PHASE1	5
PHASE2	2
PHASE1/PHASE2	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00946985	PHASE4	TERMINATED	28-30 Month Study Comparing Paliperidone Palmitate With Oral Risperidone for Treating Adults Diagnosed With Schizophrenia Within the Past 5 Years
NCT01136772	PHASE4	COMPLETED	A Comparison of Long-acting Injectable Medications for Schizophrenia
NCT01157351	PHASE4	COMPLETED	15 Month Study for Adults Who Have Been Diagnosed With Schizophrenia and Incarcerated
NCT01193166	PHASE4	WITHDRAWN	Twelve Month Study Comparing Paliperidone Palmitate and Select Oral Antipsychotics in Adults With Schizophrenia Who Have Been Recently Discharged From an Inpatient Psychiatric Hospital
NCT01211704	PHASE4	WITHDRAWN	Paliperidone Palmitate Efficacy and Safety in Bipolar Disorder Complicated by Alcoholism
NCT01451736	PHASE4	COMPLETED	Oral Risperidone Versus Injectable Paliperidone Palmitate for Treating First-Episode Schizophrenia
NCT01527305	PHASE4	COMPLETED	A Study to Evaluate the Effectiveness and Safety of Paliperidone Palmitate in Subjects With Acute Schizophrenia
NCT01682161	PHASE4	COMPLETED	A Comparative Study to Evaluate the Evolution of Medication Satisfaction and Adherence in Patients Unsatisfied With Current Oral Atypical Antipsychotics by Switching Medication to Paliperidone Palmitate
NCT01685931	PHASE4	COMPLETED	A Study of Paliperidone Palmitate in Patients With Schizophrenia Previously Unsuccessfully Treated by Oral Antipsychotics
NCT01860781	PHASE4	COMPLETED	The Effect of Paliperidone Palmitate in Schizophrenia
NCT01947803	PHASE4	COMPLETED	A Safety and Effectiveness Study of Paliperidone Palmitate in Chinese Patients With Schizophrenia
NCT02146547	PHASE4	COMPLETED	European Long-acting Antipsychotics in Schizophrenia Trial
NCT03080194	PHASE4	UNKNOWN	The Effect of a Community-based LAI-treated Management Model on the Violence Risk of Patients With Schizophrenia
NCT00073320	PHASE3	COMPLETED	Intramuscular Injections of Paliperidone Palmitate in the Arm or Buttock of Subjects With Schizophrenia
NCT00101634	PHASE3	COMPLETED	Efficacy and Safety of a Long Acting Anti-Psychotic Versus Placebo in Patients With Schizophrenia
NCT00111189	PHASE3	COMPLETED	A Study of the Efficacy (Effectiveness) of Paliperidone Palmitate in the Prevention of Recurrence of the Symptoms of Schizophrenia.
NCT00119756	PHASE3	COMPLETED	A Safety and Tolerability Study of Paliperidone Palmitate Injected in the Shoulder or the Buttock Muscle in Patients With Schizophrenia
NCT00210548	PHASE3	COMPLETED	A Study to Evaluate the Effectiveness and Safety of 3 Doses of Paliperidone Palmitate in Treating Subjects With Schizophrenia
NCT00210717	PHASE3	COMPLETED	A Study to Compare the Effectiveness and Safety of Flexibly Varied Doses of Paliperidone Palmitate and Risperidone in Treating Patients With Schizophrenia
NCT00589914	PHASE3	COMPLETED	Comparison of Paliperidone Palmitate and RISPERDAL CONSTA in Patients With Schizophrenia
NCT00604279	PHASE3	COMPLETED	A Comparative Study of Paliperidone Palmitate and Risperidone Long Acting Injection (LAI) in Participants With Schizophrenia
NCT01051531	PHASE3	COMPLETED	A Safety, Tolerability, and Treatment Response Study of Paliperidone Palmitate Administered to Patients With Schizophrenia
NCT01193153	PHASE3	COMPLETED	A Study to Evaluate the Efficacy of Paliperidone Palmitate in the Prevention of Relapse of the Symptoms of Schizoaffective Disorder
NCT01258920	PHASE3	COMPLETED	A Study of Paliperidone Palmitate in Japanese Patients With Schizophrenia
NCT01281527	PHASE3	COMPLETED	Paliperidone Palmitate Flexible Dosing in Schizophrenia
NCT01299389	PHASE3	COMPLETED	An Efficacy and Safety Study of Paliperidone Palmitate in Participants With Schizophrenia
NCT01448720	PHASE3	COMPLETED	Treatment of Patients With Recently Exacerbated Schizophrenia With Paliperidone Palmitate
NCT01795547	PHASE3	COMPLETED	Aripiprazole Once-monthly Versus Paliperidone Palmitate in Adult Patients With Schizophrenia
NCT02713282	PHASE3	COMPLETED	A Study of Transition to the Paliperidone Palmitate 3-Month Formulation In Participants With Schizophrenia Previously Stabilized on the Paliperidone Palmitate 1-Month Formulation
NCT03345979	PHASE3	COMPLETED	A Study of Aripiprazole Lauroxil or Paliperidone Palmitate for the Treatment of Schizophrenia
NCT00074477	PHASE2	COMPLETED	Safety and Efficacy of an Anti-Psychotic in Patients With Schizophrenia
NCT01606254	PHASE2	COMPLETED	A Pharmacokinetic and Safety Study of Paliperidone Palmitate (JNS010) in Participants With Schizophrenia
NCT04754750	PHASE1/PHASE2	COMPLETED	Differences in Schizophrenia With One-month and 3-month Paliperidone Palmitate Treatment
NCT01110317	PHASE1	COMPLETED	A Study of Paliperidone Blood Concentrations in Patients With Schizophrenia After Administration of Paliperidone Palmitate
NCT01559272	PHASE1	COMPLETED	A Study to Assess the Pharmacokinetics, Safety, and Tolerability of Paliperidone Palmitate in Patients With Schizophrenia
NCT01942382	PHASE1	COMPLETED	A Clinical Pharmacology Study of JNS010 (Paliperidone Palmitate) in Patients With Schizophrenia
NCT04572685	PHASE1	COMPLETED	Evaluate the PK of LY03010 Process 1 and Process 2 Drug Product vs INVEGA SUSTENNA After Intramuscular Injection in Schizophrenia Patients
NCT04922593	PHASE1	COMPLETED	Relative Bioavailability of LY03010 Compared to Listed Drug
NCT01362426	Not specified	COMPLETED	Paliperidone Palmitate Effectiveness Assessment Registry - Longitudinal (PEARL)
NCT02600741	Not specified	COMPLETED	Family Intervention in Recent Onset Schizophrenia Treatment (FIRST)

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).