Chemistry:Paliperidone palmitate

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Short description: Atypical antipsychotic medication

Paliperidone palmitate
Clinical data
Trade namesInvega Hayfera, Invega Sustenna, Invega Trinza, others
Other namesPP; PP1M; PP3M; PP6M; JNS-010; RO-92670; RO92670
MedlinePlusa607005
License data
Routes of
administration		Intramuscular
Drug classAtypical antipsychotic
Legal status
Legal status
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC39H57FN4O4
Molar mass664.907 g·mol−1
3D model (JSmol)

Paliperidone palmitate (PP), sold under the brand names Invega Sustenna, Xeplion, Shansida (Chinese: 善思达), Erzofri and Psokadron for the once‑monthly formulation, and as Invega Trinza/Trevicta (three‑monthly) and Invega Hafyera/Byannli (six‑monthly), is a long-acting injectable atypical antipsychotic of the benzisoxazole class, used in the treatment of schizophrenia and schizoaffective disorder.[1][6][7] The original product was developed by Janssen Pharmaceuticals, Inc. (Johnson & Johnson), which continues to manufacture most of the branded versions worldwide. It is an antipsychotic ester – specifically the palmitate ester of paliperidone – and acts as a long-lasting form of paliperidone.[7] Paliperidone palmitate is formulated as an aqueous suspension, has a strong smell similar to alcohol, and is administered by intramuscular injection into deltoid or gluteal muscle once every 1, 3, or 6 months depending on the formulation.[7][7][8][6] A formulation for injection once every 6 months is also pending regulatory approval as of September 2021.[6][9]

Pharmacokinetics

With the once-monthly formulation of paliperidone palmitate, the time to peak is 13 days and the elimination half-life is 25 to 49 days; for the 3-month formulation, the time to peak is 30 to 33 days and the half-life is 84 to 95 days (deltoid muscle) or 118 to 139 days (gluteal). These data come from a 2021 review whose authors included employees of Janssen Research & Development, the manufacturer of paliperidone palmitate.[10] The peak-to-trough ratio of paliperidone palmitate at steady state ranges from 1.56 to 1.70 with the 1- and 3-month formulations.[10] No pharmacokinetic data for the 6-month formulation has been released as of January 2021.[11]

However, a 2025 case report described a patient who still had measurable plasma paliperidone concentrations in the low therapeutic range 886 days (2.5 years) after her last injection, indicating that in some individuals the drug may be released from the depot far longer than the predicted half‑life.[12]

The pharmacokinetic profile was originally derived from a 2009 pooled analysis of 18,530 paliperidone concentration samples from 1,795 subjects across six Phase I trials and five Phase II and III trials funded by Johnson & Johnson Pharmaceutical Research and Development, LLC.[13]

Invega Sustenna, Invega Trinza, and Invega Hafyera all utilize nanoparticle technology.[14] The NanoCrystal® technology used in all three long-acting paliperidone products is manufactured by Alkermes plc. The technology was originally developed by Elan Drug Technologies, a business unit of Elan Corporation, plc; Alkermes acquired the technology when it purchased Elan's drug delivery unit in 2011 for approximately $960 million.[15] Nanocrystals of paliperidone palmitate form a depot in the muscle. The 3-month formulation of paliperidone palmitate, Invega Trinza or Trevicta, has larger crystal sizes than the 1-month formulation, which dissolve more slowly at the injection site, allowing for its longer duration.[11]

v · d · e Pharmacokinetics of long-acting injectable antipsychotics
Medication Brand name Class Vehicle Dosage Tmax t1/2 single t1/2 multiple logPc Ref
Aripiprazole lauroxil Aristada Atypical Watera 441–1064 mg/4–8 weeks 24–35 days ? 54–57 days 7.9–10.0
Aripiprazole monohydrate Abilify Maintena Atypical Watera 300–400 mg/4 weeks 7 days ? 30–47 days 4.9–5.2
Bromperidol decanoate Impromen Decanoas Typical Sesame oil 40–300 mg/4 weeks 3–9 days ? 21–25 days 7.9 [16]
Clopentixol decanoate Sordinol Depot Typical Viscoleob 50–600 mg/1–4 weeks 4–7 days ? 19 days 9.0 [17]
Flupentixol decanoate Depixol Typical Viscoleob 10–200 mg/2–4 weeks 4–10 days 8 days 17 days 7.2–9.2 [17][18]
Fluphenazine decanoate Prolixin Decanoate Typical Sesame oil 12.5–100 mg/2–5 weeks 1–2 days 1–10 days 14–100 days 7.2–9.0 [19][20][21]
Fluphenazine enanthate Prolixin Enanthate Typical Sesame oil 12.5–100 mg/1–4 weeks 2–3 days 4 days ? 6.4–7.4 [20]
Fluspirilene Imap, Redeptin Typical Watera 2–12 mg/1 week 1–8 days 7 days ? 5.2–5.8 [22]
Haloperidol decanoate Haldol Decanoate Typical Sesame oil 20–400 mg/2–4 weeks 3–9 days 18–21 days 7.2–7.9 [23][24]
Olanzapine pamoate Zyprexa Relprevv Atypical Watera 150–405 mg/2–4 weeks 7 days ? 30 days –
Oxyprothepin decanoate Meclopin Typical ? ? ? ? ? 8.5–8.7
Paliperidone palmitate Invega Sustenna Atypical Watera 39–819 mg/4–12 weeks 13–33 days 25–139 days ? 8.1–10.1
Perphenazine decanoate Trilafon Dekanoat Typical Sesame oil 50–200 mg/2–4 weeks ? ? 27 days 8.9
Perphenazine enanthate Trilafon Enanthate Typical Sesame oil 25–200 mg/2 weeks 2–3 days ? 4–7 days 6.4–7.2 [25]
Pipotiazine palmitate Piportil Longum Typical Viscoleob 25–400 mg/4 weeks 9–10 days ? 14–21 days 8.5–11.6 [18]
Pipotiazine undecylenate Piportil Medium Typical Sesame oil 100–200 mg/2 weeks ? ? ? 8.4
Risperidone Risperdal Consta Atypical Microspheres 12.5–75 mg/2 weeks 21 days ? 3–6 days –
Zuclopentixol acetate Clopixol Acuphase Typical Viscoleob 50–200 mg/1–3 days 1–2 days 1–2 days 4.7–4.9
Zuclopentixol decanoate Clopixol Depot Typical Viscoleob 50–800 mg/2–4 weeks 4–9 days ? 11–21 days 7.5–9.0
Note: All by intramuscular injection. Footnotes: a = Microcrystalline or nanocrystalline aqueous suspension. b = Low-viscosity vegetable oil (specifically fractionated coconut oil with medium-chain triglycerides). c = Predicted, from PubChem and DrugBank. Sources: Main: See template.

History

Paliperidone palmitate was first approved by the United States Food and Drug Administration (FDA) on July 31, 2009, under the brand name Invega Sustenna, for the acute and maintenance treatment of schizophrenia in adults.[26] Health Canada followed on June 30, 2010, issuing a Notice of Compliance for the same indication.[27] Australia's Therapeutic Goods Administration registered the product on July 28, 2010.[28] The European Medicines Agency (EMA) authorized the once‑monthly injection under the brand name Xeplion on March 4, 2011. In China, the drug was approved in January 2012 and launched later that year under the brand name Shansida (善思达);[29] marketed by Xian-Janssen Pharmaceutical Limited (which is the Janssen (Johnson & Johnson) subsidiary in China), it was the first once-monthly long-acting injectable atypical antipsychotic available in the country.[30][31] The approval was based on a multi-center clinical trial funded by Xian-Janssen Pharmaceutical Ltd. which demonstrated that Shansida monotherapy was non-inferior to a combination of oral risperidone and long-acting injectable risperidone microspheres (brand name Risperdal Consta) for acute schizophrenia.[30] In Japan, the once‑monthly injection was approved in September 2013 under the brand name Xeplion (ゼプリオン, Zepurion) and was launched on November 19, 2013.[32][33]

Globally, the paliperidone palmitate long-acting injectable market was valued at approximately US$4.1 billion in 2024 and is projected to reach US$6.3 billion by 2031.[34] In the United States alone, sales of the Invega franchise (including Sustenna, Trinza, and Hafyera) reached $3.1 billion in 2024, an 8% increase over the previous year.[35] The market is served primarily by Janssen Pharmaceuticals, with generic competition expected to begin after the key U.S. patent expires on January 26, 2031.[36]

Society and culture

FDA label expansion and marketing controversy

In January 2018, the U.S. Food and Drug Administration (FDA) expanded the label for Invega Sustenna to state that the drug "may delay time to arrest and/or incarceration" in patients with schizophrenia. The revised label was based on the Paliperidone Palmitate Research in Demonstrating Effectiveness (PRIDE) study, a Janssen‑sponsored, open‑label, 15‑month trial that enrolled 444 adults aged 18 to 65 who had been taken into custody at least twice in the previous two years, and at least once in the prior 90 days; about 60% had a concurrent substance use disorder and 14% were homeless.[37][38] Participants were randomized to once‑monthly paliperidone palmitate or one of seven daily oral antipsychotics. The study, conducted between May 2010 and December 2013, found a significantly longer time to treatment failure—a composite measure that included arrest and/or incarceration, psychiatric hospitalization, treatment discontinuation because of safety or tolerability, treatment supplementation because of inadequate efficacy, need for increased psychiatric services to prevent hospitalization, and suicide—in the injectable group than in the oral antipsychotic group.[39][40]

The label expansion, which granted Janssen three additional years of market exclusivity for paliperidone palmitate, attracted significant criticism from mental health experts and the media. In February 2018, The Marshall Project published an investigation reporting that the new label allowed Johnson & Johnson to market Invega Sustenna as a way to keep people out of prison or jail. John Snook, executive director of the Treatment Advocacy Center, described the "stay-out-of-jail" marketing approach as a "depressing commentary" on the state of mental health treatment. Critics noted that the PRIDE study did not compare Invega Sustenna with other long-acting injectable antipsychotics, only with daily oral antipsychotics, and that the reduced rate of incarceration was likely due to improved drug adherence rather than a unique property of paliperidone palmitate.[41][42]

A 2022 review of internal pharmaceutical industry documents, published in the Journal of Correctional Health Care, identified Janssen as one of at least two companies that directly marketed antipsychotics to jails and prisons to increase sales. The review found that marketing strategies included targeted promotions, indirect "educational" advertising, and efforts to influence state formulary advisory boards.[43]

Deaths

In April 2014, it was reported that 21 Japanese people who had received shots of the long-acting injectable paliperidone palmitate had died, out of 10,700 individuals prescribed the drug.[44][45][46][47][48][49][50]

An observational study of the French pharmacovigilance database reviewed 473 adverse drug reaction reports linked to paliperidone palmitate between 1 January 2013 and 31 December 2019. The investigators identified 13 deaths and 14 life‑threatening events linked to paliperidone palmitate. The reactions were primarily cardiorespiratory, with cardiac arrests and sudden unexpected deaths often occurring 10–14 days after a once‑monthly injection (or 11–24 days after a three‑monthly injection), consistent with peak plasma drug levels. The authors hypothesised that supratherapeutic drug levels may underlie these events.[51]

A 2017 case report details the severe, prolonged episode of drug-induced parkinsonism in a 68‑year‑old man that ultimately led to his death roughly five months after receiving two injections of paliperidone palmitate (234 mg followed one week later by 156 mg). The authors state that "practitioners should be cognizant of the potential long‑term consequences of paliperidone LAI."[52]

A 47‑year‑old man (Japan, 2017) developed acute and persistent circulatory failure after receiving paliperidone palmitate injections. Despite surgical resection of the hip tissue suspected of containing the depot, he died of multiple organ failure.[53]

In 2019, it was reported that a 33-year-old man in France was found dead in his room at his parents' home after receiving a single 819 mg injection of Trevicta (paliperidone palmitate three‑monthly formulation). Toxicological analysis of femoral blood revealed paliperidone at 240 μg/L; no other substance was detected. The authors concluded that paliperidone poisoning was the highly likely cause of death.[54]

A 2021 case report documented a 72‑year‑old woman with Lewy body dementia who developed fatal neuroleptic malignant syndrome (NMS) after receiving a single 156 mg intramuscular injection of paliperidone palmitate.[55] Multiple additional case reports of NMS linked to paliperidone palmitate have been published, including a 63-year-old man (2025) who survived after treatment, and cases in a 29-year-old woman who developed severe, treatment‑refractory NMS after two doses of paliperidone palmitate (2025) and a 24-year-old man (2025).

Suicides and homicides

On January 17, 2020, a video titled "Medical Help" was uploaded to YouTube by 26-year-old Wail Ardab of Palatka, Florida, who developed severe dystonia and insomnia after taking Invega Trinza injections.[56] On March 5, 2020, Ardab committed suicide by jumping from Memorial Bridge in Palatka.[57]

From June 2023 to April 2024, Serbian television presenter Bojana Janković (née Nikolić), known for hosting the show City, posted to the internet forum Bluelight that she was bedridden with symptoms consistent with neuroleptic-induced deficit syndrome after receiving six depot injections of paliperidone palmitate (four shots of Invega Sustenna and two shots of Invega Trinza). She wrote: "My main problem is 0 motivation, low energy and anhedonia. Also i have cognitive issues. Beddriden mostly..."[58][59] The injections were prescribed by her private psychiatrist and friend around the time of her divorce from Ognjen Janković, a member of the hip-hop group Beogradski Sindikat. She died by suicide in Belgrade on April 19, 2024, aged 46.[60]

On December 28, 2021, 19-year-old Peyton Moyer fatally shot his mother and her boyfriend in Watkinsville, Georgia, while under the influence of the long-acting injectable paliperidone palmitate (Invega Sustenna).[61] On November 2, 2023, Moyer was sentenced to life in prison.[62]

Lawsuits

From 2019 to 2024, Maria Francesca Gioia, a former medical student acting as a pro se plaintiff, filed nine product liability lawsuits against Janssen Pharmaceuticals and related parties. She alleged that taking Invega Sustenna (paliperidone palmitate) caused her memory loss, hypothyroidism, Horner's syndrome, nerve damage, motor tremors, vocal tics, confusion, loss of taste and sensation, post-traumatic stress disorder, and metabolic syndrome (including hypertension, diabetes, and stroke), which ended her career as a primary care physician.[63] All nine lawsuits were dismissed on procedural grounds: Gioia I–II for failure to state a claim, Gioia III for failure to prosecute, and Gioia IV–V for lack of subject matter jurisdiction. The court also noted that the side effects she alleged were already listed on Invega's FDA-approved warning label.[64]

In June 2020, a Florida lawsuit was filed on behalf of Lilith Geohaghan, an 82-year-old assisted living resident with Lewy body dementia, against the assisted living facility and several healthcare providers. The complaint alleged that despite her family's explicit instructions to the contrary, she was administered multiple large doses of Invega Sustenna in late 2018. The lawsuit claims that the injections led to a rapid decline in her health, resulting in nearly a dozen falls and two hospitalizations within just over a month. Her treating physicians subsequently diagnosed her with toxic encephalopathy, directly attributing the condition to the Invega Sustenna injections. The complaint further alleged that the injections caused a permanent loss of mobility and function from which she never recovered, describing the use of the drug as a form of "chemical restraint" and outside the standard of care. The case highlights concerns about the off-label use of antipsychotics in elderly dementia patients, a practice for which the drug carries a black box warning from the FDA due to an increased risk of death.[65]

In May and June 2022, Adilah Patton, a 28‑year‑old pretrial detainee in Indianapolis, was forcibly injected twice with Invega Sustenna while in custody at the Marion County Adult Detention Center. A federal lawsuit filed on her behalf alleges that the injections were administered without a medical assessment, a prescription, or the consent of her court‑appointed guardian. The lawsuit describes the injections as assault, battery, excessive force, and violations of the Fourteenth Amendment right to informed consent.[66][67]

In September 2024, Haitian immigrant Cassandra Fameux filed a criminal complaint alleging that her husband, Michigan anesthesiologist Dr. Paul Gregory St. Claire, and psychiatrist Dr. Dominic Barberio forcibly injected her monthly from 2017 to 2021 with unprescribed Invega Sustenna—sometimes at doses up to 256 mg—as "punishment" when her husband was angry. Divorce court testimony and a recorded conversation indicate Barberio admitted she was not schizophrenic; two psychiatrists found she had PTSD, not bipolar disorder or schizophrenia. A subsequent police investigation led to a recommendation that her husband be charged with domestic assault.[68]

Brand names

In May 2015, a formulation of paliperidone palmitate was approved by the U.S. Food and Drug Administration under the brand name Invega Trinza.[69][2] A similar prolonged release suspension was approved in 2016 by the European Medicines Agency originally under the brand name Paliperidone Janssen, later renamed to Trevicta.[70] In September 2021, a newer formulation of paliperidone palmitate, Invega Hafyera, was approved by the US FDA.[3]

References

  1. ↑ 1.0 1.1 "Invega Sustenna- paliperidone palmitate injection". 31 January 2019. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1af14e42-951d-414d-8564-5d5fce138554. 
  2. ↑ 2.0 2.1 "Invega Trinza- paliperidone palmitate injection, suspension, extended release". 31 January 2019. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c39e65d7-fa44-4e4c-8b12-a654d3ed0eae. 
  3. ↑ 3.0 3.1 "Invega Hafyera- paliperidone palmitate injection, suspension, extended release". https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=6cd61892-d2cb-434d-83ed-5c1b2c4e7a0b. 
  4. ↑ "Byannli EPAR". 28 April 2020. https://www.ema.europa.eu/en/medicines/human/EPAR/byannli-previously-paliperidone-janssen-cilag-international. 
  5. ↑ "Byannli Product information". https://ec.europa.eu/health/documents/community-register/html/h1453.htm. 
  6. ↑ 6.0 6.1 6.2 "Paliperidone palmitate - Johnson & Johnson - AdisInsight". https://adisinsight.springer.com/drugs/800040526. 
  7. ↑ 7.0 7.1 7.2 7.3 "A review of paliperidone palmitate". Expert Review of Neurotherapeutics 12 (12): 1383–1397. December 2012. doi:10.1586/ern.12.137. PMID 23237346. 
  8. ↑ "Paliperidone 3-Month Injection for Treatment of Schizophrenia: A Narrative Review". Frontiers in Psychiatry 12. 2021. doi:10.3389/fpsyt.2021.699748. PMID 34621193. 
  9. ↑ "Paliperidone Palmitate 6-month (PP6M)". Archives of Psychiatry Research 57 (2): 229–232. 1 June 2021. doi:10.20471/dec.2021.57.02.13. ISSN 2671-1079. 
  10. ↑ 10.0 10.1 "Pharmacokinetic Characteristics of Long-Acting Injectable Antipsychotics for Schizophrenia: An Overview". CNS Drugs 35 (1): 39–59. January 2021. doi:10.1007/s40263-020-00779-5. PMID 33507525. 
  11. ↑ 11.0 11.1 "Therapeutic Drug Monitoring of Long-Acting Injectable Antipsychotic Drugs". Therapeutic Drug Monitoring 43 (1): 79–102. February 2021. doi:10.1097/FTD.0000000000000830. PMID 33196621. 
  12. ↑ "Paliperidone poisoning and measurable plasma concentrations 2.5 years after last administered dose: A case report". British Journal of Clinical Pharmacology 91 (6): 1580–1585. June 2025. doi:10.1111/bcp.16036. PMID 38450747. 
  13. ↑ "Population pharmacokinetics of intramuscular paliperidone palmitate in patients with schizophrenia: a novel once-monthly, long-acting formulation of an atypical antipsychotic". Clinical Pharmacokinetics 48 (9): 585–600. 2009. doi:10.2165/11316870-000000000-00000. PMID 19725593. 
  14. ↑ "Invega Sustenna vs Invega Trinza vs Invega Hafyera. What's the difference?". 2024-09-25. https://www.drugs.com/medical-answers/invega-sustenna-invega-trinza-invega-hafyera-3562432/. 
  15. ↑ "J&J trumpets early success for 3-month Invega Sustenna PhIII schizophrenia trial". FierceBiotech. 2014-03-20. https://www.fiercebiotech.com/r-d/j-j-trumpets-early-success-for-3-month-invega-sustenna-phiii-schizophrenia-trial. 
  16. ↑ "Long-term treatment of chronic psychotics with bromperidol decanoate: clinical and pharmacokinetic evaluation.". Current Therapeutic Research 34 (1): 1–6. 1983. 
  17. ↑ 17.0 17.1 "Clopenthixol and flupenthixol depot preparations in outpatient schizophrenics. III. Serum levels". Acta Psychiatrica Scandinavica. Supplementum 279: 41–54. 1980. doi:10.1111/j.1600-0447.1980.tb07082.x. PMID 6931472. 
  18. ↑ 18.0 18.1 "Anxiolytic sedatives, hypnotics and neuroleptics.". Martindale: The Extra Pharmacopoeia (30th ed.). London: Pharmaceutical Press. 1993. pp. 364–623. 
  19. ↑ "Future of depot neuroleptic therapy: pharmacokinetic and pharmacodynamic approaches". The Journal of Clinical Psychiatry 45 (5 Pt 2): 50–9. May 1984. PMID 6143748. 
  20. ↑ 20.0 20.1 "Kinetics of fluphenazine after fluphenazine dihydrochloride, enanthate and decanoate administration to man". British Journal of Clinical Pharmacology 7 (4): 325–31. April 1979. doi:10.1111/j.1365-2125.1979.tb00941.x. PMID 444352. 
  21. ↑ "Explaining the pharmacokinetics of fluphenazine through computer simulations. (Abstract.)". 19th Annual Midyear Clinical Meeting of the American Society of Hospital Pharmacists.. Dallas, Texas. 1984. 
  22. ↑ "The pharmacology of fluspirilene (R 6218), a potent, long-acting and injectable neuroleptic drug". Arzneimittel-Forschung 20 (11): 1689–98. November 1970. PMID 4992598. 
  23. ↑ "Haloperidol decanoate. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in psychosis". Drugs 33 (1): 31–49. January 1987. doi:10.2165/00003495-198733010-00002. PMID 3545764. 
  24. ↑ "Pharmacokinetics of haloperidol decanoate. A 2-year follow-up". International Pharmacopsychiatry 17 (4): 238–46. 1982. doi:10.1159/000468580. PMID 7185768. 
  25. ↑ "On the pharmacokinetics of perphenazine: a clinical study of perphenazine enanthate and decanoate.". Current Therapeutic Research 36 (6): 1071–88. 1984. 
  26. ↑ "Drug Approval Package: INVEGA SUSTENNA (paliperidone palmitate)". U.S. Food and Drug Administration. 2009-07-31. https://www.accessdata.fda.gov/drugsatfda_docs/nda/2009/022264_invega_sustenna_toc.html. 
  27. ↑ "Summary Basis of Decision for Invega Sustenna". Health Canada. 2010-11-01. https://dhpp.hpfb-dgpsa.ca/review-documents/resource/SBD00076. 
  28. ↑ myHealthbox. "INVEGA SUSTENNA paliperidone (as palmitate) 75 mg modified release suspension for injection pre-filled syringe". https://myhealthbox.eu/en/invega-sustenna/4486144. 
  29. ↑ "善思达（棕榈酸帕利哌酮注射液）" (in zh). 2011-12-19. https://drugs.dxy.cn/drug/DRU1505267690737867. 
  30. ↑ 30.0 30.1 "精神分裂症长效针剂善思达上市 [Long-acting injectable Shansida for schizophrenia launched"] (in zh). 2012-06-15. https://m.medlive.cn/cms/research/42158. 
  31. ↑ "CAFC维持Janssen重磅抗精神病药物棕榈酸帕利哌酮的给药方案专利有效" (in zh). 2025-07-28. https://vdev.tip-lab.com/cafc-upheld-janssen-patent-invega-sustenna/. 
  32. ↑ "XEPLION® Aqueous Suspension for IM Injection". Drug Delivery System 31 (5): 469–475. 2016. doi:10.2745/dds.31.469. "Paliperidone palmitate long-acting injection (Xeplion® aqueous suspension for IM injection, PP) is the long-acting injectable antipsychotic for schizophrenia, which approved in Japan on September 2013.". 
  33. ↑ "17 deaths reported in Japan after drug injections". Business Standard. 2014-04-09. https://www.business-standard.com/article/pti-stories/17-deaths-reported-in-japan-after-drug-injections-114040901001_1.html. "The drug, brand-named Xeplion, is estimated to have been used by 10,700 people since it was released in Japan on November 19…" 
  34. ↑ "Paliperidone Palmitate Long-Acting Injection - Global Market Share and Ranking, Overall Sales and Demand Forecast 2025-2031". 2025-04-25. https://www.qyresearch.com/reports/4717715/paliperidone-palmitate-long-acting-injection. 
  35. ↑ "Johnson & Johnson (JNJ) Wins Patent Dispute Over Invega Sustenna". GuruFocus. 2025-07-09. https://www.gurufocus.com/news/2967150/johnson-johnson-jnj-wins-patent-dispute-over-invega-sustenna. 
  36. ↑ "When do the INVEGA SUSTENNA patents expire, and when will INVEGA SUSTENNA go generic?". 2026-04-07. https://www.drugpatentwatch.com/blog/when-do-invega-sustenna-patents-expire/. 
  37. ↑ "Design and rationale of the Paliperidone Palmitate Research in Demonstrating Effectiveness (PRIDE) study: a novel comparative trial of once-monthly paliperidone palmitate versus daily oral antipsychotic treatment for delaying time to treatment failure in persons with schizophrenia". The Journal of Clinical Psychiatry 75 (12): 1388–1393. December 2014. doi:10.4088/JCP.13m08965. PMID 25375367. 
  38. ↑ "New Label for LAI Paliperidone Breaks FDA Ground by Including Real-World Data". Psychiatric News (American Psychiatric Association) 53 (7). 2018-02-16. doi:10.1176/appi.pn.2018.pp2b5. https://psychiatryonline.org/doi/full/10.1176/appi.pn.2018.pp2b5. 
  39. ↑ "Real-world outcomes of paliperidone palmitate compared to daily oral antipsychotic therapy in schizophrenia: a randomized, open-label, review board-blinded 15-month study". Journal of Clinical Psychiatry 76 (5): 554–561. 2015. doi:10.3791/52781. PMID 25938576. 
  40. ↑ "Landmark Schizophrenia Data That Brings Hope in Breaking the Cycle of Hospitalization and Incarceration Receives FDA Approval for Inclusion in INVEGA SUSTENNA® (paliperidone palmitate) Label" (Press release). Janssen Pharmaceuticals, Inc. 2018-01-03. Retrieved 2026-05-27 – via JNJ.com.
  41. ↑ "A Drug Company Says This Shot Will Keep You Out of Prison". The Marshall Project. 2018-02-14. https://www.themarshallproject.org/2018/02/14/a-drug-company-says-this-shot-will-keep-you-out-of-prison. 
  42. ↑ "Johnson & Johnson's stay-out-of-jail marketing for schizophrenia blockbuster Invega Sustenna raises eyebrows". FiercePharma. 2018-02-15. https://www.fiercepharma.com/regulatory/j-j-s-stay-out-jail-marketing-plan-for-schizophrenia-blockbuster-raises-eyebrows. 
  43. ↑ "Marketing Antipsychotics to Correctional Facilities: A Review of Pharmaceutical Industry Documents". Journal of Correctional Health Care 28 (5): 325–328. October 2022. doi:10.1089/jchc.21.04.0026. PMID 36190495. 
  44. ↑ "21 users of schizophrenia drug dead". The Japan Times Online (The Japan Times). April 18, 2014. http://www.japantimes.co.jp/news/2014/04/18/national/21-users-of-schizophrenia-drug-dead/#.U1U0EcfgVQY. 
  45. ↑ "Schizophrénie: controverse autour d'un médicament au Japon". Médecine. April 9, 2014. http://www.lapresse.ca/sciences/medecine/201404/09/01-4755962-schizophrenie-controverse-autour-dun-medicament-au-japon.php. 
  46. ↑ "20 minutes - Un médicament anti-schizophrénie tue". 20 minutes. April 9, 2014. http://www.20min.ch/ro/news/monde/story/M-doc-anti-schizophr-nie-fait-17-morts-25477540. 
  47. ↑ "Deaths reported after Xeplion injections". Life & Style. NZ Herald News. http://www.nzherald.co.nz/lifestyle/news/article.cfm?c_id=6&objectid=11235899. 
  48. ↑ Japan Today (April 10, 2014). "17 deaths reported after schizophrenia drug injections". http://www.japantoday.com/category/national/view/17-deaths-reported-after-schizophrenia-drug-injections. 
  49. ↑ Kermit Cole (April 18, 2014). "21 Dead in Japan From New Johnson & Johnson Antipsychotic". https://www.madinamerica.com/2014/04/21-dead-japan-new-antipsychotic/. 
  50. ↑ "Schizophrenia drug blamed for 17 deaths". June 29, 2023. http://www.skynews.com.au/health/article.aspx?id=966055. 
  51. ↑ "Fatal and life-threatening ADRs associated with paliperidone palmitate: an observational study in the French pharmacovigilance database". Clinical Toxicology 59 (9): 786–793. September 2021. doi:10.1080/15563650.2021.1878206. PMID 33555955. 
  52. ↑ "Drug-induced parkinsonism: A case report". The Mental Health Clinician 7 (2): 65–68. March 2017. doi:10.9740/mhc.2017.03.065. PMID 29955500. 
  53. ↑ "The possibility of the treatment for long-acting injectable antipsychotics induced severe side effects". The American Journal of Emergency Medicine 35 (8): 1211.e1–1211.e2. August 2017. doi:10.1016/j.ajem.2017.04.063. PMID 28460810. 
  54. ↑ "Death following an intramuscular injection of paliperidone: A case report". Toxicologie Analytique et Clinique 32 (2): 132–136. November 2019. doi:10.1016/j.toxac.2019.10.006. https://www.researchgate.net/publication/337356064. Retrieved November 5, 2025. 
  55. ↑ "Development of Neuroleptic Malignant Syndrome in a Patient with Lewy Body Dementia after Intramuscular Administration of Paliperidone". Case Reports in Neurological Medicine 2021: 1–4. 2021. doi:10.1155/2021/8879333. PMID 33489400. 
  56. ↑ Ardab W (January 17, 2020). Medical Help. YouTube. Retrieved November 5, 2025.
  57. ↑ "Dive team recovers body from river". Palatka Daily News (Palatka, Florida). March 6, 2020. https://www.palatkadailynews.com/dive-team-recovers-body-river. 
  58. ↑ bojana, post to "Coming off Invega/Xeplion (paliperidone) injections v 8.0," Bluelight, December 24, 2023, https://www.bluelight.org/community/threads/coming-off-invega-xeplion-paliperidone-injections-v-8-0.934528/post-15958591. "So im 10 months off. I have some emotions, i can cry, lost weight, listen to some music. My main problem is 0 motivation, low energy and anhedonia. Also i have cognitive issues. Beddriden mostly.. When do you think it will go away? Im loosing hope"
  59. ↑ bojana, post to "Coming off Invega/Xeplion (paliperidone) injections v 8.0," Bluelight, March 3, 2024, https://www.bluelight.org/community/threads/coming-off-invega-xeplion-paliperidone-injections-v-8-0.934528/post-16002558. "They really killed everything in me and about me, im different person who suffers enormasly every day. I juste believed medical doctros and their knowledge. […] I dont accept undignefied life, i was mother, jurnalist, tv host, happiest women ever who adored life, kids, family, friends. Everything is gone. Everything. Somehow deep in my heart i have small hope of being my self again, its just that i am tiered and i had way to much suffering. Life is not worth living anymore, and i cant allowe everybody around me to suffer with me. Id rather be dead, than be this person who i have become."
  60. ↑ "DECU POSLALA IZ KUĆE, PA OTIŠLA U SMRT! Isplivali novi detalji o Bojani Nikolić! Ugovarala jednu stvar sa sestrom, žalila se NA OVE SIMPTOME!" (in Serbian). Republika.rs. April 22, 2024. https://www.republika.rs/zabava/estrada/537062/bojana-nikolic-se-zalila-na-jednu-stvar-pre-smrti. 
  61. ↑ "Doomed by Design: How a Dangerous Drug, a Broken System, and a Failing DA Failed A Mentally Ill Teen". The Oklahoma Post. March 27, 2025. https://theokpost.com/civil-rights/doomed-by-design-how-a-dangerous-drug-a-broken-system-and-a-failing-da-failed-a-mentally-ill-teen/2025/03/27/. 
  62. ↑ "Watkinsville man sentenced to life in prison for killing parents in 2021". Athens Banner-Herald (Athens, Georgia). November 2, 2023. https://www.onlineathens.com/story/news/crime/2023/11/02/watkinsville-man-pleads-guilty-to-murdering-parents-in-2021/71424119007/. 
  63. ↑ Gioia v. Janssen Pharmaceuticals, 19-CV-04629 (E.D.N.Y. February 16, 2021).
  64. ↑ Gioia v. Patterson, Belknap, Webb & Tyler, 2:23-cv-08163 (E.D.N.Y. April 19, 2024).
  65. ↑ "Invega Sustenna Lawsuit Claims Nursing Home Illegally Injected Dementia Resident With Antipsychotic Drug". AboutLawsuits.com. 2020-06-15. https://www.aboutlawsuits.com/invega-sustenna-chemical-restraint-lawsuit-172937/. 
  66. ↑ "Lawsuit alleges mentally ill woman received forced injections while detained by Marion County authorities". The Indiana Lawyer. 2024-06-11. https://www.theindianalawyer.com/articles/lawsuit-alleges-mentally-ill-woman-received-forced-injections-while-detained-by-marion-county-authorities. 
  67. ↑ "Marion County sheriff, Wellpath accused of forced drug injections on mentally ill inmate". The Indianapolis Star. 2024-06-11. https://www.indystar.com/story/news/investigations/2024/06/11/marion-county-sheriff-wellpath-accused-forced-drug-injections-inmate-mentally-ill-indianapolis/74055346007/. 
  68. ↑ "From Hotel Lobby To Psychiatric Ward: The Troubling Ordeal Of Cassandra Fameux". Black Star News. 7 March 2026. https://blackstarnews.com/from-hotel-lobby-to-psychiatric-ward-cassandra-fameux/. 
  69. ↑ "Invega Trinza (paliperidone palmitate) NDA approval letter". http://www.accessdata.fda.gov/drugsatfda_docs/appletter/2015/207946Orig1s000ltr.pdf. 
  70. ↑ "Trevicta (previously Paliperidone Janssen)". Summary of the European public assessment report (EPAR) for Trevicta. EMC. September 17, 2018. http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/004066/human_med_001829.jsp&mid=WC0b01ac058001d124. 



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