Pharmacokinetics and tolerability of paliperidone palmitate injection in Chinese subjects

Si, Tianmei; Su, Yun-Ai; Liu, Yi; Zhang, Hongyan; Li, Huafang; Qu, Rui; Shen, Liang

doi:10.1002/hup.2388

Cited by 15 publications

(6 citation statements)

References 27 publications

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“…Previous pharmacokinetic studies demonstrated that PP1M achieves therapeutic, steady-state plasma levels rapidly on initiation without the necessity of oral supplementation. 34 Early symptomatic improvement (within a few days) observed with PP1M therapy may be attributed to its unique pharmacokinetics, though the complete therapeutic effect requires several weeks (eg, longer time to relapse with PP1M compared to oral antipsychotics). 24 , 35 – 38 These results are consistent with the association of PANSS reduction at week 5 on better symptomatic outcomes observed in the current study.…”

Section: Discussionmentioning

confidence: 99%

Factors related to improvement of symptoms, function, and caregiver burden in Chinese patients with schizophrenia after switching to paliperidone palmitate once-monthly from oral antipsychotics

Li¹,

Feng²,

Lu³

et al. 2018

NDT

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BackgroundPaliperidone palmitate once-monthly (PP1M) demonstrated symptomatic and functional remission in patients with schizophrenia. This post hoc analysis aimed to identify factors associated with improved clinical outcomes in patients switching to PP1M (75–150 mg eq.).MethodsThe improved patient outcomes were observed as Positive and Negative Symptom Scale (PANSS, symptoms) score <70:66.7% (407/610), Personal and Social Performance (PSP, function) score >70:34.3% (199/581), and Involvement Evaluation Questionnaire (IEQ, caregiver burden) reduction ≥6:50.2% (270/538). Independent variables including demographics, disease duration, employment status, and clinical scores were screened individually using a univariate analysis and subsequently, variables (cutoff p<0.15) were analyzed using a multivariate regression analysis for association with better clinical outcomes at week 13.ResultsThe factors significantly associated with favorable clinical outcomes were reduction in PANSS at week 5 (odds ratio [OR]=1.14, 95% CI=1.11–1.17) with symptom reduction; baseline PSP total score (OR=1.07, 95% CI=1.05–1.10), PSP change at week 5 (OR=1.07, 95% CI=1.05–1.10), PANSS reduction at week 5 (OR=1.06, 95% CI=1.03–1.08) with functional improvement, reduction in PANSS at week 5 (OR=1.02, 95% CI=1.01–1.03), and total IEQ score at baseline (OR=1.09, 95% CI=1.07–1.11) with caregiver burden reduction.ConclusionThus, symptom and functional improvements with caregiver burden reduction were observed in patients, and PANSS reduction at week 5 was commonly associated with favorable outcomes.

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Section: Discussionmentioning

confidence: 99%

Factors related to improvement of symptoms, function, and caregiver burden in Chinese patients with schizophrenia after switching to paliperidone palmitate once-monthly from oral antipsychotics

Li¹,

Feng²,

Lu³

et al. 2018

NDT

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“…High PK variability of long-acting injectable suspensions via intramuscular administration is well documented. [10][11][12][13] Our data confirmed that GSK2878175 LAI was long-acting in humans, but the doses were not high enough to demonstrate sufficient drug levels for the >9 weeks above target concentrations suggested from the combination study.…”

Section: Rg101-06mentioning

confidence: 60%

Randomized clinical trials towards a single‐visit cure for chronic hepatitis C: Oral GSK2878175 and injectable RG‐101 in chronic hepatitis C patients and long‐acting injectable GSK2878175 in healthy participants

Deng

Campbell

Han

et al. 2020

Journal of Viral Hepatitis

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Single‐visit cures for chronic hepatitis C are lacking. We conducted two clinical studies towards the goal of developing a regimen for single‐visit cure. In a randomized, open‐label, Phase 2 study (RG101‐04), investigators enrolled 26 adult chronic hepatitis C patients to evaluate safety and efficacy of single subcutaneous injection of RG‐101 (4 mg/kg) and daily oral tablets of GSK2878175 (20 mg) for 6, 9 or 12 weeks. In another randomized, double‐blind, single dose Phase 1 study (RG101‐06), investigators enrolled 18 healthy men to assess safety and PK of GSK2878175 long‐acting injectable at 100, 200 or 400 mg. In RG101‐04, SVR48 rates were 50%, 56% and 89%, for the 6, 9 and 12 weeks treatment arms, respectively. All AEs were mild or moderate in severity (≤Grade 2). In RG101‐06 at 400 mg, the mean duration of GSK2878175 plasma levels above in vitro therapeutic concentrations for GT1b was 41 days. All AEs were Grade 2 or less. In conclusion, single injection of RG‐101 combined with 12 weeks of GSK2878175 oral tablets was generally well tolerated and resulted in high SVR rates in chronic hepatitis C patients. Single injections of GSK2878175 long‐acting injectable were also well tolerated; however, higher doses would be required if used in combination with RG‐101 to achieve the SVR rates observed in the oral combination study to enable a single‐visit curative regimen.

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“…Among the pharmacokinetic studies, the first one was an open-label, randomized, parallel-group, multicenter study in patients with chronic schizophrenia. 25 On day 1, 48 eligible subjects were randomly assigned in a 1:1:1 ratio to 25, 100, or 150 mg PP groups; the same dose as that assigned on day 1 was injected on day 8 on the other side of the gluteal muscle. The plasma concentrations of paliperidone gradually increased to a C max at a mean t max of 13 days.…”

Section: Resultsmentioning

confidence: 99%

Critical evaluation of paliperidone in the treatment of schizophrenia in Chinese patients: a systematic literature review

Zhang¹,

Zhao

et al. 2016

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BackgroundPaliperidone (9-hydroxyrisperidone), the major active metabolite of risperidone, has been introduced as a novel atypical antipsychotic agent in many countries. It is available both as an oral extended-release (ER) formulation and as a long-acting injection (paliperidone palmitate, PP), which have been approved for treating schizophrenia in the People’s Republic of China since 2009 and 2012, respectively. This systematic review summarizes the efficacy, effectiveness, and safety of paliperidone in the treatment of schizophrenia in the Chinese population.MethodsA systematic literature search was conducted on the databases covering international and Chinese core journals, published from January 1, 2008, to May 22, 2015.ResultsA total of 122 publications were retrieved, of which 63 studies were identified for inclusion; most studies were related to paliperidone ER (n=53), nine were related to PP, and one study was related to both agents. Paliperidone ER demonstrated at least comparable efficacy with active comparators, including risperidone, olanzapine, ziprasidone, or aripiprazole, and was found to be superior with respect to the onset of action and improvement in the Personal and Social Performance Scale score. Paliperidone ER appeared to be associated with a lower risk of metabolic syndromes; the most common treatment-emergent adverse events were extrapyramidal symptoms, akathisia, insomnia, and somnolence. Results from interventional and observational studies showed that PP was also an effective and well-tolerated treatment for Chinese patients with schizophrenia. The findings were generally consistent with those observed in non-Chinese populations.ConclusionBoth paliperidone ER and PP were effective and well-tolerated agents for the treatment of schizophrenia in the Chinese population according to the data we reviewed. No new safety signals specific for the Chinese population were raised for paliperidone. Further studies may be needed to collect more data on long-term treatment of schizophrenia in the People’s Republic of China.

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Pharmacokinetics and tolerability of paliperidone palmitate injection in Chinese subjects

Abstract: The pharmacokinetics of paliperidone palmitate are linear with respect to time in Chinese subjects with schizophrenia at injections from 25 to 150 mg eq.

Cited by 15 publications

References 27 publications

Factors related to improvement of symptoms, function, and caregiver burden in Chinese patients with schizophrenia after switching to paliperidone palmitate once-monthly from oral antipsychotics

Factors related to improvement of symptoms, function, and caregiver burden in Chinese patients with schizophrenia after switching to paliperidone palmitate once-monthly from oral antipsychotics

Randomized clinical trials towards a single‐visit cure for chronic hepatitis C: Oral GSK2878175 and injectable RG‐101 in chronic hepatitis C patients and long‐acting injectable GSK2878175 in healthy participants

Critical evaluation of paliperidone in the treatment of schizophrenia in Chinese patients: a systematic literature review

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