Perseris (risperidone sustained-release 1-month depot) / Indivior, Reckitt Benckiser, HLS Therap - LARVOL DELTA

Population Pharmacokinetic-Based Strategies for Switching Patients with Schizophrenia Between Long-Acting Injectable Formulations of Risperidone: R064766 or RBP-7000 to TV-46000. (PubMed, Neurol Ther) - "These simulations revealed switching to TV-46000 4-6 weeks after the last dose of R064766 and 4 weeks after the last dose of RBP-7000 provided generally comparable PK exposures at first dose and steady state of TV-46000. Clinician discretion will determine which switching strategy is most appropriate in context based on factors such as patient preference, scheduling convenience, and concerns about tolerability."

Journal • PK/PD data • CNS Disorders • Psychiatry • Schizophrenia

Revisiting risperidone: new formulations - new futures? (ECNP 2025) - "In clinical practice it has since been largely replaced by other atypical LAIs subsequently developed that include paliperidone (monthly, three-monthly, six-monthly), olanzapine (two-weekly, monthly) and aripiprazole (monthly, two-monthly)...These include risperidone subcutaneous monthly (Perseris) [2] risperidone subcutaneous one or two-montly (Uzedy) [3], risperidone in-situ microspheres (Okedi) [4] and risperidone extended release microspheres (Rykindo) [5]... The new formulations of risperidone LAI overall improve ease of use, increase rapidity of onset, add multiple injection site options and extend treatment duration intervals allowing for greater flexibility, simplicity and patient acceptability in clinical practice. The efficacy and safety profile of risperidone is well established and the new formulations offer the potential of use of a risperidone LAI in a broader range of clinical settings and thus, may improve the use and acceptance of LAIs in both the..."

Bipolar Disorder • CNS Disorders • Mood Disorders • Psychiatry • Schizophrenia

Clinical Utility of Long-Acting Injectable Risperidone in Schizophrenia and Bipolar I Disorder: A Review of Clinical Studies. (PubMed, Psychol Res Behav Manag) - "To date, five different risperidone LAI formulations have been marketed - including a second biweekly microsphere injection (LY03004), a newer monthly intramuscular formulation using in situ microparticles (ISM) technology that does not require an oral risperidone run-in, and two subcutaneous formulations (RBP-7000 and TV-46000)...To facilitate this, healthcare providers should develop a comprehensive understanding of these formulations to select the most suitable option. While risperidone ISM, RBP-7000, and TV-46000 may enhance treatment feasibility and adherence, further research is needed to build an evidence base comparable to that available for BW-RLAI, particularly in the treatment of BD."

Journal • Review • Bipolar Disorder • CNS Disorders • Mood Disorders • Psychiatry • Schizophrenia

Diffusion dimensionality modeling of subcutaneous/intramuscular absorption of antibodies and long-acting injectables. (PubMed, J Pharmacokinet Pharmacodyn) - "The diffusion dimensionality models were challenged with previously published subcutaneous absorption data for 13 antibody drugs and insulin lispro, and the long-acting injectable antipsychotic drugs: subcutaneous Perseris™, intramuscular Invega Sustenna®, Risperdal Consta®, and olanzapine...Three antibodies (CNTO5825, ACE910 and ustekinumab) were best described by the 2-dimensional diffusion equation. The 2- and 3-dimensional diffusion equations were equivalent for ABT981, guselkumab, adalimumab, nemolizumab, omalizumab, and secukinumab. Golimumab, DX2930, AMG139, and mepolizumab were best described by the 3-dimensional diffusion equation. All the long-acting antipsychotic dosage forms except Risperdal Consta were modeled satisfactorily. Diffusion dimensionality models are a parsimonious and effective approach for modeling drug absorption profiles of subcutaneously and intramuscularly administered small molecule and protein drugs and their dosage forms."

Journal • CNS Disorders

Understanding drug release mechanisms of risperidone in situ forming implant depots in rabbits. (PubMed, J Control Release) - "To explore the in vivo drug release mechanisms, risperidone in situ forming implants with different PLGA attributes (i.e., molecular weight (MW), lactide:glycolide (L/G) ratio, blockiness, and end group) were prepared based on the reference listed drug Perseris (risperidone extended-release injectable suspension)...These results indicate that drug release in vivo may be degradation dominated and that depot degradation followed bulk erosion. This study provides an understanding of the in vivo mechanisms controlling drug release from in situ forming implant formulations."

Journal • Preclinical

Switching patients with schizophrenia from RBP-7000, a subcutaneous, once-monthly risperidone, to TV-46000, a long-acting subcutaneous antipsychotic: population pharmacokinetic–based strategies (ECNP 2024) - "PopPK simulations revealed switching to TV-46000 4 weeks after the last dose of RBP-7000 provided generally comparable PK exposures at first dose and at steady state of TV-46000. If clinicians seek to avoid higher Cmax peaks associated with switching to TV-46000 q2m, then q1m can be administered. Clinician discretion will determine whether to initiate q1m or q2m TV-46000 4 weeks after the last dose of RBP-7000 based on a variety of factors, such as patient preference, scheduling convenience, and concerns about tolerability or symptom breakthrough."

Clinical • PK/PD data • CNS Disorders • Psychiatry • Schizophrenia

Towards in vitro - In vivo correlation models for in situ forming drug implants. (PubMed, J Control Release) - "The predictability of the model passed external validation using the reference listed drug (RLD), Perseris®. IVIVC could not be developed when formulations with different PLGA molar ratios of lactic acid to glycolic acid (L/G) were included. The present work provides a comprehensive understanding of the impact of the testing method attributes on drug release from in situ forming implants, which is a valuable practice for level A IVIVC development."

Journal • Preclinical

An Open-Label Study to Assess Monthly Risperidone Injections (180 mg) Following Switch from Daily Oral Risperidone (6 mg) in Stable Schizophrenic Patients. (PubMed, Clin Drug Investig) - P4 | "The results support the use of 180 mg RBP-7000 in schizophrenic patients stable on 6 mg/day oral risperidone and a second injection site in the upper arm."

Journal • CNS Disorders • Psychiatry • Schizophrenia

In brief: Three new injectable antipsychotic drugs. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal • Bipolar Disorder • CNS Disorders • Mood Disorders • Psychiatry • Schizophrenia

In situ forming risperidone implants: Effect of PLGA attributes on product performance. (PubMed, J Control Release) - "Perseris (risperidone) for extended-release injectable suspension was selected as the reference listed drug (RLD)...This is the first report evaluating the impact of PLGA property variation (over a narrow range) on the performance of in situ forming implants. The knowledge gained will provide a better understanding of the mechanisms underlying risperidone in situ forming implant performance and will aid the development of future products."

Journal

In Vivo Characterization of Perseris and Compositionally Equivalent Formulations. (PubMed, Int J Pharm) - "Although the erosion mechanism appeared to be similar between in vitro and in vivo, there were in vitro-in vivo differences concerning the drug release kinetics, phase separation rates and swelling behavior. This work provides a comprehensive in vitro/in vivo understanding of Perseris and the developed compositionally equivalent formulations, which will be beneficial for future development of generic as well as novel PLGA in situ forming implant products."

Journal • Preclinical • CNS Disorders • Psychiatry • Schizophrenia

Evaluation of Patient Assistance Programs and Eligibility Criteria Offered for Long-Acting Antipsychotics Used in Patients With Schizophrenia (APA 2023) - "Of those, 70% (8/10) offer a PAP which covers the full cost for uninsured US residents, including: Abilify Maintena, Abilify Aristada, Invega Sustenna, Invega Trinza, Invega Hayfera, Risperdal Consta and Haldol Decanoate. With LAI’s such as Zyprexa Relprevv, Prolixin and Perseris being the exceptions... While these PAP’s cover the entirety of the cost of most of the available medications for those without insurance, they only aid a small subset of the population of patients suffering from schizophrenia. Efforts will need to be made to decrease the gap between costs of treatment and available financial assistance programs, especially for those expereincing financial difficulty who have some form of medical insurance and high copayments."

Clinical • CNS Disorders • Psychiatry • Schizophrenia

Reverse Engineering of Perseris and Development of Compositionally Equivalent Formulations. (PubMed, Int J Pharm) - "The novelty of this dissolution method lies in its ability to control implant shape, generate reproducible data, distinguish different release phases, as well as identify formulation changes. The knowledge gained in this work and the methodology established for characterization of the implant formulations are important for implant formulation development."

Journal

PANSS Individual Item and Marder Dimension Analyses From a Pivotal Trial of RBP-7000 (Monthly Extended-Release Risperidone) in Schizophrenia Patients. (PubMed, J Clin Psychiatry) - P3 | "Schizophrenia patients with higher baseline Marder UHE scores may benefit from initiation of treatment at the 120 mg dose. Trial Registration: ClinicalTrials.gov identifier: NCT02109562."

Clinical • Journal • CNS Disorders • Depression • Mood Disorders • Psychiatry • Schizophrenia

Perseris Kit: Newly added patent in Orange Book (Orange Book) - Expiry on November 5, 2026

Patent • Schizophrenia

Perseris: PDUFA action date in US for schizophrenia on December 12, 2021 (Indivior) - H1 2021 Results

PDUFA date • Schizophrenia

Safety, Tolerability, Pharmacokinetics and Efficacy of 180 mg Subcutaneous Risperidone From 6 mg Oral Risperidone (clinicaltrials.gov) - P4; N=69; Completed; Sponsor: Indivior Inc.; N=25 ➔ 69

Clinical • Enrollment change • CNS Disorders • Psychiatry • Schizophrenia

[VIRTUAL] Alternate Injection Site (Back of Upper Arm) for Monthly Long-Acting Risperidone Injections of RBP- 7000 (APA 2021) - "Administration of 180 mg RBP-7000 in the back of the upper arm showed comparable pharmacokinetics compared with injection in the abdominal region with no clinically meaningful differences in safety or efficacy measures, supporting the back of the upper arm as an alternative injection site."

CNS Disorders • Dermatology • Pain • Psychiatry • Schizophrenia

[VIRTUAL] RBP-7000 Monthly Risperidone Injection (180 Mg) Following Switch From Daily Oral Risperidone (6 Mg) in Stable Schizophrenic Patients (APA 2021) - "Monthly injections of 180 mg RBP-7000 administered as 2 SC injections of 90 mg provided similar average plasma concentration of the total active moiety compared with 6 mg/day oral risperidone given as 3 mg twice daily. All clinical symptoms assessments remained stable throughout the study prior to and after the switch from oral risperidone. Overall, the safety profile of 180 mg RBP-7000 was consistent with the established safety profile of RBP-7000 at lower doses and other risperidone products."

Clinical • CNS Disorders • Psychiatry • Schizophrenia

[VIRTUAL] A Comparison of the Pharmacokinetics, Efficacy, and Tolerability of Long-Acting Injectable Risperidone Formulations (CPNP 2021) - "Purpose: The purpose of this review was to compare the pharmacokinetics, efficacy, and tolerability of long-acting injectable risperidone formulations: Risperdal Consta®, PerserisTM, and Risperidone ISM®. Oral antipsychotics are the backbone of schizophrenia treatment in the U.S. Long-acting injectable risperidone continues to be a mainstay of therapy due to improved adherence and efficacy rates. Consta® could be considered first-line because it is well-tolerated, offers more potential for an individualized dosing regimen, and has the greatest PANSS score reduction. As new formulations gain FDA-approval, it is essential that prescribers engage in multifactorial decision-making centered around each individual's needs."

Clinical • PK/PD data • CNS Disorders • Psychiatry • Schizophrenia

HLS Therapeutics Announces Fourth Quarter and Fiscal 2020 Financial Results (Canada Newswire) - "PERSERIS and the MyCare Psychiatry Lab Assays are products in the CNS therapeutic market, and both were approved by Health Canada in Q4....We expect to have both in the market in the second half of 2021."

Launch Canada • CNS Disorders • Schizophrenia

UPDATE 2-Drugmaker Indivior prepares for pandemic hit to run into 2021 (Reuters) - "It expects...Perseris net revenue of $17 million to $20 million."

Sales projection • CNS Disorders • Schizophrenia

Safety, Tolerability, Pharmacokinetics and Efficacy of 180 mg Subcutaneous Risperidone From 6 mg Oral Risperidone (clinicaltrials.gov) - P4; N=25; Completed; Sponsor: Indivior Inc.; N=69 ➔ 25

Clinical • Enrollment change • CNS Disorders • Psychiatry • Schizophrenia

Indivior : Provides Preliminary FY 2020 Financial Results Ahead of Guidance (Market Screener) - "Expected PERSERIS® net revenue consistent with guidance of $12m to $15m."

Sales • CNS Disorders • Schizophrenia

[VIRTUAL] Comparison of the pharmacokinetics, efficacy, and tolerability of long-acting injectable risperidone formulations (ASHP 2020) - "Purpose: The purpose of this review was to compare the pharmacokinetics, efficacy, and tolerability of long-acting injectable risperidone formulations: Risperdal Consta®, PerserisTM, and Risperdal ISM®. Oral antipsychotics are the backbone of schizophrenia treatment in the U.S. Recently, long-acting injectable risperidone formulations are gaining popularity due to improved adherence and subsequent efficacy rates. Risperdal Consta could be considered first-line when a long-acting injectable antipsychotic is warranted because it is well-tolerated, offers the most potential for an individualized dosing regimen, and has the greatest PANSS score reduction. As new formulations gain FDA-approval and become potential therapy options, it is essential that prescribers engage in multifactorial decision-making centered around each individual’s needs regarding administration, adverse effect profiles, drug cost, and other barriers not outlined in this report."

Clinical • PK/PD data • CNS Disorders • Psychiatry • Schizophrenia