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Introduction <p>This analysis used pharmacokinetic (PK) modeling to characterize dosing conversions and switching strategies from R064766, a once-every-2-weeks, intramuscular long-acting injectable antipsychotic (LAI) formulation of risperidone microspheres, and RBP-7000, a subcutaneous (sc) LAI formulation of risperidone administered in the abdomen once monthly (q1m), to TV-46000, a q1m or once-every-2-months (q2m) sc LAI formulation of risperidone.</p> Methods <p>Total active moiety (TAM; risperidone + 9-OH&#xa0;risperidone) concentration–time profiles were simulated on the basis of published population PK models with virtual populations of 5000 patients. Simulations were performed to predict TAM exposures when switching to TV-46000 q1m and q2m 2–6&#xa0;weeks after the last steady-state R064766 injection and 4&#xa0;weeks after the last dose of RBP-7000.</p> Results <p>Comparable doses of oral risperidone, TV-46000, R064766, and RBP-7000 were identified. Initiating TV-46000 4–6&#xa0;weeks after the last dose of R064766 resulted in similar trends for maximal (<i>C</i><sub>max</sub>) and minimal (<i>C</i><sub>min</sub>) plasma concentration ratios after the first injection for all TV-46000 doses and durations (q1m, q2m) compared with R064766 at steady state. Initiating TV-46000 q1m 4&#xa0;weeks after the last dose of RBP-7000 resulted in slightly higher, but generally comparable, average plasma concentrations, <i>C</i><sub>max</sub>, and <i>C</i><sub>min</sub> at first dose and at steady state for TV-46000 compared with RBP-7000; <i>C</i><sub>min</sub> of TV-46000 q2m and RBP-7000 were also comparable. Similar trends in plasma concentrations were observed for both back-of-the-upper-arm and abdominal administration when switching from R064766 and RBP-7000 to TV-46000.</p> Conclusion <p>These simulations revealed switching to TV-46000 4–6&#xa0;weeks after the last dose of R064766 and 4&#xa0;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.</p>

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Population Pharmacokinetic–Based Strategies for Switching Patients with Schizophrenia Between Long-Acting Injectable Formulations of Risperidone: R064766 or RBP-7000 to TV-46000

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年10月26日

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  • Itay Perlstein,
  • Jonathan Meyer,
  • Sharath Kumar,
  • Ziqi Yue,
  • Vijay Ivaturi,
  • Kelli R. Franzenburg,
  • Mark Suett,
  • Rolf Hansen,
  • Avia Merenlender Wagner,
  • Arti Phatak,
  • Rajendra Singh

摘要

Introduction

This analysis used pharmacokinetic (PK) modeling to characterize dosing conversions and switching strategies from R064766, a once-every-2-weeks, intramuscular long-acting injectable antipsychotic (LAI) formulation of risperidone microspheres, and RBP-7000, a subcutaneous (sc) LAI formulation of risperidone administered in the abdomen once monthly (q1m), to TV-46000, a q1m or once-every-2-months (q2m) sc LAI formulation of risperidone.

Methods

Total active moiety (TAM; risperidone + 9-OH risperidone) concentration–time profiles were simulated on the basis of published population PK models with virtual populations of 5000 patients. Simulations were performed to predict TAM exposures when switching to TV-46000 q1m and q2m 2–6 weeks after the last steady-state R064766 injection and 4 weeks after the last dose of RBP-7000.

Results

Comparable doses of oral risperidone, TV-46000, R064766, and RBP-7000 were identified. Initiating TV-46000 4–6 weeks after the last dose of R064766 resulted in similar trends for maximal (Cmax) and minimal (Cmin) plasma concentration ratios after the first injection for all TV-46000 doses and durations (q1m, q2m) compared with R064766 at steady state. Initiating TV-46000 q1m 4 weeks after the last dose of RBP-7000 resulted in slightly higher, but generally comparable, average plasma concentrations, Cmax, and Cmin at first dose and at steady state for TV-46000 compared with RBP-7000; Cmin of TV-46000 q2m and RBP-7000 were also comparable. Similar trends in plasma concentrations were observed for both back-of-the-upper-arm and abdominal administration when switching from R064766 and RBP-7000 to TV-46000.

Conclusion

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.