Fagiolini Andrea, Wang Yanlin, Bioque Miquel, Harlin Matthew, Larsen Frank, Wang Xiaofeng, Park Wansu, Rich Benjamin, Gobburu Jogarao V, Raoufinia Arash
Department of Molecular and Developmental Medicine, Division of Psychiatry, University of Siena School of Medicine, Siena, Italy.
Otsuka Pharmaceutical Development & Commercialization Inc., Princeton, NJ, USA.
Curr Med Res Opin. 2025 Feb;41(2):317-327. doi: 10.1080/03007995.2025.2456014. Epub 2025 Feb 5.
Aripiprazole 2-month ready-to-use (Ari 2MRTU) is a long-acting injectable antipsychotic that was approved for use in Europe in March 2024, for the maintenance treatment of schizophrenia in adult patients stabilized with aripiprazole; it is administered gluteal intramuscular injection once every two months. This review examines population pharmacokinetic model-based simulations relevant to the use of Ari 2MRTU in Europe, accompanied by expert commentary that contextualizes the simulations and highlights the potential implications of the availability of Ari 2MRTU for patients, caregivers, and clinicians. Various simulations conducted across 8 weeks (representing the first dosing interval), or 32 weeks (representing maintenance dosing) demonstrated an aripiprazole exposure profile for Ari 2MRTU that was similar to aripiprazole once-monthly (AOM), but with an extended dosing interval. In treatment initiation scenarios consistent with the European label, therapeutic levels of aripiprazole (i.e. ≥95 ng/mL) were maintained when transitioning from either AOM or oral aripiprazole, including with a two-injection start regimen with no requirement for 14 days of oral aripiprazole supplementation. Therapeutic levels of aripiprazole were also observed for treatment maintenance scenarios, except when dosing of Ari 2MRTU was delayed by 8 weeks. The availability of Ari 2MRTU extends the range of options for the maintenance treatment of schizophrenia in Europe. Ari 2MRTU may provide adherence benefits due to its extended dosing interval and the option to initiate treatment using a two-injection start regimen, which does not require 14 days of overlapping oral supplementation.
阿立哌唑长效注射用预充式制剂（Ari 2MRTU）是一种长效注射用抗精神病药物，于2024年3月在欧洲获批，用于接受阿立哌唑治疗病情稳定的成年精神分裂症患者的维持治疗；每两个月进行一次臀肌注射给药。本综述探讨了基于群体药代动力学模型的模拟，这些模拟与Ari 2MRTU在欧洲的使用相关，并伴有专家评论，对模拟结果进行背景分析，并强调Ari 2MRTU的可用性对患者、护理人员和临床医生的潜在影响。在8周（代表首个给药间隔）或32周（代表维持给药）内进行的各种模拟表明，Ari 2MRTU的阿立哌唑暴露曲线与每月一次的阿立哌唑（AOM）相似，但给药间隔延长。在与欧洲药品说明书一致的治疗起始方案中，从AOM或口服阿立哌唑转换时，阿立哌唑的治疗水平（即≥95 ng/mL）得以维持，包括采用两针起始方案且无需补充14天口服阿立哌唑的情况。在治疗维持方案中也观察到了阿立哌唑的治疗水平，除非Ari 2MRTU的给药延迟8周。Ari 2MRTU的可用性扩展了欧洲精神分裂症维持治疗的选择范围。Ari 2MRTU可能因其延长的给药间隔以及可采用两针起始方案开始治疗（无需1周重叠口服补充）而带来依从性方面的益处。
