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aripiprazole (Abilify Maintena / Lu AF41155 / aripiprazole ERIS)

✓ Approved

Otsuka Holdings Co., Ltd. · DRD2 · 小分子

什么是 aripiprazole？

aripiprazole 是一种小分子，由Otsuka Holdings Co., Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intramuscular (IM) Injection。

药物档案

商品名Abilify Maintena, Lu AF41155, aripiprazole ERIS
公司Otsuka Holdings Co., Ltd.
药物类别小分子
分子靶点DRD2, HTR1A, HTR2A
给药途径Injectable (Others), Intramuscular (IM) Injection
状态Approved
来源： ClinicalTrials.gov, Otsuka Holdings Co., Ltd.

作用机制

分子靶点

aripiprazole 作用于 3 个分子靶点：

DRD2dopamine receptor D2 (D2DR, D2R)
HTR1A5-hydroxytryptamine receptor 1A (PFMCD, 5-HT1A)
HTR2A5-hydroxytryptamine receptor 2A (5-HT2A, HTR2)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

aripiprazole 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersSchizophrenia✓ Approved
Psychiatric disordersBipolar disorder✓ Approved

相关研究文献

PubMedAddiction (Abingdon, England)2026-06-13

Factors associated with the percentage of individuals who initiate and discontinue naltrexone as a relapse prevention pharmacotherapy in opioid use disorder: A systematic review, meta-analysis and meta-regression.

Roberts Emmert E, Sanderson Elizabeth E, Santo Thomas T, Hickman Matthew M et al.

Naltrexone is a pharmacotherapeutic option for relapse prevention in opioid use disorder (OUD); however, studies highlight low rates of initiation and high rates of discontinuation as limiting its effectiveness. We aimed to (1) estimate the percentage of individuals with OUD who (having undergone withdrawal and wish to remain abstinent) initiate and discontinue naltrexone and (2) examine participant- and study-level factors that contribute to variation in initiation and discontinuation rates. We undertook a systematic review, random-effects meta-analysis and meta-regression searching Medline, Embase, PsychINFO and CENTRAL from database inception to 19 February 2025 for studies of any design from any geographical region involving individuals with OUD eligible to receive naltrexone as a relapse prevention pharmacotherapy (i.e. those completing opioid withdrawal and wishing to remain abstinent). Measurements included the percentage of individuals who initiate or discontinue oral, long-acting injectable depot or implantable formulations of naltrexone at 1, 3 or 6 months. Certainty was assessed using the GRADE framework. Twenty-two studies, including 124 016 individuals, reported initiation and 95 studies, including 16 969 individuals, reported discontinuation. The pooled percentage initiating oral naltrexone among those eligible was 60.3% [95% confidence interval (CI) = 38.9%-80.0%, 2014 participants, 15 studies] and depot was 18.2% (95% CI = 2.7%-42.5%, 57 383 participants, 4 studies). The pooled percentage discontinuing oral was 50.0% (95% CI = 41.9%-58.1%, 7340 participants, 34 studies) at 1 month, 61.3% (95% CI = 50.9%-71.2%, 2347 participants, 29 studies) at 3 months and 71.0% (95% CI = 57.3%-83.0%, 1889 participants, 19 studies) at 6 months. The pooled percentage discontinuing depot was 26.1% (95% CI = 19.5%-33.3%, 3589 participants, 33 studies) at 1 month, 46.7% (95% CI = 38.4%-55.1%, 3302 participants, 33 studies) at 3 months and 60.0% (95% CI = 43.2%-75.8%, 3071 participants, 22 studies) at 6 months. Statistically significantly higher percentages initiated oral naltrexone if it was the only offered pharmacotherapy (meta-regression coefficient 33.6%, 95% CI = 8.1%-59.2%, P = 0.014) and statistically significantly lower percentages discontinued oral naltrexone at 3 and 6 months if administration was supervised (meta-regression coefficient -18.6%, 95% CI = -36.6% to -1.0%, P = 0.043 and -27.3%, 95% CI = -50.1% to -4.4%, P = 0.022, respectively). There was no clear evidence that study setting (i.e. if the study was conducted in routine clinical care or an investigational setting) substantially explained or contributed to the variation in any estimates. All outcomes were very low certainty. Very low certainty evidence suggests that, among people with opioid use disorder who have undergone withdrawal and wish to remain abstinent, a substantial percentage are willing to initiate naltrexone with marked early discontinuation.

PMID 42286437
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PubMedExpert review of vaccines2026-06-13

Recent advances for the pharmaceutical production of highly attenuated poxviruses as viral vector platforms.

Weber Linus G LG, Wolff Michael W MW

Highly attenuated poxviruses serve as potent viral vectors, oncolytic agents, and therapeutic vaccines. They can accommodate and stably maintain a large genomic payload of foreign inserts. Their limited replication in human cells provides an excellent safety profile, but it concomitantly necessitates higher doses of infectious particles for full therapeutic efficacy. We review recent advances in bioprocesses for the pharmaceutical production of poxvirus-based vectors, focusing mainly on the vaccinia virus and the Orf virus. These include upstream processing using highly permissive cell substrates, optimized feeding strategies, and a virus phenotype that facilitates downstream processing. The study explores ongoing challenges and identifies strategies to adapt the downstream process to intensified upstream processes in order to achieve an economic end-to-end production. For notably increased virus yields of up to 2 log after amplification, we propose to replace classic adsorption chromatography by a collective and continuous purification platform for separating the virus from process-related impurities. Filtration operations facilitate process scalability while reducing volumes, which is beneficial for a flow-through polishing to meet pharmaceutical quality attributes. Combined with artificial intelligence modeling, these advancements alleviate financial pressures on healthcare systems and accelerate the production of novel vaccine candidates for clinical use.

PMID 42287073
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PubMedLuminescence : the journal of biological and chemical luminescence2026-06-13

A Sustainable Spectrofluorimetric Method for Lisinopril Determination Using Erythrosin B Fluorescence Quenching With Mechanistic Characterization, Quantum Mechanical Modeling, and Green Chemistry Evaluation.

Abdelzaher Ahmed M AM, Al Kamaly Omkulthom O, Abdel Rahman Mona A MA

A novel, sensitive, and environmentally sustainable spectrofluorimetric method was developed for lisinopril quantification based on Erythrosin B fluorescence quenching. The method exploits static quenching through ground-state ion-pair complex formation between dianionic Erythrosin B and dicationic lisinopril at pH 6.0. Comprehensive mechanistic investigation employing temperature-dependent Stern-Volmer analysis, thermodynamic studies, Job's method, and PM3 semi-empirical quantum mechanical calculations confirmed the static quenching mechanism driven by electrostatic interactions with binding energy of -6.90 kcal/mol (-28.87 kJ/mol). Under optimized conditions (pH 6.0, 15 μg/mL Erythrosin B, excitation/emission, 533/555 nm), the method exhibited excellent linearity over 0.01-3.0 μg/mL (r = 0.9998) with high sensitivity (LOD, 3.1 ng/mL; LOQ, 9.2 ng/mL). Validation according to ICH Q2(R2) guidelines demonstrated excellent accuracy (99.8 ± 1.119%), precision (RSD < 1.63%), robustness, and selectivity. The method was successfully applied to pharmaceutical tablets (100.02 ± 1.079% recovery) and spiked human plasma (96.19%-105.72% recovery). Comprehensive sustainability assessment using RGB12 (whiteness, 88.0/100) and EPPI (total score, 83.8) confirmed the method's superior environmental sustainability and ideal green profile. The developed method offers significant advantages including commercially available reagents, elimination of derivatization or nanomaterial synthesis, and simple instrumentation, representing an environmentally friendly alternative for routine lisinopril determination in pharmaceutical quality control and bioanalytical applications.

PMID 42286975
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PubMedProgress in neuro-psychopharmacology & biological psychiatry2026-06-13

Clozapine and obsessive-compulsive symptoms: Integrating clinical outcomes, mechanisms, and precision psychiatry approaches.

Gürcan Gamze G, Sılay Ravza Zeynep RZ

Clozapine remains the gold-standard treatment for treatment-resistant schizophrenia owing to its superior antipsychotic efficacy and anti-suicidal properties, yet it is frequently associated with the emergence of obsessive-compulsive symptoms (OCS). Epidemiological studies estimate that 20-76% of clozapine-treated patients develop OCS, which often follow a chronic or fluctuating trajectory. Early recognition is critical, as untreated symptoms may persist and substantially impair psychosocial, occupational, and cognitive functioning. Younger age at clozapine initiation, prolonged illness duration, elevated clozapine plasma concentrations, comorbid anxiety or depressive symptoms, and gene-environment interaction (G × E) mechanisms involving glutamatergic pathway genes such as SLC1A1, DLGAP3, and GRIN2B have been associated with increased vulnerability. Current evidence suggests that the pathophysiology of clozapine-associated OCS is multifactorial and involves serotonergic and dopaminergic dysregulation within orbitofrontal-striatal-thalamic circuitry, superimposed upon underlying genetic and glutamatergic susceptibility. While pharmacologically mediated mechanisms are strongly implicated, pre-existing subclinical obsessive-compulsive traits may also contribute, complicating causal attribution. Phenomenologically, OCS must be differentiated from psychotic symptoms to avoid inappropriate antipsychotic escalation, which may exacerbate compulsive symptomatology. Management requires a multimodal and individualized approach integrating careful clozapine dose optimization, selective serotonin reuptake inhibitor (SSRI) augmentation, antipsychotic combination strategies such as adjunctive aripiprazole, and cognitive-behavioral therapy with exposure and response prevention (CBT-ERP). Routine therapeutic drug monitoring, structured symptom assessment, and longitudinal functional evaluation remain essential for optimizing outcomes. In conclusion, clozapine-associated OCS represent a clinically significant and mechanistically complex phenomenon arising from interactions among pharmacological exposure, neurobiological vulnerability, and individual susceptibility factors. Early detection and integrated management can mitigate functional impairment without compromising clozapine efficacy. Future research should clarify neurobiological mechanisms, validate biomarker-informed risk stratification approaches, and prioritize patient-centered functional outcomes to advance precision psychiatry in this population.

PMID 42285472
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PubMedScientific reports2026-06-13

Optimization algorithm for improving the prediction accuracy of API solubility in green solvent.

Alasiri Ali A, Lahiq Ahmed A AA, Alshehri Abdullah A AA

Supercritical carbon dioxide (SC-CO₂) is widely used as an environmentally friendly solvent in pharmaceutical processing, where accurate prediction of drug solubility is essential for efficient formulation design, extraction processes, and process optimization. However, predicting solubility behavior in supercritical systems remains challenging due to the nonlinear interactions between thermodynamic conditions and molecular properties. In this study, a hybrid artificial intelligence framework is developed to predict the solubility of active pharmaceutical ingredients (APIs) in SC-CO₂ using a curated dataset of more than 350 experimentally reported measurements. The proposed framework integrates interpretable deep learning (TabNet) and histogram-based gradient boosting (HGB) with three metaheuristic optimization algorithms, namely the Attack-Leave Optimizer (ALO), Energy Valley Optimizer (EVO), and Botox Optimization Algorithm (BOA), to improve hyperparameter tuning and predictive performance. Model evaluation was conducted using multiple statistical indicators, five-fold cross-validation, prediction interval bootstrapping, and multi-objective Pareto front analysis to assess accuracy and robustness. Among the evaluated configurations, the EVO-tuned TabNet model demonstrated the best predictive performance, achieving a coefficient of determination of [Formula: see text]along with narrow prediction intervals, indicating strong generalization capability within the studied thermodynamic domain. Statistical analysis using the Kruskal-Wallis test confirmed significant differences between optimizer performances ([Formula: see text]). These findings demonstrate that the proposed hybrid pipeline enhances predictive accuracy and interpretability within the thermodynamic domain represented by the compiled dataset. The framework therefore provides a statistically supported computational tool for assisting solvent selection and formulation analysis in supercritical systems, while broader generalization would benefit from future expansion of experimental solubility datasets.

PMID 42286012
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PubMedJournal of pharmaceutical and biomedical analysis2026-06-13

A novel electrochemical sensing with MIP for highly selective and sensitive determination of anticancer drug erlotinib.

Erdogan-Kablan Sevilay S, Cetinkaya Ahmet A, Unal M Altay MA, Bellur Atici Esen E et al.

The sensitive and selective determination of targeted anticancer drugs is crucial for pharmaceutical quality control and therapeutic monitoring. Erlotinib (ERL), a tyrosine kinase inhibitor approved by the U.S. Food and Drug Administration (FDA) for the treatment of metastatic or locally advanced non-small cell lung cancer (NSCLC), requires reliable analytical methods due to its clinical importance and potential impurities. In this study, an ultrasensitive nanomaterial-supported molecularly imprinted polymer (MIP)-based electrochemical sensor was rationally designed for the selective detection of ERL. Zinc oxide nanoparticles (ZnONPs) were incorporated to enhance the effective surface area and increase the density of active recognition sites. The polymeric film was synthesized using 3-aminophenyl boronic acid (3-APBA) as the functional monomer, ethylene glycol dimethacrylate (EGDMA) as the cross-linker, 2-hydroxyethyl methacrylate (HEMA) as the base monomer, and 2-hydroxy-2-methylpropiophenone as the initiator. The fabricated 3-APBA/ERL/ZnONPs@MIP-modified glassy carbon electrode (GCE) was characterized by scanning electron microscopy (SEM), electrochemical impedance spectroscopy (EIS), and cyclic voltammetry (CV). The sensor exhibited a linear response in the range of 1.0 × 10-13-1.0 × 10-12 M (100-1000 fM) with a limit of detection (LOD) of 1.89 × 10-14 M (18.9 fM) and a limit of quantification (LOQ) of 6.30 × 10-14 M (63.0 fM) (r = 0.997). Selectivity and specificity studies demonstrated that ERL could be accurately quantified even in the presence of structurally related drugs and ERL-related impurities at 1000-fold excess, yielding recovery values between 98.40% and 103.76%. The sensor was successfully applied to ERL determination in tablet dosage forms, demonstrating its suitability for pharmaceutical quality control. Furthermore, density functional theory (DFT) and Monte Carlo simulations elucidated the molecular recognition mechanism, revealing a precise "lock-and-key" fit of ERL within the imprinted cavities and supporting a target-induced "site-blocking" sensing mechanism.

PMID 42284916
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