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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

PubMedAdvanced healthcare materials2026-09-10

Water-Activated Phospholipid Phase-Separation Gel as an Immunomodulatory Anti-Adhesion Barrier for Postoperative Adhesion Prevention.

Lee Jong-Ju JJ, Sung Yulseung Y, Kim Yeji Y, Yang Heesang H et al.

Postoperative adhesions remain a major complication after abdominal surgery, and current polymeric barriers often show limited tissue retention and biocompatibility. Here, we establish a water-activated phospholipid barrier strategy for postoperative adhesion prevention by converting a depot-forming phospholipid phase-separation gel (PPSG) into a gram-scale surgical barrier. In this study, solvent identity acts as a functional design determinant rather than a passive solubilizer, governing hydration-triggered gel reinforcement, intraperitoneal residence, and tolerability. Replacing ethanol with propylene glycol strengthened the gel matrix, improved barrier activation, and enabled gram-scale administration without hepatic toxicity associated with ethanol-based PPSG. Mechanistically, the structured phospholipid barrier retained gel-state immunomodulatory activity, attenuating macrophage-driven inflammatory responses and suppressing NF-κB-associated signaling. In a rat peritoneal-cecum abrasion model, propylene glycol-based PPSG completely prevented macroscopic adhesions. Together, these findings establish a water-activated phospholipid barrier platform for converting depot-forming phospholipid systems into active surgical barriers that combine durable physical separation with local immunomodulation.

PMID 42717399
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PubMedAAPS PharmSciTech2026-09-10

Correlative Spectroscopic and Structural Imaging for Resin-Embedded Extended-Release Morphine Sulfate Pellets.

Zaker Yeakub Y, Ahmed Snober S, Tian Li L, Yilmaz Huzeyfe H et al.

Correlative spectroscopic and structural imaging provides a powerful approach for characterizing the microstructure of complex pharmaceutical formulations. Laser direct infrared (LDIR) spectroscopy is an emerging, rapid spectroscopic imaging technique that complements traditional approaches by enabling non-destructive chemical and morphological analysis over large sample surfaces within minutes. In this study, the capabilities of LDIR imaging were evaluated alongside Raman mapping, SEM-EDS, laser microscopy, and micro-CT as part of a correlative workflow to characterize the microstructure and chemical composition of pharmaceutical pellets. Resin embedding enabled consistent handling and structural preservation of extended-release pharmaceutical pellets across all imaging modalities. Two commercially available morphine sulfate ER pellets (ER-1 and ER-2) with different excipient compositions were used as model systems. Laser microscopy revealed distinct differences in surface topography, while micro-CT performed before milling confirmed inherent structural features. ER-1 displayed a smooth, intact core, whereas ER-2 exhibited internal cracks and cavities. Hyperspectral LDIR imaging successfully identified major components in both formulations (hit-quality index, HQI ≥ 0.83) with strong concordance to Raman mapping (HQI ≥ 0.85). The spatial distribution of the active pharmaceutical ingredient (API) revealed a layered structure in ER-1 and a homogeneous core in ER-2. This correlative workflow, combining resin embedding with multiple imaging modalities, underscores the value of LDIR and complementary techniques for comprehensive physicochemical characterization of complex drug products. These findings highlight the utility of correlative imaging for regulatory assessment and quality control of complex extended-release formulations.

PMID 42717169
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PubMedCrystal growth & design2026-09-10

Enhanced Solubility of Famotidine through Salification.

Eilers Jane M JM, Seo Payton P, Ma Liulei L, Kelley Steven P SP et al.

Famotidine (FMT) is an active pharmaceutical ingredient that exhibits poor aqueous solubility and poor permeability. Molecular electrostatic potential and pK a calculations were used to guide a salification strategy for FMT and afforded five salts featuring carboxylic acid-containing coformers. All solids feature charge-assisted hydrogen bonds between the guanidinium group of FMT and carboxylate of the coformer. All salts exhibited good thermal and benchtop stability, and a six- to 20-fold increase in aqueous solubility was achieved, depending on the coformer used. The best performing salts include coformers on the FDA's generally recognized as safe list, making the solids promising for pharmaceutical applications.

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PubMedAAPS PharmSciTech2026-09-10

Real-Time Monitoring of Tablet API Concentration and Bioavailability via Dissolution Kinetics in Simulated Stomach Fluid by T-Ray Transmission Technique.

Rahman Anis A, Islam Rafiq R, Michniak-Kohn Bozena B

This paper introduces a real-time, separationless method for monitoring Active Pharmaceutical Ingredient (API) concentration and dissolution kinetics in oral tablets using terahertz radiation (T-ray) transmission kinetics within simulated stomach fluid. Unlike conventional techniques such as High-Performance Liquid Chromatography (HPLC), which produce only discrete data points and require labor-intensive sample preparation, the T-ray approach offers continuous, quantitative measurement and monitoring. By leveraging the unique transmission and absorption characteristics of APIs in the T-ray region, this technique enables precise, real-time quantification of API concentration without physically separating excipients from the sample. The technique captures comprehensive kinetic profiles, providing deeper insights into dissolution processes and underlying molecular interactions. Its application can enhance Process Analytical Technology (PAT) by facilitating immediate, real-time quality control and supporting continuous manufacturing in the pharmaceutical industry. Additionally, the data generated can strengthen the modeling of in vitro-in vivo correlations (IVIVC), which is crucial for drug development and bioavailability assessment. Overall, the T-ray transmission technique represents a robust, efficient, and sustainable analytical tool for pharmaceutical research and production, offering significant advantages over traditional methods in both accuracy and operational speed.

PMID 42717175
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PubMedAAPS PharmSciTech2026-09-10

From Liquid to Gel: Multifunctional Stimuli-responsive Polymers for Targeted Oral Drug Delivery.

Mishra Manoj Kumar MK, Shukla Divaker D, Sharma Shalini S, Sharma Jyoti Nanda JN et al.

Oral drug delivery is the delivery method of choice, as it is non-invasive and patients will comply with the delivery method, but many contemporary therapeutics, such as poorly soluble, permeable, and unstable drugs, fail because of rapid gastrointestinal absorption, enzyme degradation, and non-targetability. The in-situ gelling systems are now considered paradigms that no longer exist as liquids; instead, they form a depot in the gastrointestinal tract and transform into a gel in response to physiological signals such as pH, ions, or enzymes. This review will discuss how these so-called smart polymers have developed over the years, starting as simple gel-forming systems and evolving into the multifunctional platforms that are also designed to have a pointed and sustained action. Next generation in situ gels combine bioadhesion, permeation enhancement, and active targeting ligands to overcome sequential barriers to delivery transit, permeability, stability, and cellular uptake. We critically assess the chemistry, mechanisms, formulation strategies, and therapeutic use of these systems, including gastro-retention and localized therapy, as well as oral delivery of biologics. Despite encouraging preclinical results, we touch on translational issues of scalability, manufacturing, and regulatory pathways. Multifunctional stimuli-responsive polymers, which actively traverse the gastrointestinal environment, are the future of oral drug delivery because they provide precision, bioavailability, and improved patient outcomes.

PMID 42717126
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PubMedCase reports in endocrinology2026-09-10

Diagnosis of Antipsychotic Medication-Induced Severe Hypertriglyceridaemia by the Phenomenon of Pseudohyponatraemia and Successful Management With Variable-Rate Intravenous Insulin Infusion: A Case Report.

Coleman Adam A, Kettyle Grace G, Monaghan Monica M, McKeever Edward E

Hypertriglyceridaemia (HTG) is a common condition resulting from genetic and environmental factors. Second-generation antipsychotic (SGA) medications are classically associated with the development of metabolic syndrome, of which HTG is a hallmark feature. Severe HTG is the third most common cause of acute pancreatitis, which has significant associated morbidity and mortality risk. It is therefore vital to rapidly and sustainably reduce triglyceride levels in patients presenting with severe HTG. A 35-year-old gentleman with a history of psychiatric illness taking SGA medications (quetiapine and risperidone) presented to our hospital with apparent hyponatraemia. With associated hyperosmolality (302 mOsm/kg), a diagnosis of pseudohyponatraemia was made. Upon further investigation, pseudohyponatraemia was identified to be due to severe HTG (72.8 mmol/L) and hyperglycaemia (26.0 mmol/L). There were no clinical or biochemical features of pancreatitis. A variable-rate infusion of intravenous insulin was commenced. Over the 10-day admission a fall in triglycerides to 10.5 mmol/L was observed without any adverse events. Acute pancreatitis did not develop during the inpatient admission or during outpatient follow-up, and triglyceride levels have fallen substantially (3.2 mmol/L at 5 months) having been switched from quetiapine and risperidone to aripiprazole, an SGA associated with less metabolic disturbance. This case demonstrates the safe and effective management of SGA-associated severe HTG with intravenous insulin infusion to prevent acute pancreatitis. It also highlights the utility of pseudohyponatraemia as a useful way of detecting severe HTG and the impact of SGA medications in the aetiology of severe HTG.

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