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asenapine maleate (HP 3070 / HP3070 / Secuado)

✓ Approved

Hisamitsu · DRD1 · 小分子

什么是 asenapine maleate？

asenapine maleate 是一种小分子，由Hisamitsu研发。该药已获批，用于治疗相关适应症，给药途径：Transdermal。

药物档案

商品名HP 3070, HP3070, Secuado
公司Hisamitsu
药物类别小分子
分子靶点DRD1, DRD2, HTR2A
给药途径Transdermal
状态Approved
来源： ClinicalTrials.gov, Hisamitsu

作用机制

分子靶点

asenapine maleate 作用于 3 个分子靶点：

DRD1dopamine receptor D1 (DADR, D1R)
DRD2dopamine receptor D2 (D2DR, D2R)
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

asenapine maleate 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 disorderPhase I

相关研究文献

PubMedJournal of applied toxicology : JAT2026-10-26

Large-Scale Monitoring, Biochemical Mechanism, and Fitness Cost of Resistance to Chlorfenapyr in a Near-Isogenic Strain of Spodoptera litura (Lepidoptera: Noctuidae) From China.

Liu Chenghong C, Tang Juan J, Qu Cheng C, Ma Xiaoli X et al.

Spodoptera litura is a globally important polyphagous herbivore that has developed resistance to many widely used insecticides. Chlorfenapyr is a pyrrole insecticide with demonstrated efficacy against lepidopteran pests, but the susceptibility baseline and field-evolved resistance in S. litura remain poorly characterized. In this study, we built a near-isogenic strain (JZ-NIL) based on one field-collected chlorfenapyr-resistant population of S. litura and characterized patterns of cross-resistance, fitness costs, and mechanism of metabolic resistance. In comparison with the susceptible Lab-S strain, the field-sampled JZ population displayed approximately 225.0-fold resistance to chlorfenapyr. The JZ-NIL strain was built and showed 124.2-fold chlorfenapyr resistance, with no apparent cross-resistance to broflanilide, chlorpyrifos, chlorantraniliprole, emamectin benzoate, indoxacarb, and spinetoram. Assays of enzyme activity and tests of synergism showed that diethyl maleate (DEM) made a synergistic ratio of 1.9 against chlorfenapyr, and glutathione S-transferase (GST) activity in JZ-NIL was 1.8-fold significantly higher than in the strain of Lab-S, indicating that GST-mediated metabolism contributes to chlorfenapyr resistance. In addition, pupation rate, fecundity, and hatchability were significantly lower in JZ-NIL than in Lab-S. The relative fitness of JZ-NIL was 0.54 compared with Lab-S. Overall, these results indicate that GST-mediated detoxification contributes to chlorfenapyr resistance in S. litura and that this resistance is associated with significant fitness costs. Further studies are needed to clarify the metabolic and target-site mechanisms underlying chlorfenapyr resistance.

PMID 42928584
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PubMedActa ophthalmologica2026-10-24

Therapeutic efficacy and systemic pharmacokinetics of a dual-drug hydrogel contact lens for sustained glaucoma therapy.

Varshitha Vangol V, Sankararajan Umadevi U

Conventional topical therapy for glaucoma is limited by poor ocular bioavailability, rapid precorneal drug loss, frequent dosing and systemic absorption through the nasolacrimal pathway, which may reduce therapeutic efficacy and increase the risk of adverse effects. Drug-eluting hydrogel contact lenses have emerged as a promising strategy to overcome these limitations by enabling sustained ocular drug delivery. This study aimed to evaluate the therapeutic efficacy, ocular biocompatibility and systemic pharmacokinetic profile of an optimized dual-drug-loaded HEMA-based hydrogel contact lens delivering timolol maleate (TM) and brimonidine tartrate (BT) for sustained glaucoma management. Optimized hydrogel contact lenses composed of 2-hydroxyethyl methacrylate (HEMA), N, N-dimethylacrylamide (DMA), N-vinylpyrrolidone (NVP) and ethylene glycol dimethacrylate (EGDMA) were fabricated by UV photopolymerization and loaded with TM and BT (4 mg/mL each). Ocular biocompatibility was assessed using the modified Draize irritation test. Therapeutic efficacy was evaluated in a steroid-induced ocular hypertension New Zealand White rabbit model by monitoring intraocular pressure (IOP) for 24 h. Systemic drug exposure was determined by validated high-performance liquid chromatography (HPLC) analysis of plasma samples, while ocular safety was further confirmed through histopathological examination. The optimized hydrogel lens exhibited excellent ocular biocompatibility, with a maximum Draize score of 0.33 ± 0.12 that resolved completely within 48 h and no histopathological evidence of ocular tissue damage. In hypertensive rabbits, the dual-drug hydrogel lens maintained normotensive IOP (16.1 ± 0.8 mmHg) for 24 h, representing a 43.5% reduction from baseline and significantly outperforming conventional eye drops beyond 4 h (p < 0.01). Plasma concentrations of both TM and BT remained below the limit of quantification (<2.0 ng/mL) throughout the study, whereas conventional eye drops produced measurable systemic exposure (TM: 18.4 ± 2.1 ng/mL; BT: 8.2 ± 1.2 ng/mL), demonstrating effective minimization of systemic drug absorption. The optimized dual-drug-loaded hydrogel contact lens provided sustained intraocular pressure reduction, excellent ocular biocompatibility and negligible systemic drug exposure compared with conventional topical therapy. These findings highlight its potential as a sustained ocular drug-delivery platform capable of improving therapeutic efficacy, reducing systemic adverse effects and enhancing long-term treatment adherence in glaucoma management. Further long-term preclinical investigations and clinical studies are warranted to support clinical translation.

PMID 42920388
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PubMedPesticide biochemistry and physiology2026-10-23

Inheritance and biochemical mechanism of abamectin resistance in a near-isogenic strain of Panonychus citri (Acari: Tetranychidae).

Liu Xun-Yan XY, Zhang Chun-Yu CY, Pan Deng D, Dou Wei W et al.

The citrus red mite, Panonychus citri, has developed severe resistance to the widely used pesticide like abamectin. Understanding the inheritance, cross-resistance profile, and biochemical mechanism of pesticide resistance in P. citri is critical for developing effective resistance management strategies. Here, we established an abamectin-resistant near-isogenic strain (NIL-Aba) by backcrossing the susceptible strain (SS strain) with a field collected abamectin-resistant strain (NN-Aba strain) for eight generations, coupled with continuous abamectin selection. The NIL-Aba strain exhibited 2278.44-fold resistance to abamectin relative to the SS strain, and showed cross-resistance with high level to emamectin benzoate (2841.04-fold) and pyridaben (115.21-fold), moderate level to fenpropathrin (15.37-fold) and cyflumetofen (10.73-fold). Genetic analysis indicated that abamectin resistance in NIL-Aba was autosomal, polygenic, and incompletely recessive. Synergist and enzyme activity assays demonstrated that piperonyl butoxide and triphenyl phosphate significantly inhibited abamectin resistance, with synergism ratios of 2.42- and 2.57- fold, respectively. Diethyl maleate produced a smaller synergistic effect (SR = 1.60). Furthermore, the NIL-Aba strain exhibited significantly higher activities of cytochrome P450 monooxygenases, carboxylesterases and glutathione S-transferases than the SS strain, indicating the involvement of three enzyme families in abamectin detoxification. The establishment of NIL-Aba provides a genetically controlled resource for dissecting the molecular basis of abamectin resistance in P. citri. These findings also provide a theoretical foundation for rotating abamectin with other pesticides, which is crucial for prolonging its efficacy in the field against P. citri and for optimizing resistance management strategies.

PMID 42919523
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PubMedEcotoxicology (London, England)2026-10-23

Unraveling acetamiprid resistance in Aphis craccivora (Hemiptera: Aphididae): resistance risk assessment, fitness costs, cross-resistance, biochemical and molecular characterization, and in silico docking study.

Aioub Ahmed A A AAA, Hashem Ahmed S AS, Ahmed Heba H R HHR, Alkeridis Lamya A LA et al.

Aphis craccivora Koch (Hemiptera: Aphididae) is a major sucking pest of legumes. Neonicotinoid insecticides are extensively utilized for A. craccivora control. The extended use of neonicotinoids, including acetamiprid (ACP) to manage A. craccivora, has led to the development of resistance. However, the potential to delay the development of ACP resistance in A. craccivora has not yet been investigated. Our study aimed to examine the development of ACP resistance in A. craccivora over 20 generations, and the associated heritability (h2), fitness costs, biochemical mechanisms, and potential cross-resistance were evaluated. Gene expression of GST and Cyp-450 was measured under ACP exposure, and molecular docking of ACP with these proteins in the presence of diethyl maleate (DEM) and piperonyl butoxide (PBO) was analyzed. Our data showed that the ACP-resistant (ACP-R) strain of A. craccivora showed a 25.57-fold enhancement in LC₅₀ compared to the Sus-strain, with realized heritability (h²) of 0.21 and reduced fitness (0.69). The net reproduction rate (R0), mean relative growth rate (MRGR), intrinsic rate of increase (r), and finite rate of increase (λ) were markedly lower in the ACP-R strain than in the Sus-strain of A. craccivora. Upregulation of Cyp-450 (CYP18A1, CYP4CJ14) and GST (GSTS3, GSTO1) genes enhanced enzyme activity, while Car-E showed no significant correlation with ACP susceptibility. Enzyme inhibitors PBO and DEM increased ACP toxicity, and molecular docking suggested their interaction with Cyp-450 and GST proteins contributes to resistance. Our findings offer key insights into ACP resistance in A. craccivora, supporting the development of management strategies and decision-making tools.

PMID 42911287
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PubMedJournal of Korean medical science2026-10-13

Superior Efficacy of Besifovir in Reducing Hepatocellular Carcinoma Risk Compared to Tenofovir in Chronic Hepatitis B Patients: A Nationwide Cohort Study.

Shin Yoon E YE, Kim Jae Young JY, Kim Hyuk H, Yoo Jeong-Ju JJ et al.

Besifovir dipivoxil maleate (BSV) is a novel therapeutic option for the treatment of chronic hepatitis B (CHB). However, its long-term effectiveness in reducing the risk of hepatocellular carcinoma (HCC) remains unclear. We conducted a retrospective cohort study using the Korean Health Insurance Review and Assessment Service database from 2018 to 2022. A total of 32,383 patients with CHB were included (BSV, n = 2,358; tenofovir disoproxil fumarate [TDF], n = 30,025). Propensity score matching was conducted at a 1:3 ratio to minimize selection bias. The primary outcome was the incidence of HCC, with cirrhosis development as the secondary endpoint. In the overall population, 57 cases of HCC were reported in the BSV group (2,358 individuals, 5,918 person-years), while 1,268 cases of HCC were reported in the TDF group (30,025 individuals, 83,587 person-years). After propensity score matching, the incidence of HCC was significantly lower in the BSV group (9.63 per 1,000 person-years; 95% confidence interval [CI], 7.43-12.49) than in the TDF group (15.36 per 1,000 person-years; 95% CI, 13.72-17.18), with an incidence rate ratio of 1.59 (P = 0.001). This protective effect remained consistent in both cirrhotic (hazard ratio [HR], 1.609; P = 0.028) and non-cirrhotic subgroups (HR, 1.831; P = 0.002). BSV treatment demonstrated superior efficacy in reducing the risk of HCC compared to TDF, regardless of baseline cirrhosis status. These findings suggest that BSV may provide enhanced protection against HCC in patients with CHB.

PMID 42865284
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PubMedRevista peruana de medicina experimental y salud publica2026-10-13

Hampi Tariki Kit: thin-layer chromatography for semiquantitative screening of solid oral medicines in Peru.

Mónico-Rosales Gladys M GM, Mostacero-Rodríguez Fredy R FR, Quispe-Paitán B Rosa BR, Rodríguez-Calzado E Javier EJ et al.

To develop and validate rapid thin-layer chromatography (TLC) methods integrated into the Hampi Tariki kit for the semiquantitative screening of active pharmaceutical ingredients (APIs) in oral solid medications marketed in Peru. Eight TLC methods were developed and validated for tablets and capsules containing acyclovir, dicloxacillin, dimenhydrinate, ibuprofen, diclofenac sodium, paracetamol, norfloxacin, phenazopyridine hydrochloride, chlorphenamine maleate, and phenylephrine hydrochloride. Fifty-seven commercial samples available in the national market, from different manufacturing laboratories, including branded and generic products previously verified as compliant by official methods at the Centro Nacional de Control de Calidad (CNCC) of the Instituto Nacional de Salud (INS), were evaluated. Silica gel 60 F254 plates, reference standards, and analytical grade solvents were used. Validation was performed according to ICH Q2(R1) guideline, evaluating selectivity, linearity, precision, accuracy, visual detection limit, and robustness. The methods allowed for visual and densitometric differentiation of levels equivalent to 80%, 100%, and 120% of the declared content. Retention factor (Rf ) values were between 0.20 and 0.85, and multicomponent formulations presented chromatographic resolution ≥1.0. Correlation coefficients were greater than 0.99 for system and method linearity; repeatability showed coefficients of variation less than 3.0%, intermediate precision less than 5.0%, and bias against high-performance liquid chromatography (HPLC) remained within the ±3.00% range. Deliberate variations evaluated in robustness did not produce significant changes in Rf values. The developed methods demonstrated adequate analytical performance as rapid semiquantitative screening tests. Integrated into the Hampi Tariki kit, they constitute a proposal with potential to support the preliminary identification of suspicious samples and prioritize their confirmation by HPLC or other official methods.

PMID 42867952
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