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tafluprost + timolol maleate (Tapucom / STN 10111 / STN 1011101)

✓ Approved

Santen Pharmaceutical Co., Ltd. · ADRB1 · 小分子

什么是 tafluprost + timolol maleate？

tafluprost + timolol maleate 是一种小分子，由Santen Pharmaceutical Co., Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Others、Topical。

药物档案

商品名Tapucom, STN 10111, STN 1011101
公司Santen Pharmaceutical Co., Ltd.
药物类别小分子
分子靶点ADRB1, ADRB2, PTGFR
给药途径Others, Topical
状态Approved
来源： ClinicalTrials.gov, Santen Pharmaceutical Co., Ltd.

作用机制

分子靶点

tafluprost + timolol maleate 作用于 3 个分子靶点：

ADRB1adrenoceptor beta 1 (B1AR, RHR)
ADRB2adrenoceptor beta 2 (ADRBR, B2AR)
PTGFRprostaglandin F receptor (FP)
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

tafluprost + timolol maleate 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Eye disordersGlaucoma✓ Approved

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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PubMedAmerican journal of ophthalmology case reports2026-10-25

Recurrent delayed hyphema following latanoprost/netarsudil initiation in an eye with a XEN 63 gel stent: a case report.

Greco Antonio A, Calabresi Valerio V, Marenco Maria M, Garavelli Fabio F et al.

To describe recurrent delayed hyphema following initiation of fixed-dose latanoprost/netarsudil in an eye with a previous XEN 63 gel stent, and to discuss whether the associated IOP reduction may have unmasked a pre-existing peri-implant reflux pathway. A 72-year-old woman with advanced primary open-angle glaucoma and previous ab interno XEN 63 gel stent implantation developed recurrent spontaneous hyphema shortly after bimatoprost/timolol was replaced with latanoprost/netarsudil. Intraocular pressure decreased from 17-19 mmHg to 8-9 mmHg after treatment initiation. The first episode occurred nine days later, with blurred vision, a small anterior chamber hyphema, and fine endothelial blood deposits. Gonioscopy showed active blood reflux from tissue surrounding the proximal intracameral XEN segment, without bleeding from other angle structures. Recurrent episodes occurred despite conservative management and, subsequently, despite discontinuation of latanoprost/netarsudil. Because the peri-implant region was repeatedly identified as the reflux site, the XEN stent was eventually removed. No further bleeding episodes were observed after explantation. The clinical course is consistent with a susceptible peri-implant anatomical configuration contributing to recurrent blood reflux. The temporal association between latanoprost/netarsudil initiation, marked IOP reduction, and the first hyphema suggests a possible precipitating or unmasking role, but does not establish drug causality. Delayed or recurrent hyphema after XEN implantation should prompt review of recent medication changes and careful gonioscopic inspection of the proximal XEN segment.

PMID 42927338
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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 the Chinese Medical Association : JCMA2026-10-14

Nonselective beta-blockers and hepatic encephalopathy in liver cirrhosis:A meta-analysis of randomized controlled trials.

Kuo Tai-Hui TH, Chen Yu-Jen YJ, Lee Pei-Chang PC, Yang Tsung-Chieh TC et al.

Liver cirrhosis leads to portal hypertension and related complications, including ascites, esophageal varices, and hepatic encephalopathy (HE). Non-selective beta blockers (NSBBs) decrease portal pressure, but it is not yet clear whether they contribute to HE development. Therefore, we examined the association between NSBB therapy and HE in randomized controlled trials (RCTs) involving patients with cirrhosis. We systematically searched PubMed, Web of Science, ScienceDirect, and the Cochrane Library (from inception to December 31, 2024) for RCTs comparing NSBBs with a placebo, endoscopic band ligation, or injection sclerotherapy for variceal bleeding prevention in relation to HE. The risk ratios (RRs) and 95% confidence intervals (CIs) were pooled using a random-effects model. Subgroups were defined according to the comparator, NSBB type, and hepatic function status (weighted mean Child-Pugh score ≤6 vs. >6). The risk of bias was assessed using the revised Cochrane risk-of-bias tool for randomized trials (RoB 2). There were 12 relevant studies, which included 775 NSBB-treated and 771 comparator patients (54 and 57 HE events). NSBB therapy was not associated with a statistically significant change in HE risk (RR 1.04, 95% CI 0.73-1.47; p = 0.84; I² = 0%). Estimates were consistent across all subgroups of hepatic function statuses (compensation, RR 1.18, 0.44-3.14; decompensation, RR 1.02, 0.70-1.48; p = 0.79), comparators (placebo, RR 1.19, 0.79-1.80; endoscopic therapy, RR 0.72, 0.38-1.39; p = 0.20), and NSBB types (propranolol/timolol, RR 1.06, 0.72-1.55; carvedilol, RR 0.95, 0.42-2.15; p = 0.82). Current evidence does not indicate a statistically significant association between NSBB therapy and HE development in patients with cirrhosis, regardless of disease severity.

PMID 42870342
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