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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

PubMedThe Journal of organic chemistry2026-07-27

Catalytic Hydrosulfenylation of Maleic Anhydride and Its Derivatives Enabled by Proton-Coupled Electron Transfer.

Peng Dong D, Sun Jiayi J, Huang Yun Y, Zeng Xianghua X

We herein report a practical method for the efficient hydrosulfenylation of maleic anhydride and its derivatives by decavanadate-induced proton-coupled electron transfer. Preliminary mechanistic studies suggest that a thiyl radical is generated from the decavanadate polyanion and thiol through an oxidative PCET process. This method utilizes readily available thiols as a sulfur source and air as an oxidant and is capable of hydrosulfenylating a variety of maleic anhydrides and maleate esters with good diastereoselectivity.

PMID 42503765
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PubMedGels (Basel, Switzerland)2026-07-27

Construction of PEGMC Copolymerized Modified Hydrogel and Its Mechanism for Salt Retardation and Nutrient Immobilization in Dryland Soil.

Cheng Jianwei J, Xiang Rui R, Liu Jingcai J, Yang Baocun B et al.

Aiming at severe soil secondary salinization, poor water retention and insufficient salt tolerance of conventional acrylic-based modifiers in arid and semi-arid regions of China, a poly(ethylene glycol) maleate citrate (PEGMC) crosslinking monomer was synthesized through esterification, and a dual covalent-hydrogen crosslinked P(PEGMC/AA) hydrogel was fabricated via free radical copolymerization with acrylic acid (AA). The hydrogel was characterized by NMR, FTIR, SEM, TGA and elemental mapping, while its binding mechanism with saline-alkali ions was elucidated through DFT calculations and molecular dynamics simulations. Its amelioration performance was evaluated through swelling, soil water retention, desalination and pot germination experiments. The hydrogel exhibited outstanding water absorbency, salt resistance and dry-wet cycling stability, with swelling ratios of 712 g/g in deionized water and 285 g/g in 0.9% NaCl solution, and remained 200 g/g after four dry-wet cycles. It enhanced soil water retention remarkably (over 93% after 72 h). At 0.30% dosage, soil salt content declined from 7.1 g/kg to 1.3 g/kg with desalination efficiency exceeding 80%, owing to porous physical adsorption and chemical chelation toward Na+, Ca2+ and Mg2+, with a binding energy of -136.936 kJ/mol. Pot tests revealed that crop germination rate rose from 19% (blank) to 75% under severe saline-alkali stress. Meanwhile, the hydrogel inhibited nutrient leaching and favored soil-water conservation. This work first incorporated PEGMC monomer into agricultural hydrogels to construct a stable dual crosslinked network, clarifying its synergistic mechanisms for salt fixation and water retention macroscopically and microscopically. It provides a promising functional material and theoretical basis for green, efficient in situ amelioration of dryland saline-alkali soil.

PMID 42505278
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PubMedFASEB journal : official publication of the Federation of American Societies for Experimental Biology2026-07-25

Syringaresinol Attenuates Aging-Associated Ferroptosis-Relevant Stress Through an HIF-1α-GPX4 Defense Axis.

Li Ya-Ping YP, Huang Fei-Hong FH, Wu Meng-Ting MT, Chen Meng-Yi MY et al.

Ferroptosis contributes to aging-associated functional decline, yet compounds with robust organismal efficacy and defined upstream regulatory mechanisms remain limited. Here, we established a diethyl maleate (DEM)-induced glutathione depletion model in wild-type (N2) Caenorhabditis elegans as a survival-based screening platform and identified syringaresinol (Syr) as a leading hit from an in-house small-molecule library. In nematodes, Syr improved survival under DEM challenge, reduced lipid peroxidation, reactive oxygen species (ROS), and malondialdehyde levels, and alleviated age-associated oxidative lipid stress and iron imbalance during natural aging, accompanied by extended lifespan and improved healthspan-related phenotypes. In primary human foreskin fibroblasts, Syr conferred dose-dependent protection against RSL3- or erastin-induced ferroptosis, preserved cellular integrity, suppressed lipid peroxidation and ROS, and restored expression of GPX4, SLC7A11, and ferritin. In two senescence models, Syr also attenuated senescence-associated phenotypes and ferroptosis-related oxidative lipid stress, concomitant with recovery of GPX4 expression. Network-based prediction and functional perturbation identified HIF-1α as a candidate mediator of Syr-associated cytoprotection. HIF-1α knockdown weakened Syr-mediated protection and largely prevented GPX4 restoration, whereas GPX4 knockdown did not alter HIF-1α abundance. These findings support a functional HIF-1α-GPX4 defense axis in fibroblasts, while direct transcriptional regulation remains to be clarified. Overall, Syr attenuates ferroptosis-relevant oxidative lipid stress and aging-associated phenotypes in C. elegans and human fibroblast models, supporting further mechanistic and mammalian in vivo validation.

PMID 42501322
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PubMedPediatric dermatology2026-07-24

A Comprehensive Review of the Current Systemic Medical Treatment Landscape for Vascular Malformations.

Fason Claire C, Jafari Alexander J AJ, Hebert Adelaide A AA

Dermatologists play a central role in the diagnosis and medical management of vascular anomalies. Currently, vascular anomalies are categorized into vascular tumors and vascular malformations. The latest designations for the numerous types of vascular lesions are delineated in the International Society for the Study of Vascular Anomalies website (www.issva.org). The arenas for the therapy for hemangiomas, the most common vascular tumor, have been studied extensively and have been recognized as standard of care by the Society for Pediatric Dermatology, the American Academy of Dermatology and the American Academy of Pediatrics. Options for hemangioma treatment include systemic beta-blockers such as propranolol, atenolol, and nadolol, and the topical beta-blocker timolol. Vascular malformations and overgrowth syndromes encompass a separate set of treatment regimens. Recent pharmacological and technological advances in the medical management of vascular anomalies have decreased the need for surgery in many patients while also leading to improved outcomes and quality of life. This review will guide the dermatologist through the current medical treatment landscape for vascular malformations.

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PubMedJournal of colloid and interface science2026-07-24

Core-shell structure driving bimetallic synergy promotes the high-efficiently synergistic catalytic removal of chlorobenzene and NO.

Zhao Liming L, Liu Jing J, Yang Yingju Y, Guan Zelin Z et al.

The development of bifunctional catalysts for the simultaneous removal of chlorobenzene and nitric oxide still remains an extremely challenging objective, owing to the intrinsic trade-off effect between selective catalytic reduction (SCR) and catalytic oxidation. Herein, a strategy to enhance the SCR activity and catalytic degradation ability of chlorobenzene was proposed through boosting the metal-metal interaction in the core-shell structure. The designed SiO2@CoMn2O4 core-shell catalyst with multi-active centers showed excellent synergistic elimination of NO and chlorobenzene at a temperature range of 300-320 °C. While NH3 was found to inhibit chlorobenzene oxidation, chlorobenzene had little effect on the SCR activity of SiO2@CoMn2O4 but had a positive effect on N2 selectivity. The combination of core-shell structure and bimetallic synergy well balances activity and selectivity. SiO2 core significantly enriches surface acid sites and increases the specific surface area, facilitating reactant adsorption and activation. The synergistic effect between Co and Mn ions balances the types of surface oxygen species and increased the amount of lattice oxygen, facilitating NO oxidation activity, adsorption of chlorobenzene and CCl bond cleavage. The simultaneous removal mechanism of NO and chlorobenzene was investigated through in situ diffuse reflectance Fourier transform infrared spectroscopy (DRIFTS) and theoretical calculations. Chlorobenzene undergoes dichlorination to form phenyl group with assistance of the electron-withdrawing property of Lewis acid, which then reacts with reactive oxygen species through electrophilic attack to yield intermediates such as benzoquinone, maleate, and acetate.

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PubMedAmerican journal of translational research2026-07-23

Esomeprazole plus trimebutine maleate improves symptoms, esophageal function, and acid control without increasing risks in elderly GERD: a real-world retrospective study.

He Bo B, Xing Rui R, Zhang Honglian H

Elderly patients with gastroesophageal reflux disease (GERD) often exhibit inadequate response to proton pump inhibitor monotherapy due to accompanying motility disorders. This study evaluated the real-world safety and efficacy of esomeprazole (EMZ) combined with trimebutine maleate (TM) in this population. This retrospective analysis included elderly GERD patients treated at The People's Hospital of Yongcheng from July 2022 to June 2025, categorized into EMZ monotherapy and EMZ + TM combination groups. Symptom efficacy and GerdQ scores were assessed at baseline, 4 and 8 weeks. Esophageal motility, 24-hour pH monitoring, inflammatory markers, liver and kidney function, and adverse reactions were evaluated before and after 8 weeks. A total of 184 patients were included (86 monotherapy, 98 combination). The combination group showed a higher total effective rate and lower GerdQ scores at 4 weeks and 8 weeks (all P<0.05). After 8 weeks, lower esophageal sphincter resting pressure, lower esophageal sphincter relaxation rate, and distal contractile integral were significantly higher, while ineffective contractions and total acid exposure time were significantly lower in the combination group (all P<0.05). Inflammatory markers were also significantly lower (all P<0.05). No significant differences in liver, kidney function, or adverse reactions were observed. Adding TM to EMZ improves symptom control, esophageal motility, acid exposure, and inflammatory markers in elderly GERD patients without compromising safety.

PMID 42491019
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