若生智能
Drug Database
TA

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

PubMedInflammopharmacology2026-06-12

Chemical characterization and antinociceptive and anti-inflammatory activities of the aqueous extract of Myrciaria floribunda (H. West ex Willd.) O. Berg fruit peel.

De Freitas Rosa Simone Patricia SP, da Silva Santos Izabelly Bianca IB, Pereira Wendel César eSilva WCE, de Souza Thaís Vitória Freitas TVF et al.

Natural products derived from medicinal plants represent an important source of bioactive compounds with potential therapeutic applications in the management of pain and inflammatory disorders. In this study, the chemical profile and pharmacological activities of the aqueous extract obtained from the fruit peel of Myrciaria floribunda (AeMf) were investigated. Chemical characterization was performed using high-performance liquid chromatography coupled with electrospray ionization mass spectrometry (HPLC-ESI-MSⁿ). The antinociceptive activity of AeMf was evaluated in mice using acetic acid-induced abdominal writhing, formalin, and tail immersion tests, while the anti-inflammatory potential was assessed through carrageenan-induced paw edema and peritonitis models. Chromatographic analysis revealed a chemical profile predominantly composed of organic acids and related metabolites, including quinic acid, citrate, maleate, and a fatty acid hexoside. In nociceptive models, AeMf produced a significant and dose-dependent reduction in acetic acid-induced writhing and markedly decreased paw-licking behavior in both phases of the formalin test. In addition, the extract increased tail withdrawal latency in the thermal nociception assay, indicating the involvement of both peripheral and central analgesic mechanisms. In inflammatory models, AeMf significantly inhibited carrageenan-induced paw edema, reduced leukocyte and neutrophil migration to the peritoneal cavity, and markedly suppressed the production of pro-inflammatory cytokines, including TNF-α and IL-1β. Collectively, these findings demonstrate that AeMf exerts potent antinociceptive and anti-inflammatory effects, likely mediated through the modulation of inflammatory mediators and cellular recruitment. The results highlight the therapeutic potential of Myrciaria floribunda as a promising natural source of bioactive compounds for the development of novel strategies for pain and inflammation management.

PMID 42283803
阅读全文 →
PubMedScientific reports2026-06-11

Green and applicable chromatographic approaches for the estimation of a multi-component cold and flu relief formulation along with in-vitro dissolution profiling.

Nabil Mona M, Marzouk Hoda M HM, Abbas Samah S SS, Lotfy Hayam M HM et al.

The emergence of novel pharmaceutical formulations requires the establishment of a reliable analytical method that can accurately quantify active ingredients for use in diverse quality control applications. An over-the-counter pharmaceutical combination of phenylephrine hydrochloride (PHE), chlorpheniramine maleate (CPM), and ibuprofen (IBU) is formulated to treat allergy, lessen fever, and relieve congestion. Two efficient and applicable liquid chromatographic methodologies were established, with an emphasis on ecological sustainability while preserving analytical precision and accuracy, in addition system suitability parameters were successfully determined for each method. The first approach involved high-performance thin-layer chromatography (HPTLC) combined with densitometric quantification, employing silica gel HPTLC 60 F254 aluminum sheets as the stationary phase. The developing system comprised ethyl acetate-methanol-aqueous ammonium hydroxide (8.0:2.0:0.1, by volume), and scanning was carried out at 265.0 nm. The respective resolutions (Rs) were 8.44 and 4.57 for PHE, IBU, and CPM, respectively. The second one is high-performance liquid chromatographic methodology (HPLC), whereas, efficient separation was achieved on a Kromasil 60-5-CN column using isocratic elution of 10.0 mM ammonium acetate buffer and ethanol (50: 50, v/v), adjusted with acetic acid to pH 2.5 at a flow rate of 1.3 mL/min, with DAD quantification at 265.0 nm, with overall run time about 6 min to achieve sufficient separation among the target analytes. The resolutions (Rs) were determined to be 7.62 and 3.21 for PHE, CPM, and IBU, respectively. The investigated approaches' performance was validated in adherence to the guidelines established by the International Conference on Harmonization guidelines, confirming its reliability for analytical application. Limit of detection (LOD) values were determined to be 0.02, 0.01, and 0.22 µg/band for PHE, CPM, and IBU, respectively in HPTLC method, whilst in HPLC-DAD method, LOD values were 0.03, 0.01, and 0.24 µg/mL for PHE, CPM, and IBU, respectively. These approaches can concurrently estimate the cited drugs in their raw forms, as well as their pharmaceutical combination. In addition, HPLC can monitor their dissolution profiles. Moreover, the applicability profile and ecological sustainability of the studied approaches were verified via employing up-to-date evaluation tools, along with comparisons against official and reported methodologies.

PMID 42270807
阅读全文 →
PubMedBMC public health2026-06-07

Regional health inequalities of anticancer drug accessibility under the National Drug Price Negotiation in China: a decomposition analysis.

Tuo Bingbing B, Jiang Junnan J, Zhao Haokai H, Mao Yiqing Y et al.

Equitable access to anticancer drugs is a central concern in oncology care. China initiated National Drug Price Negotiation (NDPN) in 2016, which has been associated with improved accessibility and equity in anticancer drugs. This study aims to evaluate the current regional equity in the provision of negotiated anticancer drugs in China. The study collected data on the availability of anticancer drugs negotiated by public platforms across 31 provinces. We collected province-level data on the availability of negotiated anticancer drugs in hospitals and pharmacies across 31 provinces and calculated GDP-related concentration indices (CIs). A decomposition analysis of CIs was conducted to identify determinants of inequity, and CIs were further computed within the breast cancer subgroup. The CIs were 0.125 for hospitals and 0.139 for pharmacies, indicating pro-rich inequality in the regional provision of negotiated anticancer drugs, with higher-income eastern regions offering more hospitals and pharmacies with anticancer drugs. Medical insurance expenditures (56.209%) and inpatient costs (46.745%) exacerbated hospital supply inequality. The number of pharmacists in pharmacies (63.845%) was the primary positive contributor to pharmacy access inequality. Among breast cancer drugs, Abemaciclib and Nalatinib Maleate exhibited higher CIs of 0.244 and 0.223. The regional distribution of negotiated anticancer drugs reveals substantial disparities, with affluent regions more likely to access these medications through well-resourced hospitals and pharmacies. Health expenditure and financing mechanisms further amplify these inequalities. Even within similar indications, disparities persist in the availability of different drugs. Future initiatives should prioritize measures to ensure drug access in impoverished and remote areas.

PMID 42251294
阅读全文 →
PubMedCureus2026-06-05

Postoperative Eyelid Pyogenic Granuloma: A Systematic Review of Clinical Features, Surgical Associations, and Management.

Cheung Imogen I, Cheung David D

Pyogenic granuloma (lobular capillary haemangioma) is a benign vascular lesion that may arise following trauma, inflammation, or surgery. In oculoplastic practice, it represents a recognised but likely underreported postoperative complication. We present a case of recurrent pyogenic granuloma arising from a posterior lamellar defect following eyelid reconstruction using a Hughes flap, highlighting key clinical features and management considerations. A systematic review of the literature was also performed to contextualise this case, identifying 14 studies comprising 498 cases. Lesions typically presented within weeks of surgery as rapidly growing, friable, pedunculated masses arising at sites of surgical disruption. While topical therapies such as corticosteroids and timolol may be effective in selected cases, surgical excision remains the most reliable treatment and allows histological confirmation. This case and systematic review support the theory that postoperative pyogenic granuloma represents a manifestation of dysregulated wound healing driven by aberrant angiogenesis at sites of epithelial disruption.

PMID 42245883
阅读全文 →
PubMedThe EMBO journal2026-06-04

Molecular architecture of OXGR1 reveals an evolutionary conserved mechanisms for metabolite surveillance.

Zhang Xinyue X, Lu Yujie Y, He Xinheng X, Guo Shimeng S et al.

The ability of cells to sense and respond to metabolic signals is fundamental to life, yet the molecular mechanisms underlying metabolite surveillance remain incompletely understood. Here, we elucidate the structural basis of metabolite recognition by OXGR1, a G Protein-Coupled Receptor (GPCR) that senses key intermediates in the tricarboxylic acid (TCA) cycle. Using cryo-electron microscopy, we determined cryo-EM structures of OXGR1 bound to α-ketoglutarate (AKG), itaconate (ITA), and structurally related metabolites succinate (SUC) and maleate (MA). These structures reveal a positively charged binding pocket and an extensive hydrogen-bond network that mediate selective recognition of dicarboxylic acids. In addition, we identify a distinct arrangement of hydrophobic residues that modulates ligand potency and selectivity. Mutational analysis and molecular dynamics simulations further demonstrate that noncanonical micro-switch motifs, including FRY and NLxxY, are essential for ligand recognition and receptor activation. Comparative structural and evolutionary analyses indicate that these mechanisms are conserved across species, underscoring the critical role of OXGR1 in maintaining metabolic homeostasis. Together, our findings define a mechanistic framework for metabolite sensing by OXGR1 and provide a framework for therapeutic modulation of metabolic and inflammatory diseases.

PMID 42236546
阅读全文 →
PubMedClinical ophthalmology (Auckland, N.Z.)2026-06-03

A Comprehensive Review of the Clinical Evidence Comparing Benzalkonium Chloride-Preserved and Benzalkonium Chloride-Free Latanoprost in the Treatment of Primary Open-Angle Glaucoma and Ocular Hypertension.

Kumar Harsh H, Parikh Rajul R, Chagani Amyn A, Bhojani KomelAbbas G KG et al.

This review aims to consolidate and evaluate the clinical evidence on the efficacy and safety of benzalkonium chloride (BAK)-preserved and BAK-free latanoprost in the treatment of primary open-angle glaucoma (POAG) and ocular hypertension (OHT). The primary research question addresses whether BAK-free formulations offer comparable efficacy with improved safety profiles compared to BAK-preserved formulations. An extensive literature search was conducted using PubMed up to February 2025. Keywords included "latanoprost", "primary open-angle glaucoma", "ocular hypertension", "efficacy", and "safety". Inclusion criteria were peer-reviewed clinical trials and meta-analyses comparing latanoprost with placebo or other treatments (eg. bimatoprost, travoprost, tafluprost, latanoprostene bunod). Exclusion criteria included observational studies, review articles, and studies comparing preservative-free prostaglandin analogues and omidenepag. Thirty-two studies (17 randomized clinical trials and 7 meta-analyses) were reviewed. Latanoprost, the first FDA-approved prostaglandin analogue, primarily increases uveoscleral outflow. Comparative studies indicate that latanoprost achieves a good balance between IOP reduction and tolerability compared to bimatoprost, travoprost, tafluprost, and unoprostone. Latanoprost also reduces visual field progression and maintains central corneal thickness (CCT). It improves ocular perfusion pressure (OPP), reducing the risk of glaucomatous optic neuropathy. Safety profiles show fewer side effects, such as conjunctival hyperemia, hypertrichosis, and periocular pigmentation, compared to other PGAs. BAK-free formulations demonstrate improved corneal health and patient compliance due to reduced ocular surface toxicity. Latanoprost remains a first-line therapy for POAG and OHT due to its efficacy, safety, and patient adherence. The availability of BAK-free formulations enhances its therapeutic profile, with reduced corneal toxicity making it a preferred choice for long-term glaucoma management.

PMID 42232614
阅读全文 →

注册免费账户还可查看另外 9996 篇文献

免费注册查看全部文献 →

了解更多tafluprost + timolol maleate